Page last updated: 2024-11-04

ofloxacin

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Description

Ofloxacin is a synthetic broad-spectrum antibacterial drug that belongs to the fluoroquinolone class. It works by inhibiting the activity of bacterial DNA gyrase, an enzyme essential for DNA replication and repair, leading to bacterial cell death. It is effective against a wide range of gram-positive and gram-negative bacteria, including those responsible for urinary tract infections, respiratory infections, skin infections, and gastrointestinal infections. Ofloxacin is often studied due to its high efficacy, oral bioavailability, and relatively low cost compared to other antibiotics. It is also being investigated for its potential in treating various other conditions, such as malaria, tuberculosis, and certain types of cancer. However, concerns regarding its potential for adverse effects, such as tendonitis, cartilage damage, and central nervous system disturbances, have led to restrictions in its use in some countries.'

Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID4583
CHEMBL ID4
CHEBI ID7731
CHEBI ID194135
SCHEMBL ID24373
SCHEMBL ID14163982
MeSH IDM0023430

Synonyms (251)

Synonym
ofloxacin otic
floxin in dextrose 5%
ccris 5233
ofloxacinum [latin]
dl 8280
ofloxacine
oxaldin
ofloxacino [spanish]
brn 3657947
ofloxacine [french]
(+-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid
7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 2,3-dihydro-9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-, (+-)-
floxin in dextrose 5% in plastic container
orf 18489
ofloxacina [dcit]
visiren
7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-, (+-)-
oflocet
pt 01
MLS001074203
bdbm50045004
HMS3393K06
AB00052263-13
AB00052263-12
BRD-A24228527-001-05-9
DIVK1C_000721
KBIO1_000721
exocine
hoe-280
wp-0405
tarivid
floxin otic
MLS000028749 ,
smr000058192
EU-0100904
ofloxacin, fluoroquinolone antibiotic
SPECTRUM_001186
OPREA1_242882
NCGC00178284-02
NCGC00178284-01
PRESTWICK2_000237
SPECTRUM5_001063
IDI1_000721
BSPBIO_003117
LOPAC0_000904
hoe 280
(+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
floxin
zanocin
ofx
dl-8280
oflx
ocuflox
exocin
AB00513820
C07321
82419-36-1
ofloxacin
8-fluoro-3-methyl-9-(4-methyl-piperazin-1-yl)-6-oxo-2,3-dihydro-6h-1-oxa-3a-aza-phenalene-5-carboxylic acid
DB01165
ofloxacin (jp17/usp/inn)
D00453
floxin (tn)
NCGC00094219-04
NCGC00094219-03
NCGC00094219-02
NCGC00094219-05
KBIO3_002617
KBIOSS_001666
KBIOGR_000667
KBIO2_006802
KBIO2_004234
KBIO2_001666
SPBIO_002234
SPECTRUM4_000324
SPBIO_001387
SPECTRUM2_001464
SPECTRUM3_001499
PRESTWICK1_000237
PRESTWICK0_000237
NINDS_000721
SPECTRUM1502044
PRESTWICK3_000237
BSPBIO_000313
nsc-727071
(+/-)-floxin
nsc727071
(+/-)-9-fluoro-2,2,3-de)-1,4-benzoxazine-6-carboxylic acid
BPBIO1_000345
NCGC00094219-01
NCGC00094219-06
dl8280
STK256723
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
NCGC00015772-02
O 8757 ,
ofloxacine; dl-8280; hoe-280
HMS2092B10
AC-7616
HMS2090F07
NCGC00015772-10
CHEMBL4 ,
j01ma01
nsc-758178
HMS502E03
ofloxacino
ofloxacinum
CHEBI:7731 ,
HMS1921H12
HMS1568P15
CHEBI:194135
AKOS001033517
HMS2095P15
HMS3262F10
HMS3259G07
unii-a4p49jaz9h
(+-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido(1,2,3-de)(1,4)benzoxazin-6-carbonsaeure
ofloxacin [usan:usp:inn:ban:jan]
hsdb 8030
nsc 758178
7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-
nsc 727071
a4p49jaz9h ,
BBL005605
nsc758178
pharmakon1600-01502044
tox21_110703
dtxcid1021085
dtxsid3041085 ,
ofloxacina
HMS2235C05
CCG-39210
NCGC00015772-07
NCGC00015772-03
NCGC00015772-09
NCGC00015772-04
NCGC00015772-05
NCGC00015772-06
NCGC00015772-08
BCP9000851
floxil
flobacin
FT-0670773
FT-0673216
F0472-0226
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2h-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
FT-0630905
FT-0627808
NCGC00015772-13
LP00904
EPITOPE ID:116889
S1463
HMS3369B01
F0020-0095
9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido(1,2,3-de)(1,4)benzoxazine-6-carboxylic acid, dl-
ofloxacin [who-dd]
ofloxacin [usp-rs]
ofloxacin [jan]
ofloxacin [inn]
ofloxacin [mart.]
ofloxacin [ep monograph]
ofloxacin [usan]
ofloxacin [vandf]
ofloxacin [usp monograph]
7h-pyrido(1,2,3-de)-1,4-benzoxazine-6-carboxylic acid, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-, (+/-)-
ofloxacin [orange book]
ofloxacin [mi]
HY-B0125
CS-1891
9-fluoro-3,7-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2h-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
NC00466
O0403
AKOS016042783
SCHEMBL24373
NCGC00015772-12
tox21_110703_1
KS-5011
SCHEMBL14163982
NCGC00261589-01
ofloxacin, antibiotic for culture media use only
tox21_500904
O-2800
9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7h-pyrido [1,2,3-de]-1,4-benzoxazin-6-carboxylic acid
9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
GSDSWSVVBLHKDQ-UHFFFAOYSA-N
9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7h-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid
MLS006011774
9-fluoro-3-methyl-10-(4-methylpiperazino)-7-oxo-2,3-dihydro-7h-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid
HMS3604B17
OPERA_ID_1114
AB00052263_14
AB00052263_15
mfcd00226105
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
VU0243192-7
(+/-)-9-fluoro-2, 3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
SR-01000076050-1
sr-01000076050
ofloxacin, vetranal(tm), analytical standard
ofloxacin, united states pharmacopeia (usp) reference standard
ofloxacin, pharmaceutical secondary standard; certified reference material
ofloxacin, european pharmacopoeia (ep) reference standard
83380-47-6
SR-01000076050-4
SR-01000076050-7
SBI-0050879.P003
HMS3712P15
rkl10083
Z56761309
(-)-(s)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1;(-)-(s)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7h-pyrido[1,2,3-de]-1
BCP22048
(s)-ofloxacin;levaquin;quixin
Q411447
dl-ofloxacin
monoflocet
ofloxacin (floxin)
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13),11-tetraene-11-carboxylic acid
ofloxacin,(s)
ofloxacin 100 microg/ml in acetonitrile
BCP14346
8-methyl-2,3-dihydrofuro[3,2-e]imidazo-[1,2-c]pyrimidine-9-carboxylicacid
AMY22220
BRD-A24228527-001-19-0
SDCCGSBI-0050879.P004
NCGC00015772-22
SY007392
gtpl10918
exocin (eye drops)
SR-01000076050-16
A864414
7-chloro-4-hydroxy-8-methylquinoline-3-carboxylicethylester
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-3,7-dihydro-2h-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylicacid
EN300-06482
7-fluoro-2-methyl-6-(4-methylpiperazin-1-yl)-10-oxo-4-oxa-1-azatricyclo[7.3.1.0,5,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid
1ST5740
SY052697
olfoxacin otic soln
ofloxaxin
ofloxacin ophth soln
ofloxacin (mart.)
ofloxacin (usp monograph)
ofloxacin (usan:usp:inn:ban:jan)
(3rs)-9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-pyrido(1,2,3-de)(1,4)benzoxazine-6-carboxylic acid
9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7h-(1,4)oxazino(2,3,4-ij)quinoline-6-carboxylic acid
s01ae01
ofloxacin ophthalmic
ofloxacinum (latin)
ofloxacin (usp-rs)
(+/-)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7--oxo-7h-pyrido(1,2,3-de)--1,4-benzoxazine-6-carboxylic acid
ofloxacin (ep monograph)
s02aa16

Research Excerpts

Overview

Ofloxacin is a broad-spectrum fluoroquinolone antibiotic frequently used in clinic for treating bacterial infections. OFLX is a racemic mixture of levofl Oxacin which revealed phototoxicity in patients exposed with sunlight after medication. AntoflOxacin (AFX) is a novel fluoroquolone that has been approved in China for the treatment of infections caused by a variety of bacterial species.

ExcerptReferenceRelevance
"Ofloxacin is an antibiotic that binds to DNA complexes and type II topoisomerase, causing double-stranded breaks in bacterial chromosomes."( Unique Physiological and Genetic Features of Ofloxacin-Resistant
Hamauzu, R; Hosaka, T; Hoshino, K; Kodani, S; Nakagawa, H, 2022
)
1.7
"Ofloxacin (OFL) is a broad-spectrum fluoroquinolone antibiotic frequently used in clinic for treating bacterial infections. "( Effects of ofloxacin on the structure and function of freshwater microbial communities.
Debognies, A; Deng, Y; Lu, T; Qian, H; Sun, L; Zhang, J; Zhang, Q; Zhang, Z; Zhou, Z, 2022
)
2.55
"Ofloxacin (OFL) is a highly toxic antibiotic pollutant, and there are few reports on the effects of changes in OFL levels on tomato chlorophyll fluorescence parameters."( Effect of ofloxacin levels on growth, photosynthesis and chlorophyll fluorescence kinetics in tomato.
Cao, B; Huang, T; Li, N; Li, P; Liu, S; Liu, X; Xu, K; Zhang, Y; Zhang, Z, 2023
)
2.03
"Ofloxacin (OFLX) is a racemic mixture of levofloxacin which revealed phototoxicity in patients exposed with sunlight after medication. "( Cellular and molecular mechanism of ofloxacin induced apoptotic cell death under ambient UV-A and sunlight exposure.
Amar, SK; Dwivedi, A; Kushwaha, HN; Mujtaba, SF; Pant, MC; Ray, RS; Singh, SK; Yadav, N, 2014
)
2.12
"Ofloxacin is an antimicrobial agent frequently found in significant concentrations in wastewater and surface water. "( Photocatalytic degradation of ofloxacin and evaluation of the residual antimicrobial activity.
Guimarães, JR; Maniero, MG; Peres, MS, 2015
)
2.15
"Ofloxacin is a synthetic antibiotic of the fluoroquinolone class, with activity against gram-positive and gram-negative bacteria. "( Development and evaluation of wound healing hydrogels based on a quinolone, hydroxypropyl methylcellulose and biodegradable microfibres.
Agubata, CO; Nzekwe, IT; Obitte, NC; Okereke, C; Onoja, RI, 2016
)
1.88
"Antofloxacin (AFX) is a novel fluoroquinolone that has been approved in China for the treatment of infections caused by a variety of bacterial species. "( Wild-Type and Non-Wild-Type Mycobacterium tuberculosis MIC Distributions for the Novel Fluoroquinolone Antofloxacin Compared with Those for Ofloxacin, Levofloxacin, and Moxifloxacin.
Chen, S; Dong, L; Huang, H; Köser, CU; Moradigaravand, D; Parkhill, J; Peacock, SJ; Schön, T; Shang, Y; Wang, G; Wei, G; Yu, X, 2016
)
1.27
"Ofloxacin, a quinolone, is an extensively used, well-tolerated antibacterial agent but has been reported to induce photosensitivity at low incidences. "( Ofloxacin-associated retinopathy in rabbits: role of oxidative stress.
Kaur, R; Rampal, S; Sethi, R; Singh, O; Sood, N, 2008
)
3.23
"Antofloxacin hydrochloride is a new fluoroquinolone antibiotic with broad-spectrum in vitro activity. "( Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.
Xiao, XM; Xiao, YH, 2008
)
1.23
"Levofloxacin seems to be a good alternative treatment for patients with uncomplicated spontaneous ascites infections."( A recent evaluation of empirical cephalosporin treatment and antibiotic resistance of changing bacterial profiles in spontaneous bacterial peritonitis.
Alişkan, H; Güçlü, M; Husamettin, E; Serin, E; Yakar, T, 2010
)
0.87
"Levofloxacin is a synthetic fluoroquinolone with a broad spectrum of antibacterial activity. "( Bioavailability of two oral formulations of a single dose of levofloxacin 500 mg: an open-label, randomized, two-period crossover comparison in healthy Mexican volunteers.
Burke-Fraga, V; Cariño, L; Fuentes-Fuentes, E; Galan-Herrera, JF; Namur, S; Parra, MG; Poo, JL; Rosales-Sanchez, O, 2009
)
1.21
"Levofloxacin is a fluoroquinolone that has a broad spectrum of activity against several causative bacterial pathogens of community-acquired pneumonia (CAP). "( Levofloxacin in the treatment of community-acquired pneumonia.
Elkhatib, WF; Noreddin, AM, 2010
)
1.6
"Antofloxacin hydrochloride is an effective and well-tolerated new fluoroquinolone that demonstrates clinical and bacteriological efficacies similar to levofloxacin for the treatment of AECB and AP."( A phase II study of antofloxacin hydrochloride, a novel fluoroquinolone, for the treatment of acute bacterial infections.
Bai, C; Huang, W; Mei, C; Wang, J; Xiao, Y; Xiu, Q; Xu, N; Zheng, Q, 2010
)
1.29
"Levofloxacin is a fluoroquinolone used globally to treat respiratory, skin, and genitourinary tract infections. "( Acute hepatitis associated with the use of levofloxacin.
Figueira-Coelho, J; Mendonça, P; Neta, J; Neves-Costa, J; Pereira, O; Picado, B, 2010
)
1.24
"Levofloxacin n-oxide is an impurity isolated from levofloxacin."( In silico and in vitro genotoxicity evaluation of levofloxacin n-oxide, an impurity in levofloxacin.
Guo, M; Li, J; Li, T; Wang, W; Zhang, X; Zhu, Q, 2012
)
1.14
"Levofloxacin (LVFX) is a broad spectrum third generation fluoroquinolone antibiotic, used in the treatment of severe or life-threatening bacterial infections. "( Photosensitizing mechanism and identification of levofloxacin photoproducts at ambient UV radiation.
Ali, D; Dwivedi, A; Kushwaha, HN; Mujtaba, SF; Ray, RS; Singh, SK; Yadav, N,
)
1
"Levofloxacin is a third-generation fluorinated quinolone antibiotic, is the active levo stereoisomer of ofloxacin, and has one of the most favorable adverse reaction profiles."( Levofloxacin-induced delirium: is it a dangerous drug in patients with renal dysfunction?
Dortdudak, S; Eroglu, E; Kocyigit, I; Oymak, O; Sipahioglu, M; Tokgoz, B; Unal, A; Utas, C; Yucel, HE, 2012
)
1.51
"Levofloxacin is a valuable antimicrobial agent and an optimal treatment option for AECB, CAP (as a monotherapy) and HAP (as combination therapy at a high-dose regimen). "( Levofloxacin for the treatment of respiratory tract infections.
Liapikou, A; Torres, A, 2012
)
1.62
"Levofloxacin is a broad-spectrum antibiotic that exists as a hemihydrate under ambient conditions. "( Understanding the dehydration of levofloxacin hemihydrate.
Gorman, EM; Munson, EJ; Samas, B, 2012
)
1.28
"Levofloxacin is a synthetic fluoroquinolone that is usually used to treat chronic bacterial prostatitis. "( Safety and efficacy of levofloxacin versus ciprofloxacin for the treatment of chronic bacterial prostatitis in Chinese patients.
Guo, YL; Jin, FS; Liu, DM; Shen, ZJ; Sun, YH; Zhang, ZC, 2012
)
1.3
"Levofloxacin is a third-generation fluoroquinolone with a broad spectrum of antibacterial activity, comprising enterobacteria, non-fermenters, Gram-positive cocci and some anaerobic species. "( Tissue and serum concentrations of levofloxacin 500 mg administered intravenously or orally for antibiotic prophylaxis in biliary surgery.
Geiss, HK; Hoppe-Tichy, T; Klee, F; Oberdorfer, K; Swoboda, S; von Baum, H, 2003
)
1.21
"Levofloxacin is a recently introduced fluoroquinolone."( [Achilles tendinitis associated to levofloxacin: report of 4 cases].
Aros, C; Flores, C; Mezzano, S, 2002
)
1.1
"Levofloxacin is a fluoroquinolone antibiotic commonly used to treat respiratory, urinary tract, skin and soft-tissue infections. "( Acute hepatitis associated with oral levofloxacin therapy in a hemodialysis patient.
Lee, CH; Schwalm, JD, 2003
)
1.21
"Ofloxacin is a fluoroquinolone antibacterial with potent bactericidal activities and the topical otological preparation of this drug has been clinically utilised since the late 1980s. "( A benefit-risk assessment of ofloxacin otic solution in ear infection.
Tong, MC; Wai, TK, 2003
)
2.05
"Levofloxacin-induced AIHA is a rare but serious complication of therapy. "( Levofloxacin-induced autoimmune hemolytic anemia.
Carr-Lopez, SM; Crawley, PG; Oh, YR; Probasco, JM,
)
1.37
"Ofloxacin is a quinolone administered to patients with severe infections. "( Single-dose pharmacokinetics of ofloxacin during continuous venovenous hemofiltration in critical care patients.
El Menyawi, I; Fuhrmann, V; Mittermayer, C; Ratheiser, K; Schenk, P; Thalhammer, F, 2003
)
2.05
"Levofloxacin is a new, recently commercialized fluoroquinolone. "( [Use of levofloxacin in the hospital].
Arnau, JM; Campany, D; Castells, X; Rigau, D; Vallano, A, 2003
)
1.33
"Levofloxacin is a recent fluoroquinolone and its muscular toxicity is not well documented."( A case of rhabdomyolysis with fatal outcome after a treatment with levofloxacin.
Debien, B; Nadaud, J; Olive, F; Pats, B; Perez, JP; Petitjeans, F; Villevieille, T, 2003
)
1.07
"Levofloxacin (Levaquin) is a fluoroquinolone antibacterial agent with a broad spectrum of activity against Gram-positive and Gram-negative bacteria and atypical respiratory pathogens. "( Levofloxacin: a review of its use in the treatment of bacterial infections in the United States.
Croom, KF; Goa, KL, 2003
)
1.56
"Levofloxacin is a broad-spectrum antibacterial agent with activity against a range of Gram-positive and Gram-negative bacteria and atypical organisms. "( Levofloxacin: a review of its use in the treatment of bacterial infections in the United States.
Croom, KF; Goa, KL, 2003
)
1.56
"Levofloxacine is a fluoroquinolone presenting good anti-pneumococcal activity, including against strains with reduced sensitivity to penicillin. "( [Levofloxacine for the treatment of pneumococcal pneumonia: results of a meta-analysis].
Bru, JP; Leophonte, P; Veyssier, P, 2003
)
1.5
"Levofloxacin is a broad-spectrum fluoroquinolone antibiotic with activity against many pathogens that cause bacterial infections in children, including penicillin-resistant pneumococci. "( Levofloxacin pharmacokinetics in children.
Blumer, JL; Bocchini, JA; Bradley, JS; Chien, S; Kearns, GL; Maldonado, S; Natarajan, J; Noel, GJ; Wells, TG, 2005
)
1.57
"Levofloxacin (LEV) is a fluoroquinolone antimicrobial agent. "( The interaction between levofloxacine hydrochloride and DNA mediated by Cu2+.
Cai, Z; He, Y; Song, G, 2004
)
1.24
"Levofloxacin is a fluoroquinolone antimicrobial agent for which pharmacodynamic relationships between the maximum serum antibiotic concentration (Cmax)/minimum inhibitory concentration (MIC) ratio and/or the area under the serum concentration-time curve during a 24-h dosing period (AUC(0-24))/MIC ratio and clinical and/or microbiological outcomes have been developed. "( Pharmacodynamics of levofloxacin in patients with acute exacerbation of chronic bronchitis.
Blasi, F; Cazzola, M; Donnarumma, G; Marchetti, F; Matera, MG; Sanduzzi, A; Tufano, MA, 2005
)
1.26
"Ofloxacin is a fluoroquinolone agent available as an immediate-release (IR) tablet formulation administered twice daily. "( Two open-label, randomized, crossover studies assessing the bioequivalence of ofloxacin administered as immediate-and extended-release formulations in healthy subjects.
Badri, N; Di Spirito, M; DiMarco, M; Ducharme, MP; Marier, JF; Monif, T; Morelli, G; Rampal, A; Tippabhotla, SK, 2006
)
2
"Levofloxacin is a fluoroquinolone with extensive renal elimination and enhanced penetration into lungs and Pseudomonas aeruginosa (PA) biofilms."( Levofloxacin pharmacokinetics in adult cystic fibrosis.
Boyle, MP; Brass-Ernst, L; Diener-West, M; Lee, CKK; Noschese, M; Zeitlin, PL, 2007
)
1.47
"Antofloxacin hydrochloride is a newly developed fluoroquinolone antibacterial in China, which has comparable in vitro and animal pharmacological and toxicological properties to levofloxacin and is worthy of further clinical trial. "( Pharmacokinetics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, after single oral dose administration in Chinese healthy male volunteers.
Kang, Z; Li, T; Liu, Y; Lu, Y; Xiao, Y; Zhang, M, 2008
)
1.28
"Levofloxacin (Levaquin) is a fluoroquinolone antibacterial that is the L-isomer of ofloxacin. "( Levofloxacin : a review of its use as a high-dose, short-course treatment for bacterial infection.
Anderson, VR; Perry, CM, 2008
)
1.59
"Ofloxacin may prove to be a useful new antichlamydial agent."( Comparison of the in vitro activities of ofloxacin and tetracycline against Chlamydia trachomatis as assessed by indirect immunofluorescence.
Bailey, JM; Heppleston, C; Richmond, SJ, 1984
)
1.25
"Levofloxacin is a fluoroquinolone with excellent bioavailability properties that affords potential use in the treatment of a wide variety of infections caused by Gram-positive organisms such as streptococci."( The comparative antimicrobial activity of levofloxacin tested against 350 clinical isolates of streptococci.
Biedenbach, DJ; Jones, RN, 1996
)
1.07
"Ofloxacin is a fluoroquinolone antibiotic that is excreted in the urine as unchanged drug via active tubular secretion and glomerular filtration."( Effects of ofloxacin on the pharmacokinetics and pharmacodynamics of procainamide.
Cascio, W; Griener, J; Martin, DE; Patterson, JH; Raasch, R; Shen, J, 1996
)
1.41
"Levofloxacin is a fluoroquinolone antibiotic and is the optical S-(-) isomer of the racemic drug substance ofloxacin. "( The clinical pharmacokinetics of levofloxacin.
Chow, AT; Fish, DN, 1997
)
1.19
"Ofloxacin seems to be a good alternative in the treatment of typhoid fever caused by co-trimoxazole resistant salmonellae in children aged less than 16 years."( Ofloxacin versus co-trimoxazole in the treatment of typhoid fever in children.
Akan, O; Ceyhan, M; Ecevit, Z; Figen, G; Kanra, G; Seçmeer, G, 1997
)
2.46
"Ciprofloxacin (CPFX) is a widely used fluoroquinolone antibiotic, inducing cutaneous adverse drug reactions in about 1 to 2% of the treated patients. "( Cutaneous adverse reaction to ciprofloxacin: demonstration of specific lymphocyte proliferation and cross-reactivity to ofloxacin in vitro.
Gleichmann, E; Hunzelmann, N; Rönnau, AC; Ruzicka, T; Sachs, B; Schuppe, HC; von Schmiedeberg, S, 1997
)
1.13
"Ofloxacin is a broad spectrum fluoroquinolone antibiotic with good ocular penetration. "( Retinal safety of oral and topical ofloxacin in rabbits.
Callina, C; Cohen, RG; Lahav, M; Raizman, M, 1997
)
2.02
"Ofloxacin is a potent broad-spectrum fluoroquinolone antibiotic commercially available as a topical ophthalmic preparation. "( Ofloxacin monotherapy for the primary treatment of microbial keratitis: a double-masked, randomized, controlled trial with conventional dual therapy. The Ofloxacin Study Group.
, 1997
)
3.18
"Ofloxacin is a member of 4-Quinolone broad spectrum antibiotics."( Effects of nimodipine and ofloxacin on staphylococcal brain abscesses in rats.
Ceviz, A; Ciçek, R; Gül, K; Inalöz, SS; Sanli, A; Sari, I, 1997
)
1.32
"Levofloxacin (L-ofloxacin) is a fluoroquinolone derivative. "( Successful treatment of murine listeriosis and salmonellosis with levofloxacin.
Bornitz, F; Hof, H; Kretschmar, M; Nichterlein, T, 1998
)
1.16
"Ofloxacin is an established fluoroquinolone agent which achieves good concentrations in genitourinary tract tissues and fluids. "( Ofloxacin. A reappraisal of its use in the management of genitourinary tract infections.
Balfour, JA; Lamb, HM; Onrust, SV, 1998
)
3.19
"Ofloxacin is a synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. "( Ofloxacin otic solution: a review of its use in the management of ear infections.
Markham, A; Simpson, KL, 1999
)
3.19
"Ofloxacin (OFLX) is a fluoroquinolone-antibiotic with a broad antimicrobial spectrum that may have a potential role in the treatment of bacterial endophthalmitis. "( Retinal toxicity of liposome-incorporated and free ofloxacin after intravitreal injection in rabbit eyes.
Duncker, GI; Grammer, JB; Hedderich, J; Neumann, D; Pleyer, U; Wiechens, B,
)
1.83
"Levofloxacin is a new fluoroquinolone active against S. "( [Levofloxacin in the treatment of community-acquired pneumococcal pneumonia].
Léophonte, P; Veyssier, P, 1999
)
1.48
"Ofloxacin is a broad spectrum fluoroquinolone antibiotic with good ocular penetration. "( Comparison of topical 0.3% ofloxacin with fortified tobramycin plus cefazolin in the treatment of bacterial keratitis.
Ahuja, R; Panda, A; Sastry, SS, 1999
)
2.04
"Levofloxacin is an additional option as monotherapy for the treatment of CAP."( Oral levofloxacin in the treatment of community-acquired pneumonia.
Idrahim, KY; Lima Nicodemo, E; Nicodemo, AC, 2000
)
1.26
"Levofloxacin is a useful quinolone for patients infected with osteomyelitis or tuberculosis. "( [Tolerability and safety of levofloxacinin long-term treatment].
Almela, M; Alvárez, JL; García, S; Mensa, J; Ortega, M; Soriano, A; Soriano, E; Tomás, X, 2000
)
1.21
"Levofloxacin is a valuable addition to the group of fluoroquinolone antibiotics."( Levofloxacin.
Norrby, SR, 1999
)
1.44
"Levofloxacin is a second generation fluoroquinolone with a post marketing history of well tolerated and successful use in a variety of clinical situations."( A risk-benefit assessment of levofloxacin in respiratory, skin and skin structure, and urinary tract infections.
Garvin, CG; Jung, R; Martin, SJ, 2001
)
1.11
"Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. "( Ofloxacin/beta-cyclodextrin complexation.
Bassani, VL; Eifler-Lima, VL; Guterres, SS; Koester, LS; Le Roch, M; Zuanazzi, JA, 2001
)
3.2
"Ofloxacin is a fluoroquinolone antibiotic that kills nongrowing cells, and biofilms and stationary-phase cells were comparably tolerant to this antibiotic."( Biofilms and planktonic cells of Pseudomonas aeruginosa have similar resistance to killing by antimicrobials.
Lewis, K; Spoering, AL, 2001
)
1.03
"Ofloxacin is a new broad-spectrum oral bactericidal antimicrobial agent. "( [Determination of ofloxacin in human plasma and studies of its pharmacokinetics using HPLC method].
Diao, Y; Ding, AZ; Xu, DK; Yuan, YS, 1992
)
2.06
"Ofloxacin proved to be an effective, safe, and comfortable therapy for external bacterial ocular infection."( Topical ofloxacin compared with gentamicin in the treatment of external ocular infection. Ofloxacin Study Group.
Gwon, A, 1992
)
1.44
"Ofloxacin is a fluoroquinolone with activity against gram-positive and gram-negative aerobic and facultatively anaerobic bacteria, chlamydiae, and some related organisms, such as mycoplasmas or mycobacteria. "( Oral ofloxacin: a critical review of the new drug application.
Sanders, WE, 1992
)
2.24
"Ofloxacin is a new fluoroquinolone with a spectrum of activity similar to other fluoroquinolones with activity which includes Chlamydia trachomatis, Mycobacterium spp., Mycoplasma spp. "( Ofloxacin clinical pharmacokinetics.
Bailey, EM; Lamp, KC; Rybak, MJ, 1992
)
3.17
"Ofloxacin is a new fluoride quinolone which has been shown to be active both in vitro and in vivo against Mycobacterium tuberculosis. "( [Treatment of urogenital tuberculosis with ofloxacin. Preliminary study].
Alberte, A; Amón Sesmero, J; Estebanez Zarranz, MJ; Martínez-Sagarra, JM; Rodríguez Toves, A, 1992
)
1.99
"Ofloxacin is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. "( Ofloxacin. A reappraisal of its antimicrobial activity, pharmacology and therapeutic use.
Faulds, D; Todd, PA, 1991
)
3.17
"Ofloxacin is a promising new antibiotic for the treatment of acute lower respiratory infections."( Treatment of lower respiratory infections in outpatients with ofloxacin compared with erythromycin.
Hooton, TM; Lipsky, BA; Pecoraro, RE; Peugeot, RL, 1991
)
1.24
"Ofloxacin is a new oral quinolone antibiotic with good to excellent activity against many of the usual and atypical pulmonary pathogens."( Treatment of pneumonia: new strategies for changing pathogens.
Ashby, BL,
)
0.85
"Ofloxacin is a proven antibiotic substance useful in the treatment of lower respiratory tract infections."( Ofloxacin in lower respiratory tract infections.
Petermann, W, 1991
)
2.45
"Ofloxacin was found to be an effective drug with few adverse reactions."( Double-blind comparative study of ofloxacin (Hoe 280) and trimethoprim-sulfamethoxazole in the treatment of patients with acute exacerbations of chronic bronchitis and chronic obstructive lung disease.
Boye, NP; Gaustad, P, 1991
)
1.28
"Ofloxacin appears to be an effective and safe oral therapy for the treatment of infections caused by N."( Evaluation of ofloxacin in the treatment of uncomplicated gonorrhea.
Benes, S; Covino, JM; Cummings, MC; Draft, K; McCormack, WM; Smith, BL,
)
1.21
"Ofloxacin is a newly licensed fluoroquinolone with an antimicrobial spectrum similar to ciprofloxacin. "( Ofloxacin.
Scheld, WM; Tunkel, AR, 1991
)
3.17
"Ofloxacin is a quinolone carboxylic acid with a broad spectrum of activity for gram-negative pathogens that are common causes of urologic infections including cystitis, pyelonephritis, and prostatitis. "( Worldwide clinical experience with ofloxacin in urologic cases.
Corrado, ML, 1991
)
2
"Ofloxacin appears to be a safe, effective, well-tolerated alternative to trimethoprim-sulfamethoxazole for preventing gram-negative infection in acute leukemia, but more effective prophylaxis of gram-positive infections is still needed."( Ofloxacin versus trimethoprim-sulfamethoxazole for prevention of infection in patients with acute leukemia and granulocytopenia.
Kern, W; Kurrle, E,
)
2.3
"Ofloxacin appears to be an effective drug for the eradication of S."( Treatment of Salmonella paratyphi A infection with oral ofloxacin.
Murata, M; Ohnishi, K,
)
1.1
"Ofloxacin is a new fluorinated quinolone antibiotic with a broad spectrum of activity against a variety of gram-positive and -negative bacteria including Enterobacteriaceae, Pseudomonas aeruginosa, and methicillin-resistant Staphylococcus aureus. "( Ofloxacin: a review.
Rybak, MJ; Smythe, MA, 1989
)
3.16
"Ofloxacin is a well-tolerated fluoroquinolone antimicrobial agent."( The safety profile of ofloxacin.
Smith, JA; Tack, KJ, 1989
)
1.31
"Ofloxacin was found to be a safe, well-tolerated therapeutic agent, which was as effective clinically as amoxicillin or erythromycin and with an advantage of less frequent administration."( Ofloxacin in community-acquired lower respiratory infections. A comparison with amoxicillin or erythromycin.
Garcia, JG; Griffith, DE; Kohler, RB; Stocks, JM; Wallace, RJ, 1989
)
2.44
"Ofloxacin (Tarivid) is a 4-quinolone of the latest generation. "( [Assessment of the genotoxic risk caused by the gyrase inhibitor ofloxacin using sister chromatid exchange rate analysis].
Brugger, P; Klein, G; Kullich, W, 1988
)
1.96
"Ofloxacin is a fluoroquinolone available for oral use showing good absorption with high blood levels and quite satisfactory tissue, penetration particularly in O.R.L."( [The use of ofloxacin in otorhinolaryngology].
Cavallo, GP; Giordano, C,
)
1.23
"Ofloxacin (OFL) is a new broad-spectrum drug with potentially valuable antimycobacterial activity. "( Effectiveness of ofloxacin against Mycobacterium tuberculosis and Mycobacterium avium, and rifampin against M. tuberculosis in cultured human macrophages.
Crowle, AJ; Elkins, N; May, MH, 1988
)
2.06
"Ofloxacin is a valuable addition to the range of antimicrobial agents available for the oral treatment of bacterial infection."( Pharmacokinetics of ofloxacin and the effect on the faecal flora of healthy volunteers.
Hancock, P; Harris, K; Leigh, DA; Travers, G; Walsh, B, 1988
)
1.32
"Ofloxacin appears to be an effective treatment for lower genital tract infections with Ch."( Efficacy of ofloxacin in the treatment of non-gonococcal urethritis in men and genital infections caused by Chlamydia trachomatis in men and women.
Nayagam, AT; Oriel, JD; Ridgway, GL, 1988
)
1.38
"Ofloxacin is a 4-quinolone antibiotic with rapid bactericidal activity against a wide variety of organisms. "( Ofloxacin: its pharmacology, pharmacokinetics, and potential for clinical application.
Drew, RH; Gallis, HA, 1988
)
3.16
"Ofloxacin is a new fluoroquinolone with excellent in vitro activity against N. "( [One-dose treatment of male gonococcal urethritis by ofloxacin].
Baury, A; Casin, I; Lassau, F; Morel, P; Perol, Y, 1987
)
1.97
"Ofloxacin is a new fluoroquinolone derivative active against Gram-positive and Gram-negative bacteria including obligate anaerobes. "( Susceptibility in vitro of gram-positive aerobe and anaerobe bacteria to ofloxacin.
Debbia, E; Gianrossi, G; Mannelli, S; Schito, GC, 1987
)
1.95
"Ofloxacin is a new oral antibacterial fluoro-quinolone, endowed with potent bactericidal activity over a very broad bacterial spectrum. "( Ofloxacin: in vitro and in vivo activity.
Caro, B; Erani, E; Guerra, L; Xerri, L, 1987
)
3.16
"Ofloxacin appears to be an appropriate antibiotic for short term therapy of acute, uncomplicated, lower urinary tract infections, comparing favourably with trimethoprim-sulphamethoxazole treatment in this study."( Ofloxacin versus trimethoprim-sulphamethoxazole in acute cystitis.
Bjertnaes, A; Block, JM; Hafstad, PE; Holte, M; Ottemo, I; Peterson, LE; Rolstad, T; Svarva, PL; Walstad, RA, 1987
)
2.44
"Ofloxacin proved to be an effective and well-tolerated substance."( Clinical experience with ofloxacin in upper and lower urinary tract infections. A comparison with co-trimoxazole and nitrofurantoin.
Ludwig, G; Pauthner, H, 1987
)
1.3
"Ofloxacin is a new quinolone-carboxylic acid derivative with a broad spectrum of activity, excellent bioavailability after oral administration and insignificant metabolisation. "( [Summarized results of clinical phase II and III studies with ofloxacin (HOE 280) in Europe].
Blomer, R; Bruch, K; Zahlten, RN, 1986
)
1.95
"Ofloxacin is a new fluoroquinolone with in vitro activity against the three main urethritis-causing pathogens: i.e. "( [Treatment with ofloxacin (RU 43280) of uncomplicated bacterial urethritis in males].
Bianchi, A; Casin, I; Dolivo, M; Morel, P; Perol, Y, 1986
)
2.06
"Ofloxacin is a fluoroquinolone that is mainly eliminated through the kidneys. "( [Pharmacokinetics of ofloxacin in the elderly (65-85 years) with normal renal function after a single oral dose of 200 mg].
Bryskier, A; Couet, W; Darchis, JP; Fourtillan, JB; Lefebvre, MA; Modai, J; Veyssier, P; Vincent Du Laurier, M, 1986
)
2.03
"Ofloxacin is a new quinolone carboxylic acid compound. "( In-vitro activity of ofloxacin, a quinolone carboxylic acid compared to other quinolones and other antimicrobial agents.
Kumada, T; Neu, HC, 1985
)
2.03

Effects

Levofloxacin has a high bioavailability and a broad antibacterial spectrum which covers the common pathogens found in acute and chronic diabetic foot infections. CiprofloxacIn has a four-fold greater in-vitro activity than levofl Oxacin against Pseudomonas aeruginosa. LevoflOxacin is a low photosensitizing potential when administered to healthy subjects.

Ofloxacin (OX) has been reported as an active antibacterial drug for topical infections and it is effective against both positive and negative bacterial strains. Levofloxac in has been shown to be effective in Helicobacter pylori eradication. Oflxacin has no significant effect on perinatal outcomes.

ExcerptReferenceRelevance
"Levofloxacin has a high bioavailability and a broad antibacterial spectrum which covers the common pathogens found in acute and chronic diabetic foot infections. "( Tissue and serum levofloxacin concentrations in diabetic foot infection patients.
Baertsch, U; Born, B; Geiss, HK; Hamann, A; Hoppe-Tichy, T; Kusterer, K; Oberdorfer, K; Swoboda, S; von Baum, H, 2004
)
1.27
"Ofloxacin acyl chloride has a tertiary amino function in its structure and the derivatives from ofloxacin acyl chloride reacting with amino analytes can be ionized by an acid treatment and analyzed by simple capillary zone electrophoresis."( An ionizable chromophoric reagent for the analysis of primary amine-containing drugs by capillary electrophoresis.
Chen, SH; Kou, HS; Kwan, AL; Lin, FM; Wu, HL; Wu, SM, 2005
)
1.05
"Levofloxacin has a tolerability profile similar to that of other oral fluoroquinolones, with gastrointestinal and central nervous system effects reported most commonly."( Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy.
Bryson, HM; Davis, R, 1994
)
1.42
"Ciprofloxacin has a four-fold greater in-vitro activity than levofloxacin against Pseudomonas aeruginosa, but levofloxacin has a four-fold higher area under the serum concentration-time curve (AUC) for an equivalent dose. "( The antibacterial efficacy of levofloxacin and ciprofloxacin against Pseudomonas aeruginosa assessed by combining antibiotic exposure and bacterial susceptibility.
Holt, HA; MacGowan, AP; Wootton, M, 1999
)
1.14
"Levofloxacin has a low photosensitizing potential when administered to healthy subjects."( Photoreaction potential of orally administered levofloxacin in healthy subjects.
Boccumini, LE; Campbell, TA; Fowler, CL; Kaidbey, KH; Puertolas, LF, 2000
)
1.18
"Levofloxacin has a powerful and rapid bactericidal activity, particularly against pneumococci, whatever the level of penicillin resistance."( [Treatment of community-acquired pneumonia with levofloxacin: 500 mg once a day or 500 mg twice a day?].
Bru, JP; Zuck, P,
)
0.9
"Levofloxacin has a reduced CNS adverse event rate compared with ofloxacin."( Safety of the new fluoroquinolones compared with ciprofloxacin.
Ball, P, 2000
)
1.07
"Levofloxacin has a very low phototoxicity-inducing potential confirmed by pre-clinical animal studies and the results of post-marketing surveillance (PMS)."( Latest industry information on the safety profile of levofloxacin in Japan.
Yagawa, K, 2001
)
1.07
"Ofloxacin has a good safety profile, but, as with other fluoroquinolones, it should not be used in children or in pregnant or nursing women."( Ofloxacin.
Scheld, WM; Tunkel, AR, 1991
)
2.45
"Ofloxacin (OX) has been reported as an active antibacterial drug for topical infections and it is effective against both positive and negative bacterial strains."( Aloe vera and ofloxacin incorporated chitosan hydrogels show antibacterial activity, stimulate angiogenesis and accelerate wound healing in full thickness rat model.
Andleeb, A; Azam, M; Khan, A; Mehmood, A; Tehseen, S; Yar, M, 2023
)
1.99
"Ofloxacin has no significant effect on perinatal outcomes."( Pregnancy outcomes in women reporting exposure to ofloxacin in early pregnancy.
Ahn, HK; Choi, JS; Chung, JH; Han, JY; Ryu, HM; Shin, YJ, 2018
)
1.46
"Levofloxacin has been proposed to replace clarithromycin for Helicobacter pylori treatment. "( Effect of fluoroquinolone resistance on 14-day levofloxacin triple and triple plus bismuth quadruple therapy.
Graham, DY; Liang, X; Liao, J; Liu, W; Lu, H; Sun, Q; Xiao, S; Zhang, W; Zheng, Q, 2013
)
1.26
"Ofloxacin (OFX) has been used as second-line drug against MDR-TB."( Proteomic analysis of ofloxacin-mono resistant Mycobacterium tuberculosis isolates.
Bisht, D; Deo, N; Lata, M; Sharma, D; Tiwari, PK; Venkatesan, K, 2015
)
1.45
"Levofloxacin, has twice the antimicrobial activity and same toxicity of ofloxacin."( Levofloxacin for prophylaxis in breast cancer surgery compared with ofloxacin.
Kinoshita, H; Koh, M; Morimoto, K, 2002
)
1.45
"Levofloxacin has good coverage against both Gram-positive and Gram-negative pathogens. "( Comparative antimicrobial activity of levofloxacin and ciprofloxacin against Streptococcus pneumoniae.
Garrison, MW, 2003
)
1.21
"Levofloxacin has been shown to be effective in Helicobacter pylori eradication. "( Levofloxacin-based triple therapy vs. quadruple therapy in second-line Helicobacter pylori treatment: a randomized trial.
Cammarota, G; Candelli, M; Carloni, E; Cazzato, IA; Cremonini, F; Di Caro, S; Gabrielli, M; Gasbarrini, A; Gasbarrini, G; Nista, EC; Ojetti, V; Santarelli, L; Zocco, MA, 2003
)
1.56
"Ofloxacin has been advocated by the WHO in case of MDR-TB, when susceptibility to test results are not available before starting the new treatment, in the continuation period (18 months) and if resistance is proven to at least isoniazid and rifampicin."( Ofloxacin in multidrug resistant tuberculosis.
Gawde, AS; Morye, VK; Walwaikar, PP, 2003
)
2.48
"Ofloxacin has the best aqueous penetration in human eyes, as compared with ciprofloxacin and tobramycin, which suggests ofloxacin could be the preferred topical medicine for the prevention and treatment of endophthalmitis."( [Aqueous humor penetration of topically applied ofloxacin, ciprofloxacin and tobramycin].
Wu, XD; Yang, YH; Yao, K; Zhang, Z, 2003
)
2.02
"levofloxacin has proven to be successful reducing the recurrence rate."( [Mitigated erysipelas after implantation of foreign material].
Sauer, J; Seifert, A; Weyer, T, 2004
)
0.84
"Levofloxacin has a high bioavailability and a broad antibacterial spectrum which covers the common pathogens found in acute and chronic diabetic foot infections. "( Tissue and serum levofloxacin concentrations in diabetic foot infection patients.
Baertsch, U; Born, B; Geiss, HK; Hamann, A; Hoppe-Tichy, T; Kusterer, K; Oberdorfer, K; Swoboda, S; von Baum, H, 2004
)
1.27
"Levofloxacin has been proposed as an alternative for these refractory infections."( High levels of dual resistance to clarithromycin and metronidazole and in vitro activity of levofloxacin against Helicobacter pylori isolates from patients after failure of therapy.
Branca, G; Cammarota, G; Fadda, G; Gasbarrini, A; Gasbarrini, GB; Schito, AM; Spanu, T, 2004
)
1.06
"Ofloxacin acyl chloride has a tertiary amino function in its structure and the derivatives from ofloxacin acyl chloride reacting with amino analytes can be ionized by an acid treatment and analyzed by simple capillary zone electrophoresis."( An ionizable chromophoric reagent for the analysis of primary amine-containing drugs by capillary electrophoresis.
Chen, SH; Kou, HS; Kwan, AL; Lin, FM; Wu, HL; Wu, SM, 2005
)
1.05
"Ofloxacin has higher corneal penetration and ability to exceed MIC90 of common ocular contaminants than ciprofloxacin, and would be a more appropriate prophylactic choice for canine cataract patients."( Ciprofloxacin and ofloxacin aqueous humor concentrations after topical administration in dogs undergoing cataract surgery.
Erb, HN; Kern, TJ; Yu-Speight, AW,
)
2.13
"Levofloxacin has been proposed as an alternative to classic therapy in secondary resistance to Helicobacter pylori."( Role of the preliminary susceptibility testing for initial and after failed therapy of Helicobacter pylori infection with levofloxacin, amoxicillin, and esomeprazole.
Capodicasa, S; Cappello, G; Coraggio, D; Grossi, L; Marzio, L, 2006
)
1.16
"Levofloxacin has excellent activity against common respiratory pathogens and therefore is likely to be effective in treating children with persistent or recurrent otitis media."( An open-label, double tympanocentesis study of levofloxacin therapy in children with, or at high risk for, recurrent or persistent acute otitis media.
Arguedas, A; Blumer, J; Dagan, R; Leibovitz, E; McNeeley, DF; Melkote, R; Noel, GJ; Pichichero, M, 2006
)
1.21
"Levofloxacin has been evaluated for the treatment of community-acquired pneumonia (CAP) in numerous randomized clinical trials."( Levofloxacin for the treatment of community-acquired pneumonia.
File, TM; Lynch, JP; Zhanel, GG, 2006
)
1.47
"Levofloxacin has established efficacy and safety in the treatment of community-acquired pneumonia (CAP) in adults, and its use as an alternative therapy for children with CAP has been proposed."( Comparative study of levofloxacin in the treatment of children with community-acquired pneumonia.
Arguedas, A; Blumer, JL; Bradley, JS; Melkote, R; Noel, GJ; Sáez-Llorens, X, 2007
)
1.27
"Levofloxacin has good tissue penetration and an adequate concentration can be maintained in the urinary tract to treat uropathogens."( Levofloxacin : a review of its use as a high-dose, short-course treatment for bacterial infection.
Anderson, VR; Perry, CM, 2008
)
1.48
"Levofloxacin has a tolerability profile similar to that of other oral fluoroquinolones, with gastrointestinal and central nervous system effects reported most commonly."( Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy.
Bryson, HM; Davis, R, 1994
)
1.42
"Ofloxacin has been reported to diffuse readily into the cerebrospinal fluid (CSF) in subjects with both inflamed and uninflamed meninges. "( Kinetics of ofloxacin and its metabolites in cerebrospinal fluid after a single intravenous infusion of 400 milligrams of ofloxacin.
Dreyhaupt, T; Kinzig, M; Kolenda, H; Nau, R; Prange, HW; Sörgel, F, 1994
)
2.11
"Ofloxacin has the advantage of a once-daily regimen, compared to the twice-daily regimen with ciprofloxacin."( A randomised, multinational study with sequential therapy comparing ciprofloxacin twice daily and ofloxacin once daily.
Akalin, E; Bassaris, H; Calangu, S; Kitzes, R; Kosmidis, J; Milicevic, M; Noack, H; Raz, R; Salewski, E; Sukalo, M,
)
1.09
"Ofloxacin has potent activity against Gram-negative species but is less effective against Gram-positive species including Streptococcus pneumoniae."( Evaluation of the effects of ambroxol on the ofloxacin concentrations in bronchial tissues in COPD patients with infectious exacerbation.
Bouvet, O; Bressolle, F; Chanez, P; Fabre, D; Galtier, M; Godard, P; Michel, FB; Paganin, F, 1995
)
1.27
"Ciprofloxacin has the highest activity against Gram-positive is higher than other quinolones."( In vitro antibacterial activity of FA103, a new quinolone derivative of C-7 position with 7-perhydrodiazepinone.
Asaoka, T; Imamori, K; Maebashi, K; Matsuda, H; Matsumoto, M; Tahara, Y, 1995
)
0.77
"Ofloxacin has been used for prevention and treatment of burn infection in 40 burnt subjects. "( [Experience in the use of ofloxacin in the prevention and treatment of wound infection in burns].
Alekseev, AA; Dutikov, VN; Elagina, LV; Iakovlev, VP; Izotova, GN; Kashin, ID; Krutikov, MG, 1995
)
2.03
"Ofloxacin has been successfully used in the treatment of typhoid fever and Salmonella infectious of adults for many years. "( Ofloxacin versus co-trimoxazole in the treatment of typhoid fever in children.
Akan, O; Ceyhan, M; Ecevit, Z; Figen, G; Kanra, G; Seçmeer, G, 1997
)
3.18
"Ofloxacin has the advantage against ciprofloxacin of exceeding the MICs for Staphylococcus and Chlamydia. "( A comparative study of the distribution of ofloxacin and ciprofloxacin in prostatic tissues after simultaneous oral ingestion.
Cheng, C; Foo, KT; Li, MK; Png, JC; Rekhraj, IR; Tan, E, 1997
)
2
"Levofloxacin has enhanced activity against pneumococci compared with clinically available quinolones."( The bactericidal activity of levofloxacin compared with ofloxacin, D-ofloxacin, ciprofloxacin, sparfloxacin and cefotaxime against Streptococcus pneumoniae.
George, J; Morrissey, I, 1997
)
1.09
"Levofloxacin has demonstrated clinical efficacy in the treatment of community-acquired respiratory-tract infections, genitourinary infections, skin and skin-structure infections, acute bacterial sinusitis, and infections of the head and neck."( Levofloxacin and trovafloxacin: the next generation of fluoroquinolones?
Ernst, EJ; Ernst, ME; Klepser, ME, 1997
)
1.43
"Ofloxacin has been reported in the literature as a cause of seizures in patients with compromised renal function."( Ofloxacin-induced seizure.
Hon, JK; Mulpur, TG; Walton, GD, 1997
)
2.46
"ofloxacin has established efficacy in the treatment of a wide variety of urinary tract infections, although, like other fluoroquinolones, it should be used rationally to preserve its activity. "( Ofloxacin. A reappraisal of its use in the management of genitourinary tract infections.
Balfour, JA; Lamb, HM; Onrust, SV, 1998
)
3.19
"Levofloxacin has enhanced activity against gram-positive aerobic organisms, including penicillin-resistant pneumococci."( Levofloxacin: a therapeutic review.
Garrison, MW; Schoonover, L; Wimer, SM,
)
1.27
"Ciprofloxacin has a four-fold greater in-vitro activity than levofloxacin against Pseudomonas aeruginosa, but levofloxacin has a four-fold higher area under the serum concentration-time curve (AUC) for an equivalent dose. "( The antibacterial efficacy of levofloxacin and ciprofloxacin against Pseudomonas aeruginosa assessed by combining antibiotic exposure and bacterial susceptibility.
Holt, HA; MacGowan, AP; Wootton, M, 1999
)
1.14
"Ofloxacin has been formulated as a 0.3% otic solution for the treatment of ear infections."( Ofloxacin otic solution: a review of its use in the management of ear infections.
Markham, A; Simpson, KL, 1999
)
2.47
"Levofloxacin has been reported to have in vitro activity against both gram-positive and gram-negative bacteria. "( Bactericidal activity of levofloxacin and ciprofloxacin on clinical isolates of different phenotypes of Pseudomonas aeruginosa.
Amicosante, G; Franceschini, N; Marchetti, F; Perilli, M; Segatore, B; Setacci, D, 2000
)
1.22
"Levofloxacin has a low photosensitizing potential when administered to healthy subjects."( Photoreaction potential of orally administered levofloxacin in healthy subjects.
Boccumini, LE; Campbell, TA; Fowler, CL; Kaidbey, KH; Puertolas, LF, 2000
)
1.18
"Levofloxacin has a powerful and rapid bactericidal activity, particularly against pneumococci, whatever the level of penicillin resistance."( [Treatment of community-acquired pneumonia with levofloxacin: 500 mg once a day or 500 mg twice a day?].
Bru, JP; Zuck, P,
)
0.9
"Levofloxacin has such an activity profile."( A population pharmacokinetic analysis of the penetration of the prostate by levofloxacin.
Boccumini, L; Corrado, M; Drusano, GL; Gombert, M; Kahn, J; North, D; Oefelein, M; Preston, SL; Van Guilder, M; Weisinger, B, 2000
)
1.05
"Ofloxacin has superior antibacterial effect under the conditions studied."( Effect of topical povidone-iodine versus topical ofloxacin on experimental Staphylococcus keratitis.
Goldberg, MA; Lustbader, J; MacDowell, AL; Melki, SA; Safar, A; Scharper, M; Scharper, P; Yaghouti, F; Zeligs, B, 2000
)
1.28
"Ofloxacin has not been associated with ototoxicity in animal models or in children participating in the clinical trials."( Efficacy of ofloxacin and other otic preparations for acute otitis media in patients with tympanostomy tubes.
Goldblatt, EL, 2001
)
1.41
"Levofloxacin has been involved in only a few case reports of adverse events, which include QTc prolongation, seizures, glucose disturbances, and tendonitis."( A risk-benefit assessment of levofloxacin in respiratory, skin and skin structure, and urinary tract infections.
Garvin, CG; Jung, R; Martin, SJ, 2001
)
1.11
"Levofloxacin has a reduced CNS adverse event rate compared with ofloxacin."( Safety of the new fluoroquinolones compared with ciprofloxacin.
Ball, P, 2000
)
1.07
"Levofloxacin has a very low phototoxicity-inducing potential confirmed by pre-clinical animal studies and the results of post-marketing surveillance (PMS)."( Latest industry information on the safety profile of levofloxacin in Japan.
Yagawa, K, 2001
)
1.07
"Ofloxacin has antitubercular activity and has exclusive renal clearance."( Safety of an ofloxacin-based antitubercular regimen for the treatment of tuberculosis in patients with underlying chronic liver disease: a preliminary report.
Agarwal, SR; Nandeesh, HP; Saigal, S; Sarin, SK, 2001
)
1.4
"Ciprofloxacin has better activity against gram-negative bacilli, an advantage which may be negated by ofloxacin's longer half-life and higher serum levels."( Ofloxacin vs ciprofloxacin: a comparison.
Nicolau, D; Nightingale, CH; Quintiliani, R, 1992
)
2.21
"Ofloxacin has favorable pharmacokinetics with almost 100% bioavailability; peak serum concentrations obtained one to two hours following oral dosing are higher than those achieved with ciprofloxacin."( Ofloxacin.
Scheld, WM; Tunkel, AR, 1991
)
2.45
"Ofloxacin has certain attributes that make it a potentially useful drug in the treatment of urologic infections."( Worldwide clinical experience with ofloxacin in urologic cases.
Corrado, ML, 1991
)
1.28
"Ofloxacin has been evaluated in an in vitro model where microorganisms were exposed to the varying concentrations met in human serum after the oral administration of a 200 mg dose. "( Ofloxacin: bactericidal effect in an in vitro pharmacokinetic model.
Broggio, R; Guerra, L; Xerri, L, 1986
)
3.16
"Ofloxacin has proven to be effective in soft tissue infections and pneumonia after surgical intervention."( Treatment of surgical infections with a modern quinolone: therapy of soft tissue infections and pneumonia with ofloxacin.
Fritzen, T; Marx, E; Uy, J, 1986
)
1.2

Actions

Ofloxacin can cause retarded ossification and arthropathy in young animals. There is no published information about its teratogenicity in humans. Levofloxacins may produce a faster clinical response than older macrolides, allowing for shorter hospital stay.

ExcerptReferenceRelevance
"Levofloxacin can cause severe thrombocytopenia. "( Levofloxacin-induced severe thrombocytopenia.
Polprasert, C; Prayongratana, K, 2009
)
1.6
"Levofloxacin may produce a faster clinical response than older macrolides, allowing for shorter hospital stay."( Clinical outcomes for hospitalized patients with Legionella pneumonia in the antigenuria era: the influence of levofloxacin therapy.
Carratalà, J; Dorca, J; Fernández-Sabé, N; Gudiol, F; Manresa, F; Mykietiuk, A; Verdaguer, R, 2005
)
1.05
"Ciprofloxacin and ofloxacin inhibit proliferation and DNA synthesis of these 3 human TCC lines in vitro. "( Inhibition of human transitional cell carcinoma in vitro proliferation by fluoroquinolone antibiotics.
Dixon, PS; Peretsman, SJ; Seay, TM, 1996
)
0.85
"Ofloxacin can cause retarded ossification and arthropathy in young animals, but there is no published information about its teratogenicity in humans. "( Ofloxacin during the second trimester of pregnancy.
Friedman, S; Hod, M; Merlob, P; Peled, Y, 1991
)
3.17
"Ofloxacin generated lower titers, ranging from 1:14 for indole-positive Proteus spp."( Serum bactericidal activity of ciprofloxacin and ofloxacin in volunteers.
Machka, K; Milatovic, D, 1987
)
1.27
"Ofloxacin did not cause any point mutations, nor did it induce any in vivo or in vitro chromosome mutation in the systems tested."( [No indications for the mutagenicity of ofloxacin].
Bruch, K; Mayer, D, 1986
)
1.26

Treatment

Levofloxacin treatment had no effect on IL-6 activities and concentrations in uninfected broilers. Both ofloxAcin-placebo treatment and tobramycin-erythromycin treatment were more effective in sterilizing the external ocular adnexa.

ExcerptReferenceRelevance
"Ofloxacin treatment failed to counter the bacterial proliferation in Pyn-STm coinfected mice."( Plasmodium-Salmonella Coinfection Induces Intense Inflammatory Response, Oxidative Stress, and Liver Damage: A Mice Model Study for Therapeutic Strategy.
Maurya, AK; Mittal, S; Pal, A; Pandey, AK; Patel, DK; Singh, D; Tiwari, N, 2018
)
1.2
"Levofloxacin treatment did not affect the cytokine mRNA level and nuclear factor-κB-dependent promoter activity."( Levofloxacin reduces inflammatory cytokine levels in human bronchial epithelia cells: implications for aerosol MP-376 (levofloxacin solution for inhalation) treatment of chronic pulmonary infections.
Dudley, MN; Griffith, DC; Lomovskaya, O; Sabet, M; Tarazi, Z; Tsivkovskii, R, 2011
)
1.5
"Levofloxacin treatment was stopped and the patient made a full recovery."( Acute hepatitis associated with the use of levofloxacin.
Figueira-Coelho, J; Mendonça, P; Neta, J; Neves-Costa, J; Pereira, O; Picado, B, 2010
)
1.13
"Levofloxacin treatment abolished bacteremia within 24 h in animals with confirmed pre-infusion bacteremia, and reduced tachypnea and leukocytosis but not fever during the first 2 days of infusions."( Levofloxacin cures experimental pneumonic plague in African green monkeys.
Barr, EB; Brasel, TL; Gigliotti, AP; Koster, F; Layton, RC; McDonald, JD; Mega, W, 2011
)
1.5
"Levofloxacin-based treatment for H. "( Levofloxacin versus clarithromycin in a 10 day triple therapy regimen for first-line Helicobacter pylori eradication: a single-blind randomized clinical trial.
Aresti-Zárate, S; Ayestarán, B; Campos, MR; Carrascosa, MF; Cobo, M; Cuadrado-Lavín, A; Dierssen-Sotos, T; Fernández-Pousa, A; González-Colominas, E; Hernández, M; Pascual, EL; Salcines-Caviedes, JR, 2012
)
1.62
"Ofloxacin-treated patients showed increased endotoxin neutralizing capacity (ENC) 30 min after clamping compared to controls (15.8+/-15 vs 262.8+/-709 p=0.005) and increased IL-6 levels preoperatively and 30 min after clamping."( Oral antibiotic prophylaxis can influence the inflammatory response in aortic aneurysm repair: results of a randomized clinical study.
Holzheimer, RG, 2003
)
1.04
"Ciprofloxacin/dexamethasone treatment is also superior to improvement in clinical response by visit, absence of otorrhea by visit, and reduction of otorrhea volume by visit."( Topical ciprofloxacin/dexamethasone otic suspension is superior to ofloxacin otic solution in the treatment of children with acute otitis media with otorrhea through tympanostomy tubes.
Anon, JB; Conroy, PJ; Dupre, SJ; Hogg, G; Kreisler, LS; Lanier, B; McLean, C; Potts, S; Reese, B; Roland, PS; Stroman, DW; Wall, GM, 2004
)
1.18
"Levofloxacin treatment at 24 hours, but not at 0 hours, resulted in a significant decrease in the number of C."( Effect of levofloxacin on the viability of intracellular Chlamydia pneumoniae and modulation of proinflammatory cytokine production by human monocytes.
Baltch, AL; Bopp, LH; Carlyn, CJ; Carpenter, AN; Hibbs, JR; Michelsen, PB; Ritz, WJ; Smith, RP, 2004
)
1.21
"Levofloxacin treatment was supplemented with piperacillin/tazobactam."( Failure of levofloxacin treatment in community-acquired pneumococcal pneumonia.
Bettaccini, AA; Brigante, G; Endimiani, A; Grossi, P; Luzzaro, F; Toniolo, AQ, 2005
)
1.2
"Levofloxacin treatment had no effect on IL-6 activities and concentrations in uninfected broilers."( Role of interleukin-6 in the pathogenesis of an avian model of Staphylococcus aureus arthritis.
Cheng, GF; Gu, CQ; Hu, XY; Li, XM; Wang, DH; Zhou, Q; Zhou, SQ, 2007
)
0.85
"Both ofloxacin-placebo treatment and tobramycin-erythromycin treatment were more effective than no treatment in sterilizing the external ocular adnexa. "( Perioperative ofloxacin vs. tobramycin: efficacy in external ocular adnexal sterilization and anterior chamber penetration.
Discepola, MJ; Goldstein, DA; Jackson, WB; Kirsch, LS, 1995
)
1.17
"Levofloxacin-treated mice (40 mg/kg once a day) showed no evidence of pyelonephritis in the kidneys, whereas the kidneys of mice treated with the same dose of ciprofloxacin showed only a reduction in the severity of the lesions."( In vivo efficacies of levofloxacin and ciprofloxacin in acute murine hematogenous pyelonephritis induced by methicillin-susceptible and-resistant Staphylococcus aureus strains.
Barrett, JF; Frosco, MB; Kulwich, BA; Licata, L; Melton, JL; Stewart, FP, 1996
)
1.11
"Ofloxacin treatment gave good result in reduction of otorrhea, regardless of the earlier treatment of chronic otitis media."( [Clinical success of treatment of chronic otitis media using topical and peroral administration of ofloxacin].
Dzelalija, B; Kovacić, M, 1999
)
1.24
"Ofloxacin treatment led to significantly more biofilm eradication than the other antibiotic group on day 4 (62 vs."( Ofloxacin for the treatment of urinary tract infections and biofilms in spinal cord injury.
Delaney, G; Hayes, K; Hsieh, J; Nicosia, S; Potter, P; Reid, G, 2000
)
2.47
"Levofloxacin treatment failed in a patient who had pneumococcal pneumonia and had received three previous courses of levofloxacin therapy."( Levofloxacin treatment failure in a patient with fluoroquinolone-resistant Streptococcus pneumoniae pneumonia.
Denys, GA; Kays, MB; Smith, DW; Wack, ME, 2002
)
1.45
"Ofloxacin treatment did not change the total magnesium concentrations in tissues, as determined with ashed samples."( Synergistic effect of ofloxacin and magnesium deficiency on joint cartilage in immature rats.
Lozo, E; Riecke, K; Schwabe, R; Stahlmann, R; Vormann, J, 2002
)
1.35
"Ofloxacin treatment eradicated or controlled 85% (86/101) of the Gram positive and 89% (17/19) of the Gram negative organisms cultured, compared with 83% (103/124) and 78% (29/37), respectively, after gentamicin treatment."( Topical ofloxacin compared with gentamicin in the treatment of external ocular infection. Ofloxacin Study Group.
Gwon, A, 1992
)
1.44
"Ofloxacin treatment was discontinued in three patients."( Oral ofloxacin once daily and doxycycline in the treatment of acute exacerbations of chronic bronchitis.
Ammälä, K; Aro, A; Backman, R; Keistinen, T; Lehtipuu, AL; Punakivi, L; Saarelainen, P; Veneskoski, T; Vilkka, V, 1990
)
1.51
"Ofloxacin treatment was used for the treatment of lower respiratory tract infections in 35 patients."( Severe infections treated with intravenous ofloxacin: a prospective clinical multicentre Swiss study.
Regamey, C; Steinbach-Lebbin, C, 1990
)
1.26
"Ofloxacin by pretreatment with five oral doses of 50 mg/kg did not increase serum concentrations of theophylline (5 mg/kg, i.v."( Lack of effect of ofloxacin on theophylline pharmacokinetics in rats.
Miyazaki, K; Okazaki, O; Tachizawa, H, 1987
)
1.33
"A treatment with ofloxacin for 7 days was inferior to 14 days for febrile UTI in men and should therefore not be recommended."( Antimicrobial for 7 or 14 Days for Febrile Urinary Tract Infection in Men: A Multicenter Noninferiority Double-Blind, Placebo-Controlled, Randomized Clinical Trial.
Abgrall, S; Aparicio, C; Aumaitre, H; Bercot, B; Bernard, L; Bourgarit-Durand, A; Bruyere, F; Canoui, E; Chabrol, A; Charlier, C; Chevret, S; de Lastours, V; Desseaux, K; Empana-Barat, F; Escaut, L; Etienne, M; Ferreyra, M; Fontaine, JP; Garrait, V; Gatey, C; Grall, N; Jaureguiberry, S; Lafaurie, M; Lefort, A; Madeleine, I; Meyssonnier, V; Molina, JM; Mongiat-Artus, P; Morrier, M; Pacanowski, J; Piet, E; Talarmin, JP, 2023
)
1.25
"Treatment with ofloxacin resulted in a bacteriological conversion similar to that following conventional treatment ( p>0.05, Fisher's exact test)."( Bacteriological conversion in twenty urinary tuberculosis patients treated with ofloxacin, rifampin and isoniazid: a 10-year follow-up study.
Castiñeiras, AA; Della-Latta, P; Herreras, A; Pérez-Pascual, P; Zarranz, JE, 2002
)
0.88
"The treatment with ofloxacin in accordance with the above scheme resulted in a rapid improvement of the patient state: the intoxication lowered, the expectoration and the sputum viscosity decreased, the body temperature normalized by the 5th day."( [An attempt to use ofloxacin in patients with mucoviscidosis].
Apul'tsina, ID; Chuchalin, AG; GUgutsidze, EN; Kuchkina, NV; Samsonova, MV; Sokolov, AS, 1996
)
0.94
"Treatment with ofloxacin for 2 or 3 d is equally effective in adults with uncomplicated enteric fever caused by nalidixic acid sensitive strains of S."( Short courses of ofloxacin for the treatment of enteric fever.
Day, NP; Le, TP; Mai, XT; Nguyen, TC; Nguyen, TL; Nguyen, TT; Parry, C; Smith, MD; Solomon, T; To, SD; Wain, J; White, NJ,
)
0.81
"Treatment with ofloxacin in a combined regimen achieved a success rate of 78%."( Quinolones and multidrug-resistant tuberculosis.
Maranetra, KN, 1999
)
0.64
"Treatment with ofloxacin significantly reduced the need for additional courses of antibiotics (28.4%, 12.9-43.9, p=0.0006)."( Once daily oral ofloxacin in chronic obstructive pulmonary disease exacerbation requiring mechanical ventilation: a randomised placebo-controlled trial.
Abroug, F; Belghith, M; Besbes, L; Elatrous, S; Marghli, S; Nouira, S, 2001
)
1
"Treatment with ofloxacin and ciprofloxacin at 50 mg/kg 18 h after infection did not significantly increase survival rates compared with those of untreated controls."( Antipneumococcal activity of ciprofloxacin, ofloxacin, and temafloxacin in an experimental mouse pneumonia model at various stages of the disease.
Azoulay-Dupuis, E; Bedos, JP; Hardy, DJ; Pocidalo, JJ; Swanson, RN; Vallée, E, 1991
)
0.9
"Pretreatment with ofloxacin and norfloxacin did not influence theophylline disposition, but theophylline clearance fell from 0.054 to 0.027 l.h-1.kg-1 in the presence of enoxacin, without a change in the apparent volume of distribution."( Effects of enoxacin, ofloxacin and norfloxacin on theophylline disposition in humans.
Goto, M; Kawakatsu, K; Ohkita, C; Sano, M; Takeyama, M; Yamamoto, I; Yamashina, H, 1988
)
0.92
"Treatment with ofloxacin in 15 patients with chronic renal failure at different stages is reported with respect to patients undergoing hemodialysis treatment. "( [Ofloxacin treatment in nephrologic problem patients with various degrees of chronic renal failure (including dialysis treatment). Preliminary results].
Dörfler, A; Schulz, W, 1986
)
1.53

Toxicity

There were no significant differences between the two groups except for indication. The side-effect profile of levofloxacin was compared with that of other fluoroquinolones based on European and international data from approximately 130 million prescriptions.

ExcerptReferenceRelevance
" No major laboratory toxicities or clinically significant adverse effects were noted in either the ofloxacin or placebo group."( Pharmacokinetics and safety of single rising doses of ofloxacin in healthy volunteers.
Beals, B; Dudley, MN; Flor, S; Marchbanks, CR, 1992
)
0.75
" The two dosage regimens of ofloxacin, 200 or 400 mg every 12 h, appear to be safe and provide serum drug concentrations in excess of the MICs for most susceptible pathogens over the entire dosing interval."( Safety and pharmacokinetics of multiple doses of intravenous ofloxacin in healthy volunteers.
Flor, S; Guay, DR; Matzke, GR; McMahon, FG; Opsahl, JA; Vargas, R, 1992
)
0.82
" LD50 values were 1,881 mg/kg for males and 1,803 mg/kg for females in mice, 1,478 mg/kg for males and 1,507 mg/kg for females in rats and more than 250 mg/kg in females monkeys."( Acute oral toxicity of the new quinolone antibacterial agent levofloxacin in mice, rats and monkeys.
Akahane, K; Furuhama, K; Kato, M; Takayama, S; Yoshida, M, 1992
)
0.52
" No adverse effects on fertility or teratogenicity were noted at any dose."( Reproductive toxicity of the new quinolone antibacterial agent levofloxacin in rats and rabbits.
Fujikawa, K; Harada, S; Ohura, K; Sasaki, T; Takayama, S; Watanabe, T, 1992
)
0.52
" There were no significant differences between the ofloxacin and placebo groups in either protocol in the proportion of subjects reporting adverse experiences."( Safety and pharmacokinetics of single dose intravenous ofloxacin in healthy volunteers.
Flor, S; Guay, D; Tack, K, 1991
)
0.78
" The only other adverse event that occurred in more than one volunteer was headache."( Safety of multiple doses of ofloxacin in healthy volunteers.
Beals, BS; Flor, SC; Stein, GE, 1991
)
0.58
" A treatment course of ofloxacin, once-a-day for three days, was as safe and effective as a standard course of TMP/SMX, twice a day for seven days."( Randomized study to evaluate efficacy and safety of ofloxacin vs. trimethoprim and sulfamethoxazole in treatment of uncomplicated urinary tract infection.
Basista, MP, 1991
)
0.84
"The safety profile of ofloxacin was evaluated on the basis of adverse reactions and abnormal laboratory values seen in United States clinical trials and phase I studies addressing specific issues."( The safety profile of ofloxacin.
Smith, JA; Tack, KJ, 1989
)
0.91
" In all, 130 adverse reactions have been recorded in 116 patients (5."( Safety profile of ofloxacin: the Italian data base.
Fostini, R; Granata, F; Koverech, A; Picari, M; Recchia, G; Toniolo, D, 1986
)
0.6
" In all, 21 adverse events were recorded in 19 patients (3."( Safety profile of ofloxacin in elderly patients.
Benedetti, M; Dalle Vedove, P; Fostini, R; Girelli, M; Recchia, G, 1988
)
0.61
" The study indicates that ofloxacin is a safe and effective agent in the treatment of various infections."( Clinical safety and efficacy of ofloxacin.
Concia, E; Grossi, P; Malfitano, A; Marone, P; Perversi, L, 1988
)
0.86
" In a perinatal and postnatal toxicity study in rats using doses of up to 360 mg/kg, no adverse effects were observed."( Reproductive toxicity of ofloxacin.
Akiyama, Y; Harada, S; Matsuhashi, K; Mochida, K; Ohura, K; Takayama, S; Watanabe, T; Yamashita, N, 1986
)
0.57
" Adverse reactions were seen in nine of 24 patients who received ciprofloxacin and in six of 23 who received ofloxacin."( The efficacy and safety of ciprofloxacin and ofloxacin in chronic Pseudomonas aeruginosa infection in cystic fibrosis.
Høiby, N; Jensen, T; Koch, C; Nielsen, CH; Pedersen, SS, 1987
)
0.79
" Despite differences in patient characteristics, underlying disease, and concurrent medications, ofloxacin and ciprofloxacin were associated with a similar spectrum and incidence of adverse reactions."( Long-term safety of ofloxacin and ciprofloxacin in the treatment of mycobacterial infections.
Berning, SE; Iseman, MD; Madsen, L; Peloquin, CA, 1995
)
0.83
"(S)-10-[(S)-(8-Amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyli c acid hemihydrate (CAS 151390-79-3, DV-7751a) a new quinolone antibacterial agent, was examined for LD50 value, phototoxicity and convulsion inducing potential in laboratory animals."( LD50 value, phototoxicity and convulsion induction test of the new quinolone antibacterial agent (S)-10-[(S)-(8-amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyl ic acid hemihydrate in la
Akahane, K; Kato, M; Nomura, M; Shimoda, K, 1996
)
0.29
"To elucidate the mechanism of phototoxicity induced as a side effect by some of the new quinolone antibiotics, we studied sparfloxacin (SPFX), lomefloxacin, enoxacin, ofloxacin, and ciprofloxacin."( Participation of reactive oxygen species in phototoxicity induced by quinolone antibacterial agents.
Arakane, K; Hirobe, M; Mashiko, S; Nagano, T; Ryu, A; Umezawa, N, 1997
)
0.49
" The most frequently reported drug-related adverse events were nausea and headache."( Double-blind evaluation of the safety and pharmacokinetics of multiple oral once-daily 750-milligram and 1-gram doses of levofloxacin in healthy volunteers.
Callery-D'Amico, SV; Chien, SC; Chow, AT; Fowler, CL; Nayak, R; Williams, RR; Wong, FA, 1998
)
0.51
"Levofloxacin-induced-neurological adverse events such as convulsion, involuntary movement (tremor, myoclonus and chorea-like) and visual hallucination in two elderly patients are reported."( [Levofloxacin-induced neurological adverse effects such as convulsion, involuntary movement (tremor, myoclonus and chorea like), visual hallucination in two elderly patients].
Fukayama, M; Inamatsu, T; Kita, Y; Masuda, Y; Yasuda, H; Yoshida, A, 1999
)
1.48
"3%, respectively, experienced adverse events related or possibly related to the study therapy."( Efficacy and safety of oral levofloxacin compared with clarithromycin in the treatment of acute sinusitis in adults: a multicentre, double-blind, randomized study. The Canadian Sinusitis Study Group.
Anstey, RJ; Lasko, B; Lau, CY; Martel, A; Reddington, JL; Saint-Pierre, C, 1998
)
0.59
" The overall incidence of any adverse effect was 70% (1,000 mg) to 95% (750 mg) for levofloxacin-treated patients and 71% for those taking the placebo."( Pharmacokinetics and safety of high-dose and extended-interval regimens of levofloxacin in human immunodeficiency virus-infected patients.
Baird, B; Chow, AT; Fowler, CL; Masur, H; Natarajan, J; Piscitelli, SC; Spooner, K; Walker, RE; Williams, RR, 1999
)
0.75
"Because increased hepatotoxicity was observed with first line antituberculous agents using four drug standard induction therapy in orthotopic liver transplant patients, we evaluated the efficacy and adverse effects of a novel continuation regimen for the treatment of tuberculosis in orthotopic liver transplant patients at a University Hospital in New York City."( Tuberculosis in orthotopic liver transplant patients: increased toxicity of recommended agents; cure of disseminated infection with nonconventional regimens.
Emre, S; Meyers, BR; Miller, C; Papanicolaou, GA; Sheiner, P, 2000
)
0.31
" No adverse reactions were observed in seven patients (46%)."( [Tolerability and safety of levofloxacinin long-term treatment].
Almela, M; Alvárez, JL; García, S; Mensa, J; Ortega, M; Soriano, A; Soriano, E; Tomás, X, 2000
)
0.59
" Topical ofloxacin has no demonstrable adverse effects on middle ear or cochlear function."( Safety of ofloxacin otic and other ototopical treatments in animal models and in humans.
Gates, GA, 2001
)
1.13
" During clinical trials, 12 per cent of patients treated with levofloxacin experienced an adverse event considered to be related to the study drug compared with 13 per cent of the patients with a comparator."( [Levofloxacin adverse effects, data from clinical trials and pharmacovigilance].
Carbon, C,
)
0.93
" Ciprofloxacin is well tolerated; the incidence of adverse events is low and serious adverse events are rare."( Safety of the new fluoroquinolones compared with ciprofloxacin.
Ball, P, 2000
)
1.07
" Severe drug adverse events were noted for enoxacin, pefloxacin and fleroxacin, which were phototoxic."( History of quinolones and their side effects.
Rubinstein, E, 2001
)
0.31
"The side-effect profile of levofloxacin was compared with that of other fluoroquinolones based on European and international data from approximately 130 million prescriptions."( Comparison of side effects of levofloxacin versus other fluoroquinolones.
Carbon, C, 2001
)
0.88
"This paper focuses on the development of four major adverse drug reactions (ADRs) associated with some fluoroquinolones: convulsions, phototoxicity, cardiac effects, and hepatotoxicity."( Latest industry information on the safety profile of levofloxacin in Japan.
Yagawa, K, 2001
)
0.56
"Hepatotoxicity is a major side-effect of antitubercular drugs (ATD)."( Safety of an ofloxacin-based antitubercular regimen for the treatment of tuberculosis in patients with underlying chronic liver disease: a preliminary report.
Agarwal, SR; Nandeesh, HP; Saigal, S; Sarin, SK, 2001
)
0.68
" This case series describes the probable association between multiple adverse events and the use of pyrazinamide and levofloxacin in the treatment of individuals with suspected latent multidrug-resistant tuberculosis infection."( Adverse events associated with pyrazinamide and levofloxacin in the treatment of latent multidrug-resistant tuberculosis.
Dolovich, LR; Holbrook, A; Loeb, M; Papastavros, T; Whitehead, L, 2002
)
0.77
" The Naranjo scale was used to assess patients for musculoskeletal, central nervous system, gastrointestinal and dermatological adverse events."( Adverse events associated with pyrazinamide and levofloxacin in the treatment of latent multidrug-resistant tuberculosis.
Dolovich, LR; Holbrook, A; Loeb, M; Papastavros, T; Whitehead, L, 2002
)
0.57
"Fourteen individuals developed musculoskeletal adverse effects (11 were deemed to be probably related to combination therapy)."( Adverse events associated with pyrazinamide and levofloxacin in the treatment of latent multidrug-resistant tuberculosis.
Dolovich, LR; Holbrook, A; Loeb, M; Papastavros, T; Whitehead, L, 2002
)
0.57
" Given the severity of some of the adverse events, a better understanding of dosing and clearer guidelines for monitoring therapy are imperative if these drugs are to be prescribed together."( Adverse events associated with pyrazinamide and levofloxacin in the treatment of latent multidrug-resistant tuberculosis.
Dolovich, LR; Holbrook, A; Loeb, M; Papastavros, T; Whitehead, L, 2002
)
0.57
" Other adverse effects include neutropenia, fever, phlebitis, nephrotoxicity, ototoxicity, thrombocytopenia, interstitial nephritis, lacrimation, linear IgA bullous dermatosis, necrotizing cutaneous vasculitis and toxic epidermal necrolysis."( Uncommon vancomycin-induced side effects.
Baptista, MI; Da Cunha, CA; Kondo, W; Martins, LT; Rocha, JL, 2002
)
0.31
" The adverse reactions in the two groups were 13."( [Multicenter evaluation on the efficacy and safety of sparfloxacin in the treatment of acute bacterial infections].
Cai, Y; Liang, D; Miao, J; Qiu, D; Wen, C; Xu, N, 2002
)
0.31
"Domestic sparfloxacin is effective and safe in treating acute bacterial infections."( [Multicenter evaluation on the efficacy and safety of sparfloxacin in the treatment of acute bacterial infections].
Cai, Y; Liang, D; Miao, J; Qiu, D; Wen, C; Xu, N, 2002
)
0.31
"Both treatments were well-tolerated, with the majority of adverse events being GI in nature."( Efficacy and safety of azithromycin vs levofloxacin in the outpatient treatment of acute bacterial exacerbations of chronic bronchitis.
Amsden, GW; Baird, IM; Simon, S; Treadway, G, 2003
)
0.58
"5% levofloxacin ophthalmic solution was found to be safe and effective in treating pediatric bacterial conjunctivitis."( Efficacy and safety of 0.5% levofloxacin ophthalmic solution for the treatment of bacterial conjunctivitis in pediatric patients.
Lichtenstein, SJ; Rinehart, M, 2003
)
1.09
"Although it is well known that a variety of antibacterials may incidentally cause malignant arrhythmia, the list of drugs causing arrhythmia and the impact of these adverse effects are still uncertain."( Generating signals of drug-adverse effects from prescription databases and application to the risk of arrhythmia associated with antibacterials.
Bagnardi, V; Botteri, E; Carobbio, A; Corrao, G; Falcone, C; Leoni, O; Zambon, A, 2005
)
0.33
"A novel microsphere formulation of azithromycin given as a single dose was safe and effective for the treatment of ABS."( Efficacy and safety of a novel, single-dose azithromycin microsphere formulation versus 10 days of levofloxacin for the treatment of acute bacterial sinusitis in adults.
Breen, JD; Emparanza, P; Lesinskas, E; Murray, JJ; Tawadrous, M, 2005
)
0.54
"To compare overall rate of major adverse events associated with levofloxacin-containing regimen to standard therapy."( Levofloxacin treatment of active tuberculosis and the risk of adverse events.
Elwood, RK; FitzGerald, JM; Marra, CA; Marra, F; Moadebi, S; Shi, P; Stark, G, 2005
)
1.19
" Drug safety was assessed by evaluation of the nature of the adverse event, the likelihood of association with the study medications, and severity."( Levofloxacin treatment of active tuberculosis and the risk of adverse events.
Elwood, RK; FitzGerald, JM; Marra, CA; Marra, F; Moadebi, S; Shi, P; Stark, G, 2005
)
0.95
" There were no significant differences between the two groups except for indication (82% of patients in the levofloxacin group had an antecedent adverse event to first-line TB drugs, whereas 18% received levofloxacin because of resistance) and concurrent use of first-line drugs (majority of patients in the levofloxacin arm were not receiving concurrent isoniazid or rifampin)."( Levofloxacin treatment of active tuberculosis and the risk of adverse events.
Elwood, RK; FitzGerald, JM; Marra, CA; Marra, F; Moadebi, S; Shi, P; Stark, G, 2005
)
1.16
"Concomitant use of a levofloxacin-containing regimen resulted in a similar rate of adverse events compared with conventional first-line regimens when used for treatment of active TB, despite a history of adverse events."( Levofloxacin treatment of active tuberculosis and the risk of adverse events.
Elwood, RK; FitzGerald, JM; Marra, CA; Marra, F; Moadebi, S; Shi, P; Stark, G, 2005
)
1.26
" Safety evaluations included 72 h of digital continuous 12-lead Holter monitoring, 12-lead ECGs at baseline and at maximum serum concentration on day 3, and adverse events."( A randomized trial comparing the cardiac rhythm safety of moxifloxacin vs levofloxacin in elderly patients hospitalized with community-acquired pneumonia.
Anzueto, A; Choudhri, S; Dimarco, JP; Morganroth, J; Niederman, MS, 2005
)
0.56
" There were no statistically significant differences between the treatment groups with regard to drug-related adverse events."( Community-Acquired Pneumonia Recovery in the Elderly (CAPRIE): efficacy and safety of moxifloxacin therapy versus that of levofloxacin therapy.
Anzueto, A; Choudhri, SH; Heyder, A; Niederman, MS; Pearle, J; Restrepo, MI, 2006
)
0.54
"Intravenous/oral moxifloxacin therapy was efficacious and safe for hospitalized elderly patients with CAP, achieving > 90% cure in all severity and age subgroups, and was associated with faster clinical recovery than intravenous/oral levofloxacin therapy, with a comparable safety profile."( Community-Acquired Pneumonia Recovery in the Elderly (CAPRIE): efficacy and safety of moxifloxacin therapy versus that of levofloxacin therapy.
Anzueto, A; Choudhri, SH; Heyder, A; Niederman, MS; Pearle, J; Restrepo, MI, 2006
)
0.72
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" First group (NA, OFX) showed greater intrinsic tenotoxicity for young adult than immature tenocytes, second group (PEF) was highly toxic for immature and young adult cells."( Age-dependent effects on redox status, oxidative stress, mitochondrial activity and toxicity induced by fluoroquinolones on primary cultures of rabbit tendon cells.
Debray, M; Dutot, M; Martin, C; Pouzaud, F; Rat, P; Warnet, JM, 2006
)
0.33
" Adverse effects noted were nausea in 4 patients, vomiting in one and meteorism in another one, which were all difficult to distinguish from the enteric infection."( Open study on efficacy and safety of levofloxacin in treatment of uncomplicated typhoid fever.
Chen, K; Nelwan, RH; Paramita, D, 2006
)
0.6
" Adverse events were assessed using a detailed grid of classification for bacillus Calmette-Guerin related adverse events."( The effect of ofloxacin on bacillus calmette-guerin induced toxicity in patients with superficial bladder cancer: results of a randomized, prospective, double-blind, placebo controlled, multicenter study.
Chopin, D; Colombel, M; Malavaud, B; Nicolas, L; Rischmann, P; Saint, F, 2006
)
0.69
"Prophylactic ofloxacin decreased the incidence of moderate to severe adverse events associated with bacillus Calmette-Guerin intravesical therapy, particularly class III events, which are primarily associated with patient dropout."( The effect of ofloxacin on bacillus calmette-guerin induced toxicity in patients with superficial bladder cancer: results of a randomized, prospective, double-blind, placebo controlled, multicenter study.
Chopin, D; Colombel, M; Malavaud, B; Nicolas, L; Rischmann, P; Saint, F, 2006
)
1.06
"In the treatment of OE in children, once-daily ofloxacin otic solution was as effective and safe as neomycin sulfate/polymyxin B sulfate/hydrocortisone otic suspension given four times daily."( Once-daily ofloxacin otic solution versus neomycin sulfate/polymyxin B sulfate/hydrocortisone otic suspension four times a day: a multicenter, randomized, evaluator-blinded trial to compare the efficacy, safety, and pain relief in pediatric patients with
Schwartz, RH, 2006
)
0.98
"We compared adverse event data for levofloxacin 500 mg and 750 mg from clinical trials in acute bacterial sinusitis, acute bacterial exacerbation of chronic bronchitis, and community-acquired pneumonia."( Comparison of the adverse event profiles of levofloxacin 500 mg and 750 mg in clinical trials for the treatment of respiratory infections.
Kahn, JB; Khashab, MM; Xiang, J, 2006
)
0.86
"Given similar adverse event profiles and the advantages of higher dose therapy, including shorter courses of therapy and potential impact on preventing resistance, clinicians should consider utilizing the 750 mg dose of levofloxacin when choosing between dosage strengths for treatment of indicated infections."( Comparison of the adverse event profiles of levofloxacin 500 mg and 750 mg in clinical trials for the treatment of respiratory infections.
Kahn, JB; Khashab, MM; Xiang, J, 2006
)
0.78
" Adverse events were mild."( [Efficacy and safety of levofloxacin treatment of community--acquired pneumonia in hospitalized patients].
Chazan, R; Grabczak, M; Karwat, KJ, 2006
)
0.63
" Incidence of adverse events in children randomized to receive levofloxacin versus nonfluoroquinolone antibiotics was compared."( Comparative safety profile of levofloxacin in 2523 children with a focus on four specific musculoskeletal disorders.
Arguedas, A; Bagchi, P; Balis, DA; Blumer, JL; Bradley, JS; Duffy, CM; Gerbino, PG; Kauffman, RE; Noel, GJ, 2007
)
0.86
"Levofloxacin was well tolerated during and for 1 month after therapy as evidenced by similar incidence and character of adverse events compared with nonfluoroquinolone antibiotics."( Comparative safety profile of levofloxacin in 2523 children with a focus on four specific musculoskeletal disorders.
Arguedas, A; Bagchi, P; Balis, DA; Blumer, JL; Bradley, JS; Duffy, CM; Gerbino, PG; Kauffman, RE; Noel, GJ, 2007
)
1.24
"In vitro cell cultures are useful for evaluating cell response to potentially toxic insults, although cell cultures may lack tissue components that may prevent or ameliorate damage in vivo."( Intrinsic cytotoxic effects of fluoroquinolones on human corneal keratocytes and endothelial cells.
Bezwada, P; Clark, LA; Schneider, S, 2008
)
0.35
" Nausea, vomiting, and diarrhoea were the most frequently reported adverse events."( Efficacy and safety of tigecycline versus levofloxacin for community-acquired pneumonia.
Calistru, PI; Castaing, N; Chernyak, V; Cooper, CA; Dartois, N; Gandjini, H; Milutinovic, S; Strausz, J; Tanaseanu, C; Zolubas, M, 2009
)
0.61
" The most common adverse drug reactions were gastrointestinal disorders (3."( [The clinical efficacy and safety of intravenous levofloxacin in the treatment of 4888 patients with bacterial infections: a multi-center trial].
, 2009
)
0.6
"Intravenous levofloxacin with a dose of 500 mg once a day is effective and safe in treating bacterial infections with low adverse reactions."( [The clinical efficacy and safety of intravenous levofloxacin in the treatment of 4888 patients with bacterial infections: a multi-center trial].
, 2009
)
0.96
" Safety and tolerability parameters included visual acuity, ophthalmoscopy, biomicroscopy, rose bengal staining, and adverse effects."( Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers.
Holdbrook, M; Krebs, W; Rinehart, M; Walters, T, 2010
)
0.64
"3% did not differ in adverse event incidence, except for transient mild/moderate dysgeusia (14% of levofloxacin-treated subjects versus 4% of ofloxacin-treated subjects)."( Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers.
Holdbrook, M; Krebs, W; Rinehart, M; Walters, T, 2010
)
0.85
"5% produced tear fluid concentrations that were well above the minimum inhibitory concentration90 for typical ocular pathogens and was safe and well tolerated."( Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers.
Holdbrook, M; Krebs, W; Rinehart, M; Walters, T, 2010
)
0.64
"The aim of this study was to assess the long-term toxic effect of ofloxacin on the testes and epididymides of 72 adult male albino rats."( Long-term ofloxacin testicular toxicity: an experimental study.
Abo El-Atta, HM; El-Harouny, MA; El-Shawaf, IM; Mostafa, T; Naser, ME; Zalata, AA, 2010
)
1
" Although very useful agents, the fluoroquinolones as a class are associated with a number of adverse events, some with considerable clinical significance."( Safety profile of the fluoroquinolones: focus on levofloxacin.
Liu, HH, 2010
)
0.61
" There was no difference among the treatment groups with regard to the incidence and severity of adverse events reported."( Efficacy and safety of Levofloxacin, Clarithromycin and Esomeprazol as first line triple therapy for Helicobacter pylori eradication in Middle East. Prospective, randomized, blind, comparative, multicenter study.
Abdelfatah, M; Assem, M; El Azab, G; Rasheed, MA; Shastery, M, 2010
)
0.66
" All three treatments were well tolerated, and no drug-related serious adverse events were observed."( Efficacy and safety of nemonoxacin versus levofloxacin for community-acquired pneumonia.
Bester, AJ; Chang, LW; Chang, YT; Chung, DT; Ho, ML; Hsu, MC; Kasumba, J; King, CH; Mitha, IH; Perng, RP; van Rensburg, DJ; Wu, RG, 2010
)
0.62
" Doripenem was generally found to be safe and well tolerated."( Safety and efficacy of intravenous doripenem for the treatment of complicated urinary tract infections and pyelonephritis.
Damiao, R; Davies, T; Kaniga, K; Kotey, P; Naber, KG; Redman, R, 2010
)
0.36
" However there is insufficient toxic information about levofloxacin n-oxide."( In silico and in vitro genotoxicity evaluation of levofloxacin n-oxide, an impurity in levofloxacin.
Guo, M; Li, J; Li, T; Wang, W; Zhang, X; Zhu, Q, 2012
)
0.87
"This randomized, prospective, multicenter, open-label study was designed to test whether a topical, electrolyzed, superoxidized solution (Microcyn Rx) is a safe and effective treatment for mildly infected diabetic foot ulcers."( An open-label, three-arm pilot study of the safety and efficacy of topical Microcyn Rx wound care versus oral levofloxacin versus combined therapy for mild diabetic foot infections.
Blume, PA; Gutierrez, A; Jordan, DA; Landsman, A; Vayser, D,
)
0.34
"Microcyn Rx is safe and at least as effective as oral levofloxacin for mild diabetic foot infections."( An open-label, three-arm pilot study of the safety and efficacy of topical Microcyn Rx wound care versus oral levofloxacin versus combined therapy for mild diabetic foot infections.
Blume, PA; Gutierrez, A; Jordan, DA; Landsman, A; Vayser, D,
)
0.59
"The physicochemical properties of racemates and stereoisomers of medicines can differ significantly, and this may affect the side-effect profile in addition to the pharmacokinetics and intended pharmacology."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
"This is a study to investigate the profile of adverse drug reactions of racemic and enantiomeric forms of drugs."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" A case-noncase approach was used to measure the disproportionality of combination between adverse drug reaction (ADR) and exposure to drug."( Safety profile of enantiomers vs. racemic mixtures: it's the same?
Bagheri, H; Caillet, C; Chauvelot-Moachon, L; Montastruc, JL, 2012
)
0.38
" Vigamox(®) containing moxifloxacin and Tosuflo(®) containing tosufloxacin were more toxic when compared with the other antibiotics."( In vitro assessment of the cytotoxicity of six topical antibiotics to four cultured ocular surface cell lines.
Ayaki, M; Iwasawa, A; Niwano, Y, 2012
)
0.38
" Bacterial clearance rate, clinical symptoms/signs, adverse reactions and disease recurrence were assessed."( Safety and efficacy of levofloxacin versus ciprofloxacin for the treatment of chronic bacterial prostatitis in Chinese patients.
Guo, YL; Jin, FS; Liu, DM; Shen, ZJ; Sun, YH; Zhang, ZC, 2012
)
0.68
" An increase in toxicity was observed during chlorination suggesting that the first transformations products formed were more toxic than the parent compound."( Aqueous chlorination of levofloxacin: kinetic and mechanistic study, transformation product identification and toxicity.
Deborde, M; El Najjar, NH; Journel, R; Vel Leitner, NK, 2013
)
0.69
" In practice, adverse events (AEs) of BCG therapy could restrict its prescription by urologists."( [Diagnosis and management of adverse events occuring during BCG therapy for non-muscle invasive bladder cancer (NMIBC): review of the Cancer Committee of the French Association of Urology].
Davin, JL; Irani, J; Larré, S; Moreau, JL; Neuzillet, Y; Pfister, C; Pignot, G; Rouprêt, M; Soulié, M; Wallerand, H, 2012
)
0.38
" More patients treated with levofloxacin than with solithromycin experienced treatment-emergent adverse events (TEAEs) during the study (45."( Randomized, double-blind, multicenter phase 2 study comparing the efficacy and safety of oral solithromycin (CEM-101) to those of oral levofloxacin in the treatment of patients with community-acquired bacterial pneumonia.
Clark, K; Craft, JC; Das, A; Fernandes, P; Jamieson, BD; Oldach, D; Schranz, J; Scott, D, 2013
)
0.88
" No adverse drug reactions were observed."( [Efficacy and safety of levofloxacin to non-gonorrheal urethritis].
Hosobe, T; Kato, T; Onodera, S; Onoe, Y; Yoshida, M, 2012
)
0.68
" Hence, new alternative schemes and monitoring of adverse effects to avoid treatment abandonment are important considerations."( Adverse effects of alternative therapy (minocycline, ofloxacin, and clofazimine) in multibacillary leprosy patients in a recognized health care unit in Manaus, Amazonas, Brazil.
Cunha, CS; Cunha, Mda G; Maia, MV,
)
0.38
" The mean time for the development of adverse effects after beginning the therapy was 15."( Adverse effects of alternative therapy (minocycline, ofloxacin, and clofazimine) in multibacillary leprosy patients in a recognized health care unit in Manaus, Amazonas, Brazil.
Cunha, CS; Cunha, Mda G; Maia, MV,
)
0.38
" Nine patients (2 with liver dysfunction, 6 with renal dysfunction and 1 with thrombocytopenia) out of 62 patients were reported to have possible adverse effects of LVFX."( [Efficacy and safety of levofloxacin in patients with nursing and healthcare-associated pneumonia].
Akata, K; Awaya, Y; Chojin, Y; Hara, K; Hata, R; Inoue, N; Ishimoto, H; Kato, K; Kawanami, T; Kawanami, Y; Mukae, H; Naito, K; Nishida, C; Noguchi, S; Obata, H; Oda, K; Ogoshi, T; Orihashi, T; Sasahara, Y; Shimabukuro, I; Shiraishi, T; Suzuki, Y; Tachiwada, T; Takaki, T; Taura, Y; Tokuyama, S; Tsuda, T; Uchimura, K; Yamasaki, K; Yatera, K; Yoshida, Y; Yoshii, C, 2014
)
0.7
" However, the pre-irradiated ofloxacin solutions in comparison to samples stored in the dark were significantly more genotoxic to bacteria, slightly increased the number of micronuclei in V79 cell line and were toxic to the yeast strain."( Evaluation of photodegradation, phototoxicity and photogenotoxicity of ofloxacin in ointments with sunscreens and in solutions.
Nałęcz-Jawecki, G; Parzonko, A; Siedlecka, E; Sikorska, K; Skrzypczak, A; Sommer, S; Welenc, I; Zgadzaj, A; Ługowska, A, 2015
)
0.94
" OFX was toxic for the bacteria and the microalgae at the spiked concentration in untreated water."( Continuous ozonation treatment of ofloxacin: transformation products, water matrix effect and aquatic toxicity.
Carbajo, JB; Fernández-Alba, AR; García-Calvo, E; Herrera, S; Letón, P; Perdigón-Melón, JA; Petre, AL; Rosal, R, 2015
)
0.7
" In the present study, the efficacy and safety of ofloxacin alone (OA) and the ofloxacin + dexamethasone combination (ODC) is compared by studying clinical cure rates and adverse drug reactions in patients with CSOM."( Efficacy and safety of ofloxacin and its combination with dexamethasone in chronic suppurative otitis media. A randomised, double blind, parallel group, comparative study.
Jha, S; Mandavia, D; Panchasara, A; Singh, A; Tripathi, C, 2015
)
0.98
" Ofloxacin was safe and well tolerated in children with MDR-TB, but exposures were well below reported adult values, suggesting that dosage modification may be required to optimize MDR-TB treatment regimens in children."( Pharmacokinetics and Safety of Ofloxacin in Children with Drug-Resistant Tuberculosis.
Castel, S; Dooley, KE; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Seddon, JA; Thee, S; Wiesner, L, 2015
)
1.61
" Adverse events associated with second-line drugs (SLDs) can have severe impact on efficient management."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"To know the frequency of adverse events due to SLDs in patients of MDR-TB."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
" Adverse events associated with treatment were recognized primarily by clinical evidence and/or laboratory investigations that were advised at baseline and whenever clinically indicated during course of treatment."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"119 adverse events were reported in 46 (46."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
"MDR-TB can be cured successfully with appropriate combination of drugs if adverse events associated with them can be managed aggressively and timely."( Frequency of adverse events observed with second-line drugs among patients treated for multidrug-resistant tuberculosis.
Hosmane, GB; Jain, A; Kushwaha, RA; Prasad, R; Singh, A; Srivastava, R, 2016
)
0.43
" Using a standard cytotoxicity assay, the products at varying concentrations were evaluated with a corneal fibroblast cell line and a macrophage-like cell line to determine their potential toxic effect in vitro."( Antibacterial activity and safety of commercial veterinary cationic steroid antibiotics and neutral superoxidized water.
Abdelkhalek, A; Bergstrom, BE; Hammac, GK; Seleem, MN; Townsend, WM; Younis, W, 2018
)
0.48
" The total incidence of adverse events during the eradication therapy did not significantly differ between the ACLA and LCLA groups (31."( Antofloxacin-based bismuth quadruple therapy is safe and effective in Helicobacter pylori eradication: A prospective, open-label, randomized trial.
He, XJ; Jiang, CS; Li, DZ; Liu, G; Wang, W; Zeng, XP, 2021
)
1.24
" Two groups exhibited similar adverse event rates (AEA 14."( Efficacy and Safety of Antofloxacin-Based Triple Therapy for Helicobacter pylori Eradication Failure in China.
He, XJ; Jiang, CS; Li, DZ; Liu, G; Wang, W; Zeng, XP, 2022
)
1.02

Pharmacokinetics

Levofloxacin (LVFX, DR-3355) was evaluated pharmacokinetic and clinically in the field of obstetrics and gynecology. Plasma concentrations were determined by high-performance liquid chromatography. Pharmacokinetic parameters were determined.

ExcerptReferenceRelevance
" Two pharmacokinetic studies were performed for each quinolone, on days four and eight of the treatment."( Effects of ketoprofen (NSAID) on the pharmacokinetics of pefloxacin and ofloxacin in healthy volunteers.
Borsa-Lebas, F; Etienne, I; Fillastre, JP; Gy, C; Humbert, G; Leroy, A, 1992
)
0.52
" The pharmacokinetic characteristics were studied."( [Determination of ofloxacin in human plasma and studies of its pharmacokinetics using HPLC method].
Diao, Y; Ding, AZ; Xu, DK; Yuan, YS, 1992
)
0.62
"Levofloxacin (LVFX, DR-3355) a new synthetic antibacterial agent, was evaluated pharmacokinetic and clinically in the field of obstetrics and gynecology and the following results were obtained."( [Pharmacokinetic and clinical evaluation of levofloxacin in obstetrical and gynecological field].
Hirayama, H; Matsuda, S; Oh, K, 1992
)
1.16
" The pharmacokinetics of ofloxacin are characterised by almost complete bioavailability (95 to 100%), peak serum concentrations in the range of 2 to 3 mg/L after a 400mg oral dose and an average half-life of 5 to 8h."( Ofloxacin clinical pharmacokinetics.
Bailey, EM; Lamp, KC; Rybak, MJ, 1992
)
2.03
" The concentration in hair of the pigmented rats correlated significantly with the daily dose, area under the plasma concentration curve (AUC), and maximum plasma concentration (Cmax) at steady state, whereas that in the albino rats correlated with the dose and Cmax only, because AUC did not increase linearly with the dose in the albino rats."( Possible effect of pigment on the pharmacokinetics of ofloxacin and its excretion in hair.
Miyazawa, N; Nakashima, M; Okazaki, O; Uematsu, T, 1992
)
0.53
"We studied the pharmacokinetic parameters of four fluoroquinolones--ofloxacin, ciprofloxacin, temafloxacin and sparfloxacin--in a mouse model of Streptococcus pneumoniae-infected lung."( Pharmacokinetics of four fluoroquinolones in an animal model of infected lung.
Azoulay-Dupuis, E; Bergogne-Bérézin, E; Pocidalo, JJ; Vallée, E, 1991
)
0.52
" Consequently, the serum half-life progressively increases when creatinine clearance decreases."( Ofloxacin pharmacokinetics in chronic renal failure and dialysis.
Lameire, N; Lehr, KH; Malerczyk, V; Ringoir, S; Rosenkranz, B; Veys, N, 1991
)
1.72
" Apparent total body and renal clearances declined and elimination half-life increased with decreasing creatinine clearance."( Pharmacokinetics of ofloxacin in healthy subjects and patients with varying degrees of renal impairment.
Flor, S; Guay, D; Matzke, G; Opsahl, J; Tack, K, 1991
)
0.6
"The pharmacokinetic properties of the new fluoroquinolones are characterized by a high volume of distribution, long biological half-life, low serum protein binding, elimination by renal and extrarenal mechanisms with high total and renal clearances, limited biotransformation and moderate to excellent bioavailability after oral administration."( Quinolone pharmacokinetics and metabolism.
Boeckk, M; Borner, K; Deppermann, N; Höffken, G; Koeppe, P; Lode, H, 1990
)
0.28
" For the other new quinolones, a decrease in glomerular filtration rate below 20-30 ml/min induces an increase in terminal half-life and a decrease in plasma and renal clearance, related to the degree of renal impairment."( Pharmacokinetics of quinolones in renal insufficiency.
Borsa-Lebas, F; Dhib, M; Fillastre, JP; Humbert, G; Leroy, A; Moulin, B, 1990
)
0.28
"The principal pharmacokinetic values of pefloxacin, ofloxacin and ciprofloxacin were obtained from a review of the literature."( [Serum pharmacokinetics and in vitro antibacterial activity of pefloxacin, ofloxacin and ciprofloxacin].
Jarlier, V; Nordmann, P,
)
0.61
" The choice of the initial dosage regimen actually takes into account toxicological, bacteriological and pharmacokinetic parameters."( A new approach to optimal antibiotic dosage regimen by coupling pharmacokinetics and killing curve parameters.
Dellamonica, P; Drugeon, HB; Etesse, H; Garraffo, R; Lapalus, P, 1990
)
0.28
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" To study the pharmacokinetic behavior at the target site in bacterial infection of the skin, drug concentrations were determined in suction blister fluid (SBF) and cantharides blister fluid (CBF), as well as in serum and saliva."( Multiple-dose pharmacokinetics of ofloxacin in serum, saliva, and skin blister fluid of healthy volunteers.
Korting, HC; Mutschler, E; Schäfer-Korting, M; Warlich, R, 1990
)
0.56
" Pharmacokinetic studies were performed on day 1 (D1) and 7 (D7)."( [Modification of ofloxacin pharmacokinetics induced by prolonged mechanical ventilation].
Bruguerolle, B; Fleurette, J; Freney, J; Gouin, F; Lambert, D; Martin, C; Meugnier, H; Saux, P, 1990
)
0.62
"The possible pharmacokinetic interaction between a new quinolone and fenbufen was investigated by comparing the plasma concentration-time profiles and serum protein binding of ofloxacin, fenbufen and its active metabolite, felbinac, in rats."( Absence of pharmacokinetic interaction between ofloxacin and fenbufen in rats.
Hayashibara, M; Ichikawa, N; Iwamoto, K; Katagiri, Y; Naora, K, 1989
)
0.73
" In the young and elderly, ofloxacin is eliminated with a half-life of five to seven hours, independent of dose."( Pharmacokinetics of ofloxacin. An overview.
Flor, S, 1989
)
0.9
" Mean plasma elimination half-life was 11."( Oral pharmacokinetics and ascitic fluid penetration of ofloxacin in cirrhosis.
Beauchant, M; Becq-Giraudon, B; Bouquet, S; Breux, JP; Silvain, C, 1989
)
0.52
" Relevant pharmacokinetic parameters were analysed by both noncompartmental and compartmental models."( Pharmacokinetics of a single dose of ofloxacin in healthy elderly subjects using noncompartmental and compartmental models.
Glerum, JH; Jones, RW; Notarianni, LJ; Rademaker, CM; van Dijk, A; Verhoef, J, 1989
)
0.55
" Ofloxacin's more favorable pharmacokinetic profile seems to compensate at least in part for the greater activity of ciprofloxacin against gram-negative bacilli in vitro."( Comparative pharmacokinetics of ofloxacin and ciprofloxacin.
Hooper, DC; Wolfson, JS, 1989
)
1.47
" The half-life of ofloxacin was markedly prolonged, to 23."( Pharmacokinetics of ofloxacin in severe chronic renal failure.
Bandai, H; Iida, N; Nakanishi, I; Okada, N; Tsubakihara, Y; Yamato, E; Yokoyama, K,
)
0.79
"Comparative physiological pharmacokinetic analysis has been carried out to elucidate the different tissue distribution characteristics among eight pyridonecarboxylic acids including newly developed NY-198."( Structure-tissue distribution relationship based on physiological pharmacokinetics for NY-198, a new antimicrobial agent, and the related pyridonecarboxylic acids.
Kato, H; Nagata, O; Nakamura, M; Okezaki, E; Terasaki, T; Tsuji, A,
)
0.13
" A dosing schedule for the quinolones was proposed on the basis of pharmacokinetic parameters and microbiologic activity."( Pharmacokinetics of the quinolones in volunteers: a proposed dosing schedule.
Andrews, JM; Griggs, D; Wise, R,
)
0.13
" Furthermore, there was a broad fluctuation of approximately 80% between the Cmax and Cmin in the plasma levels of the drug during a 12-hour dosing interval."( Pharmacokinetics and tissue distribution of ofloxacin in human subjects during a multiple dose regimen.
Bonaccorsi, S; Carlino, S; De Bernardis, E; Picari, M; Rizza, V, 1988
)
0.54
" The mean serum elimination half-life was 7 h and 80."( The pharmacokinetics of ofloxacin and a review of its tissue penetration.
Lockley, MR; Wise, R, 1988
)
0.58
" Pharmacokinetic parameters were calculated on the basis of an open three-compartment model, which resulted in a high volume of distribution for both substances (166-246 1 for ofloxacin, 178-2611 for ciprofloxacin)."( Comparative pharmacokinetics of intravenous ofloxacin and ciprofloxacin.
Borner, K; Höffken, G; Kirch, A; Koeppe, P; Lode, H; Olschewski, P; Sievers, B, 1988
)
0.73
" Pharmacokinetic parameters were determined from the plasma decay curves of the single and the last of the multiple administrations."( Pharmacokinetics of ofloxacin after single and multiple intravenous infusions in healthy subjects.
Bocquet, V; Carbon, C; Farinotti, R; Trouvin, JH; Vermerie, N, 1988
)
0.6
" However, the pharmacokinetic profile of ofloxacin is superior to that of ciprofloxacin, with more rapid absorption and a peak serum concentration several times higher."( Ofloxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.
Campoli-Richards, DM; Monk, JP, 1987
)
1.98
"The pharmacokinetic interactions of ofloxacin (2 X 200 mg) and theophylline (3 X 200 mg) were investigated in 12 healthy volunteers over a period of two weeks."( Pharmacokinetics of ofloxacin and theophylline alone and in combination.
Beck, S; Fourtillan, JB; Granier, J; Saint-Salvi, B; Salmon, J; Surjus, A; Tremblay, D; Vincent Du Laurier, M, 1986
)
0.87
" High serum Cmax levels (4."( Multiple-dose pharmacokinetics of ofloxacin, a new broad-spectrum antimicrobial agent.
Dagrosa, EE; de Looze, S; Hajdú, P; Malerczyk, V; Toyodera, K; Verho, M, 1986
)
0.55
" The pharmacokinetic parameters were obtained using an open one-compartment model."( Pharmacokinetics of a single oral dose of ofloxacin in patients with renal failure.
Moukhtar, I; Nawishy, S; Sabbour, M, 1986
)
0.54
" An open three-compartment body model was used to calculate ofloxacin pharmacokinetic parameters."( Ofloxacin pharmacokinetics in renal failure.
Fillastre, JP; Humbert, G; Leroy, A, 1987
)
1.96
" Pharmacokinetic parameters were calculated on the basis of open two- and three-compartment models, which yielded nearly identical results."( Pharmacokinetics of ofloxacin after parenteral and oral administration.
Borner, K; Höffken, G; Kirch, A; Koeppe, P; Lode, H; Olschewski, P; Sievers, B, 1987
)
0.6
"The steady state pharmacokinetic properties of ciprofloxacin and ofloxacin were compared in cystic fibrosis patients."( Comparative pharmacokinetics of ciprofloxacin and ofloxacin in cystic fibrosis patients.
Hvidberg, EF; Jensen, T; Pedersen, SS, 1987
)
0.8
" single) and showed no significant effect on total body clearance, serum half-life (T1/2) and AUC of theophylline, while enoxacin by the same pretreatment increased significantly serum theophylline concentrations and resulted in significant effect on all the pharmacokinetic parameters."( Lack of effect of ofloxacin on theophylline pharmacokinetics in rats.
Miyazaki, K; Okazaki, O; Tachizawa, H, 1987
)
0.61
"The pharmacokinetic properties of the new quinolones are characterised by a high volume of distribution, long biological half-life, low serum protein binding, elimination mainly by the kidneys, high total and renal clearances, limited biotransformation and a moderate to excellent bioavailability after oral administration."( Comparative pharmacokinetics of new quinolones.
Borner, K; Glatzel, P; Höffken, G; Koeppe, P; Lode, H; Olschewski, P; Prinzing, C; Reimnitz, D; Sievers, B; Wiley, R, 1987
)
0.27
" In 2 patients with chronic renal failure, specific HPLC assay indicated an extended half-life for ofloxacin (approximately 13 hours) and the appearance in serum of low concentrations of both metabolites after 10 hours, persisting until the last blood sample was taken (32 hours)."( A preliminary report on the pharmacokinetics of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide in patients with chronic renal failure.
Lovering, AM; MacGowan, AP; Mackay, IG; Reeves, DS; White, LO, 1987
)
0.75
"Serum concentrations and pharmacokinetic parameters of ofloxacin were measured in 10 patients on haemodialysis treatment."( Pharmacokinetics of ofloxacin in patients on haemodialysis treatment.
Burkhardt, F; Dörfler, A; Schulz, W; Zichner, M, 1987
)
0.84
"7 hours after administration and the mean elimination half-life of OFX was 25 hours."( Ofloxacin pharmacokinetics in patients on continuous ambulatory peritoneal dialysis.
Chan, MK; Chan, WW; Chau, PY, 1987
)
1.72
" The mean serum elimination half-life was 7 h and 80."( The pharmacokinetics and tissue penetration of ofloxacin.
Dent, J; Lockley, MR; Wise, R, 1984
)
0.52
" The pharmacokinetic parameters were determined with RSTRIP, an iterative, nonlinear, weighted, least-squares regression program."( Pharmacokinetics of ofloxacin in serum and vitreous humor of albino and pigmented rabbits.
Drusano, G; Liu, W; Madu, A; Madu, C; Mayers, M; Miller, MH; Perkins, RJ, 1995
)
0.61
"The pharmacodynamic properties of levofloxacin (an optically active isomer of ofloxacin), ofloxacin, and ciprofloxacin, alone and in combination with rifampin, were evaluated over 24 to 48 h against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus (MSSA 1199 and MRSA 494, respectively) in an in vitro infection model."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
0.87
"This paper reports the pharmacokinetic characteristics of ofloxacin (Ofl) through 3 administration routes in 42 patients with respiratory tract infections."( Pharmacokinetics of ofloxacin through three administration routes.
Ling, SS; Lu, JZ; Xia, XR; Zhuo, HT, 1994
)
0.86
" These data suggest the usefulness of microdialysis for pharmacokinetic studies in the anterior chamber, since continuous and stable data can be obtained from each animal."( [Application of microdialysis for pharmacokinetic study in rabbit anterior chamber].
Fukuda, S; Inatomi, M; Kanda, Y; Koide, R; Kurata, N; Mikitani, M; Uchida, E; Uchida, N; Ueda, T; Yasuhara, H, 1995
)
0.29
" The influences of renal function, age, meals and concurrent drug administration on the pharmacokinetic parameters of LVFX were examined by the likelihood ratio test using a nonlinear mixed-effect model (NONMEM)."( Premarketing population pharmacokinetic study of levofloxacin in normal subjects and patients with infectious diseases.
Hori, R; Kagimoto, N; Nomura, H; Okumura, K; Tanigawara, Y, 1995
)
0.54
" This method was applied to the pharmacokinetic study of ofloxacin in 24 chronic obstructive pulmonary disease patients."( A reproducible, simple and sensitive HPLC assay for determination of ofloxacin in plasma and lung tissue. Application in pharmacokinetic studies.
Bouvet, O; Bressolle, F; Fabre, D; Galtier, M; Kinowski, JM; Paganin, F, 1994
)
0.77
"Bactericidal activities of isepamicin and ofloxacin against Pseudomonas aeruginosa E7 were examined using an in vitro computer programmed pharmacokinetic simulation system."( [Bactericidal activities of isepamicin and ofloxacin against Pseudomonas aeruginosa evaluated using an in vitro pharmacokinetic simulation system].
Goto, S; Kaneko, Y; Tsuji, A; Yamaguchi, K, 1994
)
0.82
" Mean +/- standard deviation levofloxacin pharmacokinetic parameters (by noncompartmental moment method) after multiple dosing were as follows: area under the concentration-time curve, 31."( Pharmacokinetics and safety of levofloxacin in patients with human immunodeficiency virus infection.
Bartlett, JA; Chow, AT; Flor, SC; Gallis, HA; Goodwin, SD; Wong, FA, 1994
)
0.85
" Elimination half-life (T1/2) of ofloxacin was markedly prolonged compared to patients with normal renal function."( Single-dose pharmacokinetics of intraperitoneal ofloxacin in patients on continuous ambulatory peritoneal dialysis.
Chan, CY; Chau, PY; Cheng, IK; Kou, M; Kumana, CR; Siu, LK, 1993
)
0.82
" There were no significant differences in any pharmacokinetic parameters of LVFX between the groups."( Effects of traditional Chinese medicines on pharmacokinetics of levofloxacin.
Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K; Yamaki, K, 1995
)
0.53
"The greater potency of ciprofloxacin in vitro to that of ofloxacin against Pseudomonas aeruginosa may be potentially offset by the more favorable pharmacokinetic profile of the latter drug."( A pharmacodynamic evaluation of ciprofloxacin and ofloxacin against two strains of Pseudomonas aeruginosa.
Larsson, AJ; Madaras-Kelly, KJ; Rotschafer, JC, 1996
)
0.87
" Using an in vitro pharmacodynamic model, 29 duplicate concentration time-kill curve experiments simulated AUC/MIC24s ranging from 52 to 508 SIT-1."( Twenty-four-hour area under the concentration-time curve/MIC ratio as a generic predictor of fluoroquinolone antimicrobial effect by using three strains of Pseudomonas aeruginosa and an in vitro pharmacodynamic model.
Hovde, LB; Madaras-Kelly, KJ; Ostergaard, BE; Rotschafer, JC, 1996
)
0.29
"We compared the pharmacodynamic activities of levofloxacin versus vancomycin, with or without rifampin, in an in vitro model with infected platelet-fibrin clots simulating vegetations."( Pharmacodynamics of once- or twice-daily levofloxacin versus vancomycin, with or without rifampin, against Staphylococcus aureus in an in vitro model with infected platelet-fibrin clots.
Palmer, SM; Rybak, MJ, 1996
)
0.81
" Blood and urine samples were obtained and pharmacokinetic parameters for procainamide were determined for each treatment period."( Effects of ofloxacin on the pharmacokinetics and pharmacodynamics of procainamide.
Cascio, W; Griener, J; Martin, DE; Patterson, JH; Raasch, R; Shen, J, 1996
)
0.68
" The pharmacokinetic parameters of both enantiomers of warfarin were comparable in the absence and presence of levofloxacin, with no significant differences noted in warfarin peak plasma concentration, time to peak plasma concentration, apparent total body clearance, and terminal disposition half-life."( Absence of an effect of levofloxacin on warfarin pharmacokinetics and anticoagulation in male volunteers.
Fowler, C; Liao, S; Nayak, RK; Palmer, M, 1996
)
0.8
"The pharmacodynamic effects of amikacin, imipenem, ofloxacin, rifampin, and vancomycin were studied on the slime-producing, oxacillin-resistant strain Staphylococcus epidermidis ATCC 35984 growing in Mueller Hinton broth or, in order to inhibit growth, incubated in phosphate-buffered saline."( Pharmacodynamic effects of antibiotics and antibiotic combinations on growing and nongrowing Staphylococcus epidermidis cells.
Hanberger, H; Nilsson, LE; Svensson, E, 1997
)
0.55
" The pharmacokinetic studies demonstrated the possible prediction of the drug blood concentrations after the multiple administrations based on the calculated parameters."( [Clinical and pharmacokinetic evaluation of ofloxacin under various regimens of administration in patients with bronchopulmonary infections].
Belousov, OB; Efremenkova, OV; Gutkin, AB; Sokolov, AV; Tishchenkova, IF, 1996
)
0.56
" The apparent differences in the calculated pharmacokinetic parameters for levofloxacin between the age groups (young versus elderly) and between the gender groups (males versus females) could be explained by differences in renal function among the subjects."( Absence of age and gender effects on the pharmacokinetics of a single 500-milligram oral dose of levofloxacin in healthy subjects.
Chien, SC; Chow, AT; Natarajan, J; Nayak, RK; Rogge, MC; Williams, RR; Wong, FA, 1997
)
0.74
" Pharmacokinetic profiles of levofloxacin from single doses and multiple (three-times-daily) doses were similar, with a moderate accumulation (observed day 10-to-day 1 ratio of the maximum plasma concentration, approximately 185% versus expected 169%; for the corresponding ratio of the area under the concentration-time curve from 0 to 8 h [AUC(0-8)], the values were observed 217% versus expected 169%) at steady state."( Pharmacokinetics and safety of oral levofloxacin in human immunodeficiency virus-infected individuals receiving concomitant zidovudine.
Chien, SC; Chow, AT; Hendrix, CW; Rogge, MC; Williams, RR, 1997
)
0.85
" MAC organisms were inoculated into tubes containing the medium with or without the addition of test drugs at either 1/10 Cmax, Cmax or C0-8h (average concentrations during the first 8 h) in the blood."( [Anti-Mycobacterium avium complex activities of KRM-1648, clarithromycin and levofloxacin in 7HSF medium at peak or average blood concentrations after their oral administration of clinical dosages].
Akaki, T; Sato, K; Tomioka, H, 1997
)
0.52
" Pharmacokinetic parameters were estimated by noncompartmental methods."( Pharmacokinetic profile of levofloxacin following once-daily 500-milligram oral or intravenous doses.
Cheung, WK; Chien, SC; Chow, AT; Curtin, C; Fowler, CL; Gisclon, LG; Natarajan, J; Rogge, MC; Williams, RR; Wong, F, 1997
)
0.59
" Mean (+/-SD) values for theophylline pharmacokinetic parameters for the levofloxacin and placebo treatments, respectively, were peak plasma concentrations (Cmax) of 11."( Absence of a pharmacokinetic interaction between intravenous theophylline and orally administered levofloxacin.
Curtin, CR; Fowler, CL; Gisclon, LG; Hafkin, B; Natarajan, J; Williams, RR, 1997
)
0.74
" This pharmacokinetic modeling could be used to determine optimal treatment dose in clinical trials in a shorter time frame with fewer patients."( Pharmacodynamics of levofloxacin: a new paradigm for early clinical trials.
Berman, AL; Chow, AT; Corrado, M; Dornseif, B; Drusano, GL; Fowler, CL; Natarajan, J; Preston, SL; Reichl, V, 1998
)
0.61
" Pharmacokinetic parameters were estimated by model-independent methods."( Double-blind evaluation of the safety and pharmacokinetics of multiple oral once-daily 750-milligram and 1-gram doses of levofloxacin in healthy volunteers.
Callery-D'Amico, SV; Chien, SC; Chow, AT; Fowler, CL; Nayak, R; Williams, RR; Wong, FA, 1998
)
0.51
"Population pharmacokinetic modeling is a useful approach to obtaining estimates of both population and individual pharmacokinetic parameter values."( Levofloxacin population pharmacokinetics and creation of a demographic model for prediction of individual drug clearance in patients with serious community-acquired infection.
Berman, AL; Chow, AT; Corrado, M; Dornseif, B; Drusano, GL; Fowler, CL; Natarajan, J; Preston, SL; Reichl, V; Wong, FA, 1998
)
0.92
"We examined the relation between the pharmacokinetic disposition and arthropathic potential of ofloxacin, a new quinolone antibacterial agent, using both male immature (3-month-old) and mature (18-month-old) beagles."( Pharmacokinetic disposition and arthropathic potential of oral ofloxacin in dogs.
Furuhama, K; Nishida, S; Ohshima, C; Sekiguchi, M; Yabe, K; Yamada, K; Yamamoto, N; Yoshida, K, 1998
)
0.76
" Plasma concentrations of ofloxacin were determined by high-performance liquid chromatography and pharmacokinetic parameters were determined."( Effect of gender on the pharmacokinetics of ofloxacin.
Abel, SR; Clark, WR; Mueller, BA; Sowinski, KM, 1999
)
0.86
" Except for terminal elimination half-life, which was 10% shorter in women, no other pharmacokinetic values were significantly different between genders."( Effect of gender on the pharmacokinetics of ofloxacin.
Abel, SR; Clark, WR; Mueller, BA; Sowinski, KM, 1999
)
0.56
"An in vitro pharmacokinetic model was used to simulate the pharmacokinetics of trovafloxacin, ofloxacin, and ciprofloxacin in human serum and to compare their pharmacodynamics against eight Streptococcus pneumoniae strains."( Pharmacodynamics of trovafloxacin, ofloxacin, and ciprofloxacin against Streptococcus pneumoniae in an in vitro pharmacokinetic model.
Lister, PD; Sanders, CC, 1999
)
0.8
"An in-vitro pharmacokinetic model was used to compare the pharmacodynamics of levofloxacin and ciprofloxacin against four penicillin-susceptible and four penicillin-resistant Streptococcus pneumoniae."( Pharmacodynamics of levofloxacin and ciprofloxacin against Streptococcus pneumoniae.
Lister, PD; Sanders, CC, 1999
)
0.84
" An in-vitro pharmacodynamic model was used."( Pharmacodynamics of levofloxacin and ofloxacin against Streptococcus pneumoniae.
Bauernfeind, A, 1999
)
0.61
" Levofloxacin pharmacokinetic parameters for HIV-infected patients were consistent with those observed in studies of healthy volunteers."( Pharmacokinetics and safety of high-dose and extended-interval regimens of levofloxacin in human immunodeficiency virus-infected patients.
Baird, B; Chow, AT; Fowler, CL; Masur, H; Natarajan, J; Piscitelli, SC; Spooner, K; Walker, RE; Williams, RR, 1999
)
1.09
" Pharmacodynamic principles can also be used to devise the optimal administration regimen for specific antimicrobial agents."( Pharmacodynamics and pharmacokinetics of levofloxacin.
Grant, EM; Nightingale, CH; Quintiliani, R, 2000
)
0.57
"For simple pharmacokinetic compartmental models, analytical solution to the governing differential equations along with common graphical methods provide a mean to evaluate the associated rate constants."( Application of direct search optimization for pharmacokinetic parameter estimation.
Ahmadi, AM; Gerayeli, A; Khorasheh, F; Sattari, S,
)
0.13
"The methodology is demonstrated with reference to experimental literature data for ciprofloxacin and ofloxacin whose pharmacokinetic behavior has been reported in terms of a two-compartment model."( Application of direct search optimization for pharmacokinetic parameter estimation.
Ahmadi, AM; Gerayeli, A; Khorasheh, F; Sattari, S,
)
0.35
" Multiple regression tested association of pharmacodynamic variables with antimicrobial effect, and logistic regression with resistance post TKC."( In vitro characterization of fluoroquinolone concentration/MIC antimicrobial activity and resistance while simulating clinical pharmacokinetics of levofloxacin, ofloxacin, or ciprofloxacin against Streptococcus pneumoniae.
Demasters, TA; Madaras-Kelly, KJ, 2000
)
0.51
" With each organism, a series of monoexponential pharmacokinetic profiles of single doses of moxifloxacin (T:1/2 = 12."( Comparative pharmacodynamics of moxifloxacin and levofloxacin in an in vitro dynamic model: prediction of the equivalent AUC/MIC breakpoints and equiefficient doses.
Firsov, AA; Kononenko, OV; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2000
)
0.56
" Inter-subject pharmacokinetic and MIC variability may impact the probability of attaining optimal AUC:MIC ratios and hence favorable clinical outcome."( The use of Monte Carlo simulation to examine pharmacodynamic variance of drugs: fluoroquinolone pharmacodynamics against Streptococcus pneumoniae.
Ambrose, PG; Grasela, DM, 2000
)
0.31
" For this to occur, the clinician should be cognizant of many clinical, microbiologic, pharmacologic, and epidemiologic data as well as fundamental pharmacodynamic concepts."( Antimicrobial pharmacodynamics.
Ambrose, PG; Grasela, D; Owens, RC, 2000
)
0.31
"93), Cmax (7."( Lack of interaction between levofloxacin and oxycodone: pharmacokinetics and drug disposition.
Fitzgerald, JF; Grant, EM; Nicolau, DP; Nightingale, C; Quintiliani, R; Zhong, M, 2001
)
0.6
"An in vitro pharmacokinetic model was used to compare the pharmacodynamics of moxifloxacin and levofloxacin against 3 Staphylococcus aureus and 3 Staphylococcus epidermidis strains."( Pharmacodynamics of moxifloxacin and levofloxacin against Staphylococcus aureus and Staphylococcus epidermidis in an in vitro pharmacodynamic model.
Lister, PD, 2001
)
0.8
"Pharmacokinetic characteristics and pharmacodynamic properties dictate antimicrobial response and, along with natural immune responses, clinical outcomes."( What have we learned from pharmacokinetic and pharmacodynamic theories?
Gilliland, KK; Paladino, JA; Schentag, JJ, 2001
)
0.31
" The elimination half-life in plasma and CSF was calculated using non-linear regression analysis."( Cerebrospinal fluid penetration and pharmacokinetics of levofloxacin in an experimental rabbit meningitis model.
Dash, AK; Destache, CJ; Larsen, C; Owens, H; Pakiz, CB, 2001
)
0.55
"An in vitro pharmacokinetic model (IVPM) was used to simulate the human serum pharmacokinetics of moxifloxacin, levofloxacin and sparfloxacin, and to compare their pharmacodynamics against Streptococcus pneumoniae exhibiting a wide range of susceptibilities to fluoroquinolones."( Pharmacodynamics of moxifloxacin, levofloxacin and sparfloxacin against Streptococcus pneumoniae.
Lister, PD; Sanders, CC, 2001
)
0.79
"This investigation explored pharmacodynamic characteristics of fluoroquinolones against Bacteroides thetaiotamicron and the potential for development of resistance."( Fluoroquinolone resistance in anaerobic bacteria following exposure to levofloxacin, trovafloxacin, and sparfloxacin in an in vitro pharmacodynamic model.
Hovde, LB; Peterson, ML; Ross, GH; Rotschafer, JC; Wright, DH, 2001
)
0.54
" However, pharmacokinetic data on oral perioperative prophylaxis in patients with preoperative surgical and anesthesiological preparation are not available."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.55
" Antibiotic concentrations were measured perioperatively and pharmacokinetic data calculated."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.55
" Pharmacokinetic data were not influenced by preoperative surgical or anesthesiological preparation."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.55
" Pharmacokinetic data confirm that oral ofloxacin may be used effectively as single-dose perioperative antibiotic prophylaxis."( Pharmacokinetic basis for oral perioperative prophylaxis with ofloxacin in general surgery.
Beger, HG; Ebeling, P; Isenmann, R; Schwarz, M; Thomsen, J; Weikert, E, 2001
)
0.82
"An in vitro pharmacodynamic investigation was conducted to explore whether the area under the concentration time curve from 0 to 24 h (AUC(0-24))/MIC ratio could predict fluoroquinolone performance against Bacteroides fragilis."( Pharmacodynamics of trovafloxacin and levofloxacin against Bacteroides fragilis in an in vitro pharmacodynamic model.
Brown, GH; Hoang, AD; Hovde, LB; Peterson, ML; Rotschafer, JC; Wright, DH, 2002
)
0.58
"In vitro and in vivo models of infection suggest that the area under the concentration-time curve (AUC): minimum inhibitory concentration (MIC) ratio is the pharmacodynamic parameter that is most predictive of bactericidal activity for the fluoroquinolones."( Pharmacodynamic profiling of levofloxacin and gatifloxacin using Monte Carlo simulation for community-acquired isolates of Streptococcus pneumoniae.
Ambrose, PG; Nicolau, DP, 2001
)
0.59
" All data were comodeled in a population pharmacokinetic analysis employing BigNPEM."( Levofloxacin penetration into epithelial lining fluid as determined by population pharmacokinetic modeling and monte carlo simulation.
Danziger, LH; Drusano, GL; Gotfried, MH; Preston, SL; Rodvold, KA, 2002
)
0.94
"Nonrandomized pharmacokinetic evaluation."( Pharmacokinetics of levofloxacin during continuous venovenous hemodiafiltration and continuous venovenous hemofiltration in critically ill patients.
Boos, C; Bruch, HP; Guenter, SG; Iven, H; Muhl, E, 2002
)
0.63
" Elimination half-life was 28."( Pharmacokinetics of levofloxacin during continuous venovenous hemodiafiltration and continuous venovenous hemofiltration in critically ill patients.
Boos, C; Bruch, HP; Guenter, SG; Iven, H; Muhl, E, 2002
)
0.63
"Results of this study suggest that an important pharmacokinetic interaction between levofloxacin and digoxin is unlikely to occur when administered concomitantly."( Absence of a pharmacokinetic interaction between digoxin and levofloxacin.
Chien, SC; Chow, AT; Natarajan, J; Rogge, MC; Williams, RR; Wong, F, 2002
)
0.78
"The main pharmacokinetic parameters af ter the first dosing were as follows: Cmax was (2."( Pharmacokinetics of multiple intravenous instillation of levofloxacin in Chinese healthy subjects.
Li, JT; Li, MN; Li, TY; Liu, Y; Lu, Y; Zhang, JW; Zhang, L; Zhang, YL, 2002
)
0.56
" The pharmacokinetic parameters in blood and in cerebrospinal fluid could be described by one compartment open model."( [Determination of levofloxacin in plasma and cerebrospinal fluid with HPLC and its pharmacokinetics in patients undergoing neurosurgical operations].
Cai, H; Lei, J; Li, R; Luo, S; Zhang, R, 1998
)
0.62
"To determine the population pharmacokinetic (PK) parameters of ofloxacin following multiple oral doses."( Ofloxacin population pharmacokinetics in patients with tuberculosis.
Ashkin, D; Berning, SE; Bulpitt, AE; Hollender, ES; Narita, M; Peloquin, CA; Stambaugh, JJ, 2002
)
2
" Higher daily doses were well tolerated, and appeared to maximize the peak concentration to minimal inhibitory concentration ratio (Cmax:MIC)."( Ofloxacin population pharmacokinetics in patients with tuberculosis.
Ashkin, D; Berning, SE; Bulpitt, AE; Hollender, ES; Narita, M; Peloquin, CA; Stambaugh, JJ, 2002
)
1.76
" Higher daily doses may offer pharmacodynamic advantages for the treatment of TB."( Ofloxacin population pharmacokinetics in patients with tuberculosis.
Ashkin, D; Berning, SE; Bulpitt, AE; Hollender, ES; Narita, M; Peloquin, CA; Stambaugh, JJ, 2002
)
1.76
"The aim of this study was to develop a rapid and sensitive method for the simultaneous determination of unbound levofloxacin in rat blood and bile using high-performance liquid chromatography coupled with microdialysis for further pharmacokinetic study."( Pharmacokinetic study of levofloxacin in rat blood and bile by microdialysis and high-performance liquid chromatography.
Chen, YF; Cheng, FC; Hung, LC; Tsai, TH; Tsai, TR, 2002
)
0.82
" In order to understand this difference in Vd(ss), first the contribution of each tissue to the Vd(ss) using pharmacokinetic parameters was estimated and it was found that the type of tissue contributing the most was muscle."( Determinant of the distribution volume at steady state for novel quinolone pazufloxacin in rats.
Hayakawa, H; Kawamura, Y; Takagi, K; Takano, YF; Tsuji, A, 2002
)
0.31
"An in vitro pharmacokinetic model (IVPM) was used to evaluate the pharmacodynamics of the 750 mg and 500 mg doses of levofloxacin against 4 ciprofloxacin-nonsusceptible Streptococcus pneumoniae."( Pharmacodynamics of 750 mg and 500 mg doses of levofloxacin against ciprofloxacin-resistant strains of Streptococcus pneumoniae.
Lister, PD, 2002
)
0.78
"To characterize the pharmacokinetic disposition of intravenous and oral levofloxacin in critically ill adults."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.81
" Pharmacokinetic evaluations were performed in 28 patients receiving intravenous levofloxacin."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.8
"05) from those observed after intravenous dosing in the same patients; other pharmacokinetic parameters were similar."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.58
" We present detailed pharmacokinetic (PK) data for amikacin (AMK), ethambutol (EMB), INH, pyrazinamide (PZA), RIF, and levofloxacin in four female bongos."( Population pharmacokinetics of antituberculous drugs and treatment of Mycobacterium bovis infection in bongo antelope (Tragelaphus eurycerus isaaci).
Aguilar, R; Auclair, B; Maslow, JN; Mikota, SK; Peloquin, CA, 2002
)
0.52
"To evaluate the pharmacokinetic profile of ofloxacin in healthy volunteers after single oral doses of 600 and 800 mg."( Dose related pharmacokinetics of ofloxacin in healthy volunteers.
Gurumurthy, P; Hemanthkumar, AK; Immanuel, C; Venkatesan, P, 2002
)
0.86
"Dose proportionality was observed in Cmax and AUC0-24 when 600 and 800 mg doses of ofloxacin were given."( Dose related pharmacokinetics of ofloxacin in healthy volunteers.
Gurumurthy, P; Hemanthkumar, AK; Immanuel, C; Venkatesan, P, 2002
)
0.82
" Levofloxacin plasma concentrations were analysed by means of HPLC and pharmacokinetic parameters were estimated using the WinNonlin pharmacokinetic software package."( Pharmacokinetic aspects of levofloxacin 500 mg once daily during sequential intravenous/oral therapy in patients with lower respiratory tract infections.
Brollo, L; Di Qual, E; Dolcet, F; Furlanut, M; Lugatti, E; Pea, F; Talmassons, G, 2003
)
1.17
"Antibacterial effect and emergence of resistance to gemifloxacin and levofloxacin were studied in an in vitro pharmacokinetic model of infection."( Mechanism of fluoroquinolone resistance is an important factor in determining the antimicrobial effect of gemifloxacin against Streptococcus pneumoniae in an in vitro pharmacokinetic model.
Bowker, KE; MacGowan, AP, 2003
)
0.55
"42 mL/min/kg]), leading to a shorter elimination half-life (5."( Pharmacokinetics and pharmacodynamics of intravenous levofloxacin in patients with early-onset ventilator-associated pneumonia.
Baldassarre, M; Brollo, L; Cusenza, A; Di Qual, E; Furlanut, M; Pea, F, 2003
)
0.57
"The differential effects of moxifloxacin and levofloxacin on the development of resistance in four Streptococcus pneumoniae isolates were examined by using an in vitro pharmacodynamic model."( Activities of mutant prevention concentration-targeted moxifloxacin and levofloxacin against Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Allen, GP; Kaatz, GW; Rybak, MJ, 2003
)
0.8
" Pharmacokinetic data on ofloxacin in critically ill patients on renal replacement therapy are sparse and conflicting."( Single-dose pharmacokinetics of ofloxacin during continuous venovenous hemofiltration in critical care patients.
El Menyawi, I; Fuhrmann, V; Mittermayer, C; Ratheiser, K; Schenk, P; Thalhammer, F, 2003
)
0.91
" Differential equations describing a 2-compartment open-infusion pharmacokinetic model were fit to each individual subject's serum concentration-time data by iterative nonlinear weighted least-squares regression analysis using Adapt II (Biomedical Simulations Resource, University of Southern California, Los Angeles, CA)."( Levofloxacin pharmacokinetics in ESRD and removal by the cellulose acetate high performance-210 hemodialyzer.
Hamburger, RJ; Kays, MB; Lucksiri, A; Mueller, BA; Scott, MK; Sowinski, KM, 2003
)
0.94
"During the last decade some studies have shown that the area under the curve (AUC)/MIC ratio is the pharmacodynamic index that best predicts the efficacies of quinolones, while other studies suggest that the predictive value of the peak concentration/MIC (peak/MIC) ratio is superior to the AUC/MIC ratio in explaining clinical and microbiological outcomes."( Pharmacodynamics of levofloxacin and ciprofloxacin in a murine pneumonia model: peak concentration/MIC versus area under the curve/MIC ratios.
Fraschini, F; Mattina, R; Mouton, JW; Scaglione, F, 2003
)
0.63
"Following the optimization of diamine-containing efflux pump inhibitors with respect to in vitro potentiation activity, in vivo stability and acute toxicity, we addressed the question of how to control the pharmacokinetic properties of the series."( The relationship between physicochemical properties, in vitro activity and pharmacokinetic profiles of analogues of diamine-containing efflux pump inhibitors.
Chamberland, S; Dudley, MN; Griffith, D; Huie, K; Landaverry, Y; Léger, R; Litman, R; Madsen, D; Renau, TE; Tembe, V; Watkins, WJ; Williams, N; Yen, R; Zhang, JZ, 2003
)
0.32
" We therefore compared the in vitro pharmacodynamic activity of ABT-492 to that of levofloxacin, an antibiotic commonly used for the treatment of pneumonia, through MIC determination and time-kill kinetic analysis."( In vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.
Danziger, LH; Gunderson, SM; Hayes, RA; Quinn, JP, 2004
)
0.77
"To compare the pharmacodynamic profiles of linezolid, levofloxacin, and vancomycin against clinical strains of Streptococcus pneumoniae, including vancomycin-tolerant and fluoroquinolone-resistant isolates."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.92
"In vitro pharmacodynamic model."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.68
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.9
" Pharmacokinetic parameters of levofloxacin, including the maximum serum concentration (C(max)), time to C(max) (T(max)), area under the concentration-time curve (AUC), volume of distribution at steady state (V(ss)/F) and clearance (CL/F) were not statistically different at first dose and during neutropenia."( Pharmacokinetics and effects on bowel and throat microflora of oral levofloxacin as antibacterial prophylaxis in neutropenic patients with haematological malignancies.
Dijstelbloem, Y; Huijgens, PC; Simoons-Smit, AM; Timmers, GJ; Touw, DJ; van Winkelhoff, AJ; Vandenbroucke-Grauls, CM, 2004
)
0.84
" Considering the major pharmacodynamic determinants for the concentration-dependent bactericidal activity of levofloxacin as applicable at the urinary level (CU/MIC of >12."( Urinary pharmacokinetics and theoretical pharmacodynamics of intravenous levofloxacin in intensive care unit patients treated with 500 mg b.i.d. for ventilator-associated pneumonia.
Baldassarre, M; Brollo, L; Di Qual, E; Furlanut, M; Nascimben, E; Pavan, F; Pea, F, 2003
)
0.76
" The pharmacokinetic parameters were determined by non-compartmental model and plasma protein binding was estimated by equilibrium dialysis technique."( Pharmacokinetics, tissue residue and plasma protein binding of ofloxacin in goats.
Baruah, H; Khonikor, HN; Roy, DC; Roy, RK, 2004
)
0.56
"Fluoroquinolones present various pharmacokinetic properties."( [Pharmacokinetics and dose adaptation of ofloxacine, pefloxacine and ciprofloxacine during haemodialysis and continuous ambulatory peritoneal dialysis].
Christmann, D; Daniel, JP; Moulin, B, 2004
)
0.59
" The pharmacokinetic profiles also reflected the effectiveness of GFLX."( Pharmacodynamics and bactericidal activity of gatifloxacin in experimental pneumonia caused by penicillin-resistant Streptococcus pneumoniae.
Fukuda, Y; Hirakata, Y; Kadota, J; Kohno, S; Miyazaki, Y; Murata, I; Tashiro, T; Tomono, K; Tsukamoto, K; Yanagihara, K, 2004
)
0.32
"We designed a 4-way crossover, ex-vivo pharmacodynamic study to compare the bactericidal rate of amoxicillin/sulbactam (AMX-SUL), azithromycin (AZM), doxycycline (DOX) and levofloxacin (LVX) against Streptococcus pneumoniae ATCC 49619."( An ex-vivo pharmacodynamic study comparing bactericidal activity of amoxicillin/sulbactam, azithromycin, doxycycline and levofloxacin against Streptococcus pneumoniae.
Arenoso, H; Bantar, C; Caruso, N; Fernández Canigia, L; Nicola, F; Soutric, J, 2004
)
0.72
" This work aimed at assessing the pharmacodynamic target attainment against Streptococcus pneumoniae using levofloxacin 500 mg, 750 mg and 1000 mg administered once daily in plasma (P) and epithelial lining fluid (ELF) of hospitalized patients with community acquired pneumonia."( Pharmacodynamic target attainment analysis against Streptococcus pneumoniae using levofloxacin 500 mg, 750 mg and 1000 mg once daily in plasma (P) and epithelial lining fluid (ELF) of hospitalized patients with community acquired pneumonia (CAP).
Chan, CK; Hoban, DJ; Marras, TK; Noreddin, AM; Sanders, K; Zhanel, GG, 2004
)
0.76
" The pharmacokinetic, safety, and pharmacodynamic data from our study suggest that a once-daily regimen of intravenous levofloxacin at 750 mg and metronidazole at 1,500 mg warrants further clinical investigation."( Pharmacokinetics and pharmacodynamics of intravenous levofloxacin at 750 milligrams and various doses of metronidazole in healthy adult subjects.
Danziger, LH; Gotfried, MH; Graham, MB; Hackett, S; Pendland, SL; Quinn, JP; Rodvold, KA; Schriever, CA; Sprandel, KA, 2004
)
0.78
" Monte Carlo simulation was used to construct pharmacodynamic models for imipenem, meropenem, ertapenem, levofloxacin, gatifloxacin, and ciprofloxacin."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.54
" In the pharmacodynamic models, imipenem and meropenem had an equal likelihood of achieving a free T>MIC > or =40% against bacteria that produced ESBLs (> or =97%) and bacteria that did not produce ESBLs (> or =98%)."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.32
" Pharmacodynamic modeling based on local ESBL-producing isolates and pharmacokinetic data from healthy humans indicated that imipenem and meropenem may have a greater likelihood of achieving pharmacodynamic targets against bacteria that produce ESBLs than ertapenem or fluoroquinolones."( Pharmacodynamic modeling of carbapenems and fluoroquinolones against bacteria that produce extended-spectrum beta-lactamases.
Burgess, DS; Frei, CR; Moczygemba, LR, 2004
)
0.32
"An intensive care unit and a clinical pharmacokinetic laboratory in two university hospitals."( Pharmacokinetics and intrapulmonary diffusion of levofloxacin in critically ill patients with severe community-acquired pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC, 2005
)
0.58
"Our results suggest that in critically ill patients who are receiving mechanical ventilation and have severe community-acquired pneumonia and creatinine clearance of >40 mL/min, the administration of 500 mg of intravenous levofloxacin once and twice daily allows for the exceeding of pharmacodynamic thresholds predictive of outcome (i."( Pharmacokinetics and intrapulmonary diffusion of levofloxacin in critically ill patients with severe community-acquired pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC, 2005
)
0.76
" To provide dosing guidance for children, 3 single-dose, multicenter pharmacokinetic studies were conducted in 85 children in 5 age groups: 6 months to <2 years, 2 to <5 years, 5 to <10 years, 10 to <12 years, and 12 to 16 years."( Levofloxacin pharmacokinetics in children.
Blumer, JL; Bocchini, JA; Bradley, JS; Chien, S; Kearns, GL; Maldonado, S; Natarajan, J; Noel, GJ; Wells, TG, 2005
)
0.95
"A prospective pharmacokinetic study was performed in Caucasian patients from an intensive care unit with respiratory support to evaluate the influence of this circumstance on the pharmacokinetic behaviour of levofloxacin."( Pharmacokinetics and pharmacodynamics of levofloxacin in intensive care patients.
Alvarez Lerma, F; Colino Gandarillas, CI; Domínguez-Gil, A; Menacho, YA; Sánchez Navarro, A, 2005
)
0.78
" The experimental data on plasma concentrations were analysed by independent-modelling techniques to estimate the following pharmacokinetic parameters: area under the plasma concentration-time curve (AUC), volume of distribution at steady state (V(ss)), plasma clearance (CL), maximum plasma concentration at steady state (C(max)(,)(ss)) and elimination half-life (t((1/2))(beta))."( Pharmacokinetics and pharmacodynamics of levofloxacin in intensive care patients.
Alvarez Lerma, F; Colino Gandarillas, CI; Domínguez-Gil, A; Menacho, YA; Sánchez Navarro, A, 2005
)
0.59
" Since the group of patients included in the study was small and also included obese individuals, it is difficult to estimate with precision the contribution of each circumstance (overweight or illness severity) to the pharmacokinetic behaviour of levofloxacin."( Pharmacokinetics and pharmacodynamics of levofloxacin in intensive care patients.
Alvarez Lerma, F; Colino Gandarillas, CI; Domínguez-Gil, A; Menacho, YA; Sánchez Navarro, A, 2005
)
0.77
"Previously, we demonstrated the importance of low-level-resistant variants to the evolution of resistance in Staphylococcus aureus exposed to ciprofloxacin in an in vitro system and developed a pharmacodynamic model which predicted the emergence of resistance."( Pharmacodynamic modeling of the evolution of levofloxacin resistance in Staphylococcus aureus.
Campion, JJ; Chung, P; Evans, ME; McNamara, PJ; Titlow, WB, 2005
)
0.78
" Previously described population pharmacokinetic models of gatifloxacin and levofloxacin administration in patients with serious CAP were utilised to simulate gatifloxacin and levofloxacin pharmacokinetics."( Comparison of gatifloxacin and levofloxacin administered at various dosing regimens to hospitalised patients with community-acquired pneumonia: pharmacodynamic target attainment study using North American surveillance data for Streptococcus pneumoniae.
Hoban, DJ; Noreddin, AM; Zhanel, GG, 2005
)
0.84
"The pharmacokinetic properties of the fluoroquinolone levofloxacin, were investigated in five cats after single intravenous and repeat oral administration at a daily dose of 10 mg/kg."( Pharmacokinetics of levofloxacin after single intravenous and repeat oral administration to cats.
Albarellos, GA; Ambros, LA; Landoni, MF, 2005
)
0.88
" Risk analysis software was used to simulate 10,000 patients by integrating published pharmacokinetic parameters, their variability, and minimum inhibitory concentration (MIC) distributions from the TSN database."( Pharmacodynamic analysis of ceftriaxone, gatifloxacin,and levofloxacin against Streptococcus pneumoniae with the use of Monte Carlo simulation.
Burgess, DS; Frei, CR, 2005
)
0.57
"Ceftriaxone maintained high probability of target attainment over a broad range of pharmacodynamic targets regardless of penicillin susceptibility (%T > MIC 0-60%)."( Pharmacodynamic analysis of ceftriaxone, gatifloxacin,and levofloxacin against Streptococcus pneumoniae with the use of Monte Carlo simulation.
Burgess, DS; Frei, CR, 2005
)
0.57
" When ofloxacin was administered intravenously, C(max) and the distribution half-life increased significantly in comparison with normal group, whereas the distribution rate constants, the apparent volume of distribution decreased."( Effects of hepatic fibrosis on ofloxacin pharmacokinetics in rats.
Chen, M; Hu, XL; Liao, ZX; Wang, H, 2006
)
1.1
"Prospective, open-label, parallel group pharmacokinetic study."( Pharmacokinetics of intravenously administered levofloxacin in men and women.
Goldman, M; Kays, MB; Lagvankar, S; Mueller, BA; Overholser, BR; Sowinski, KM, 2005
)
0.58
" Pharmacokinetic analysis was performed with ADAPT II software (University of Southern California, Los Angeles, CA)."( Pharmacokinetics of intravenously administered levofloxacin in men and women.
Goldman, M; Kays, MB; Lagvankar, S; Mueller, BA; Overholser, BR; Sowinski, KM, 2005
)
0.58
"Levofloxacin is a fluoroquinolone antimicrobial agent for which pharmacodynamic relationships between the maximum serum antibiotic concentration (Cmax)/minimum inhibitory concentration (MIC) ratio and/or the area under the serum concentration-time curve during a 24-h dosing period (AUC(0-24))/MIC ratio and clinical and/or microbiological outcomes have been developed."( Pharmacodynamics of levofloxacin in patients with acute exacerbation of chronic bronchitis.
Blasi, F; Cazzola, M; Donnarumma, G; Marchetti, F; Matera, MG; Sanduzzi, A; Tufano, MA, 2005
)
1.26
"The mean peak concentration in serum (6."( Pharmacodynamics of levofloxacin in patients with acute exacerbation of chronic bronchitis.
Blasi, F; Cazzola, M; Donnarumma, G; Marchetti, F; Matera, MG; Sanduzzi, A; Tufano, MA, 2005
)
0.64
" The aim of this study was to compare concentrations in plasma, urinary excretion (UE) and pharmacokinetic parameters of ciprofloxacin XR (1000 mg) versus those of levofloxacin (500 mg) in healthy volunteers receiving a single oral dose."( Pharmacokinetics of ciprofloxacin XR (1000 mg) versus levofloxacin (500 mg) in plasma and urine of male and female healthy volunteers receiving a single oral dose.
Dalhoff, A; Kinzig-Schippers, M; Naber, KG; Sörgel, F; Tischmeyer, U; Wagenlehner, C; Wagenlehner, FM, 2006
)
0.85
" It is based on the application of pharmacokinetic and pharmacodynamic criteria (PK/PD analysis) to optimize dosification of this type of drug."( [Pharmacokinetic/pharmacodynamic analysis to optimize antibacterial treatments: prediction of efficacy by using Montecarlo simulation techniques].
Sánchez Navarro, A, 2005
)
0.33
" The purpose of this study was to determine whether three widely used fluoroquinolone antibiotics (ciprofloxacin, ofloxacin, and norfloxacin) are substrates of Bcrp1/BCRP and to investigate the possible role of this transporter in the in vivo pharmacokinetic profile of these compounds and their secretion into the milk."( Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretion.
Alvarez, AI; Merino, G; Molina, AJ; Prieto, JG; Pulido, MM; Schinkel, AH, 2006
)
0.55
"There was no significant interaction in healthy volunteers, however, when cystic fibrosis patients were given levofloxacin with 2-h spaced calcium, the maximum plasma concentration (Cmax) decreased by 19% and time to Cmax increased by 37% (p<0."( Altered steady state pharmacokinetics of levofloxacin in adult cystic fibrosis patients receiving calcium carbonate.
Allen, SE; Amsden, GW; Pai, MP, 2006
)
0.81
"Levofloxacin significantly increased the mean area under the blood concentration-time curve (AUC) and the other pharmacokinetic parameters of ciclosporin and tacrolimus by about 25%."( Pharmacokinetic interaction between levofloxacin and ciclosporin or tacrolimus in kidney transplant recipients: ciclosporin, tacrolimus and levofloxacin in renal transplantation.
Basile, V; Capone, D; Carrano, R; Federico, S; Gentile, A; Palmiero, G, 2006
)
1.22
" These data demonstrate that not all fluoroquinolones share the same pharmacodynamic targets needed to maximize their antibacterial effect."( Pharmacodynamics of moxifloxacin and levofloxacin simulating human serum and lung concentrations.
Dalhoff, A; Schubert, S; Stass, H; Ullmann, U, 2005
)
0.6
" The method was successfully applied to an in vitro pharmacokinetic study and patient samples as well."( Validation of a levofloxacin HPLC assay in plasma and dialysate for pharmacokinetic studies.
Siewert, S, 2006
)
0.66
" These experimental data, which had not been changed by any mathematical operation, were collected and used to determine the effect of sex on the pharmacokinetic profile using parametric and non-parametric tests as well as multivariate classification tools like cluster analysis (CA) and principal component analysis (PCA)."( Influence of sex on the pharmacokinetics of ciprofloxacin and ofloxacin.
Chmielewska, A; Konieczna, L; Lamparczyk, H, 2006
)
0.59
" Recent studies with a 103-compound dataset suggested that scaling from monkey pharmacokinetic data tended to be the most accurate method for predicting human clearance."( Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
Evans, CA; Jolivette, LJ; Nagilla, R; Ward, KW, 2006
)
0.33
" In these strains, levofloxacin ED(50)s were 2- to 10-fold lower than the ED(50)/MIC ratios in the other strains and 90% E(max) AUC/MIC ratios were 2- to 4-fold lower than those predicted from pharmacodynamic modeling of efficacy against other strains."( Pharmacodynamics of levofloxacin against Pseudomonas aeruginosa with reduced susceptibility due to different efflux pumps: do elevated MICs always predict reduced in vivo efficacy?
Cho, D; Corcoran, E; Dudley, MN; Griffith, DC; Lee, A; Lofland, D; Lomovskaya, O, 2006
)
0.96
" The pharmacodynamic probability of target attainment (PTA) was evaluated by Monte Carlo simulation."( Levofloxacin pharmacokinetics and pharmacodynamics in patients with severe burn injury.
Bauling, PC; Fish, DN; Hoody, DW; Kiser, TH; Obritsch, MD; Wegzyn, CO, 2006
)
0.96
" A pharmacokinetic computerized device was used to simulate serum and epithelial lining fluid (ELF) concentrations."( A pharmacodynamic approach to antimicrobial activity in serum and epithelial lining fluid against in vivo-selected Streptococcus pneumoniae mutants and association with clinical failure in pneumonia.
Aguilar, L; Alou, L; Cafini, F; Echeverría, O; Giménez, MJ; Pérez-Trallero, E; Prieto, J; Sevillano, D, 2006
)
0.33
"The objective of this study was to determine the plasma and intrapulmonary pharmacokinetic parameters of intravenously administered levofloxacin in healthy volunteers."( Intrapulmonary pharmacokinetics and pharmacodynamics of high-dose levofloxacin in healthy volunteer subjects.
Conte, JE; Golden, JA; McIver, M; Zurlinden, E, 2006
)
0.77
"An in vitro pharmacodynamic model was used to simulate the epithelial lining fluid (ELF) concentrations following oral administration of levofloxacin 500 mg once daily and moxifloxacin 400 mg once daily in older adults."( Evaluation of bacterial kill when modelling the bronchopulmonary pharmacokinetic profile of moxifloxacin and levofloxacin against parC-containing isolates of Streptococcus pneumoniae.
Deryke, CA; Du, X; Nicolau, DP, 2006
)
0.75
"A correlation was seen between both the area under the serum concentration curve and MIC (AUC/MIC) and the peak concentration/MIC (Cmax/MIC) versus area under the bactericidal killing curve (AUBKC) or Deltalog0-24 cfu/mL."( Pharmacodynamics of moxifloxacin and levofloxacin against Streptococcus pneumoniae, Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli: simulation of human plasma concentrations after intravenous dosage in an in vitro kinetic model.
Cars, O; Odenholt, I, 2006
)
0.6
"Members of the fluoroquinolone class are being actively evaluated for inclusion in tuberculosis chemotherapy regimens, and we sought to determine the best in vitro and pharmacodynamic predictors of in vivo efficacy in mice."( Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
Balasubramanian, V; Bharath, S; Gaonkar, S; Jayaram, R; Jayashree, R; Kaur, P; Mahesh, BN; Nandi, V; Shandil, RK; Suresh, BL, 2007
)
0.7
" This study demonstrates the intracellular and extracellular killing activity of antimycobacterial drugs in a pharmacokinetic intracellular in vitro model."( Evaluation of an intracellular pharmacokinetic in vitro infection model as a tool to assess tuberculosis therapy.
Cappelletty, DM, 2007
)
0.34
" We studied the preliminary pharmacokinetic and pharmacodynamic (PK/PD) relationship of levofloxacin in CF."( Levofloxacin pharmacokinetics in adult cystic fibrosis.
Boyle, MP; Brass-Ernst, L; Diener-West, M; Lee, CKK; Noschese, M; Zeitlin, PL, 2007
)
1.18
"The objective of this study was to investigate the relationship between pharmacokinetic and pharmacodynamic parameters, on the basis of the mutant prevention concentration (MPC) concept, and the emergence of resistant mutants of Streptococcus pneumoniae to fluoroquinolone antibacterials."( Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
Homma, T; Hori, T; Sugimori, G; Yamano, Y, 2007
)
0.34
" In addition to standard pharmacokinetic parameters, the total dialysate concentration of both drugs was measured using a technically simple single-pass batch dialysis system for EDD."( Pharmacokinetics of moxifloxacin and levofloxacin in intensive care unit patients who have acute renal failure and undergo extended daily dialysis.
Czock, D; de Groot, K; Fliser, D; Hafer, C; Haller, H; Hüsig-Linde, C; Keller, F; Kielstein, JT; Kuse, E; Langhoff, A; Schöpke, T; Swoboda, S, 2006
)
0.6
"The objective of this study was to determine the plasma and intrapulmonary pharmacokinetic parameters of intravenously administered levofloxacin in subjects with stable chronic lung disease."( Intrapulmonary pharmacodynamics of high-dose levofloxacin in subjects with chronic bronchitis or chronic obstructive pulmonary disease.
Conte, JE; Golden, JA; Little, E; McIver, M; Zurlinden, E, 2007
)
0.8
" Pharmacokinetic studies of each agent were identified by separate MEDLINE searches combining the MeSH heading pharmacokinetics with the generic name of the antimicrobial."( Simulated comparison of the pharmacodynamics of ciprofloxacin and levofloxacin against Pseudomonas aeruginosa using pharmacokinetic data from healthy volunteers and 2002 minimum inhibitory concentration data.
Burgess, DS; Hall, RG, 2007
)
0.59
"To characterize the membrane transport responsible for the renal excretion and intestinal absorption of levofloxacin, we performed pharmacokinetic analysis of transcellular transport across LLC-PK(1) and Caco-2 cell monolayers."( Pharmacokinetic analysis of transcellular transport of levofloxacin across LLC-PK1 and Caco-2 cell monolayers.
Hashimoto, Y; Ishida, K; Suzuki, H; Tahara, K; Takaai, M, 2007
)
0.8
"The objective of this study was to determine the population pharmacokinetic parameters of levofloxacin, gatifloxacin, and moxifloxacin following multiple oral doses."( Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
Boom, WH; Dietze, R; Hadad, DJ; Johnson, JL; Molino, LP; Palaci, M; Peloquin, CA, 2008
)
0.84
" The mean pharmacokinetic parameters for the first dose were: maximum serum concentration (C(max)) 12."( Pharmacokinetics/pharmacodynamics of levofloxacin 750 mg once daily in young women with acute uncomplicated pyelonephritis.
Bryski, L; Duckworth, H; Harding, G; Nicolle, L; Sitar, D; Zhanel, G, 2008
)
0.61
" azithromycin once daily pharmacodynamic simulation was performed against 10(8) cfu/ml of four Streptococcus pneumoniae strains (exhibiting higher amoxicillin than penicillin MIC) and four Haemophilus influenzae strains: beta-lactamase producing, BLNAR (beta-lactamase-negative ampicillin-resistant) and BLPACR (beta-lactamase-positive amoxicillin/clavulanate-resistant)."( Levofloxacin vs. azithromycin pharmacodynamic activity against S. pneumoniae and H. influenzae with decreased susceptibility to amoxicillin/clavulanic acid.
Aguilar, L; Alou, L; Echeverría, O; Giménez, MJ; González, N; Martín, JE; Prieto, J; Sevillano, D; Torrico, M; Valdés, L, 2007
)
0.96
" The purpose of the present study was to evaluate the pharmacokinetic characteristics of a single oral dose of antofloxacin hydrochloride in Chinese healthy male volunteers."( Pharmacokinetics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, after single oral dose administration in Chinese healthy male volunteers.
Kang, Z; Li, T; Liu, Y; Lu, Y; Xiao, Y; Zhang, M, 2008
)
0.87
" Because the predicted Cmax value is similar to that of western countries, the frequency of adverse effects is thought to be same as in western countries."( Population pharmacokinetics of levofloxacin as prophylaxis for febrile neutropenia.
Fujimoto, Y; Kanbayashi, Y; Matsumoto, Y; Morimoto, Y; Nomura, K; Taniwaki, M, 2008
)
0.63
"A pharmacodynamic model was used to generate supportive data comparing tigecycline with other broad-spectrum agents against pathogens implicated in hospital-acquired pneumonia (HAP)."( A pharmacodynamic simulation to assess tigecycline efficacy for hospital-acquired pneumonia compared with other common intravenous antibiotics.
Dowzicky, M; Kuti, JL; Nicolau, DP, 2008
)
0.35
" Pharmacokinetic parameters were estimated."( The pharmacokinetics of antofloxacin in renally impaired rats.
Liu, L; Liu, XD; Pang, XY; Wang, GJ; Xie, L; Zhang, DM, 2008
)
0.64
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"Therapeutic activity, pharmacokinetic and bioavailability on animals (inbred white mouse, rabbits) were evaluated for Ofloxacin-PhPO and Pefloxacin-genova in comparison with innovator products--Tarivid and Abaktal."( [Chemotherapy activity and pharmacokinetics of the fluoroquinolones generics Ofloxacin-PhPO and Pefloxacin-genova].
Bobrov, VI; Borisov, MM; Ptitsina, SN, 2007
)
0.78
" We present some pharmacokinetic and pharmacological properties of the L-Asp hexapeptide-tagged drugs and enzyme."( Targeted drug delivery to bone: pharmacokinetic and pharmacological properties of acidic oligopeptide-tagged drugs.
Kobayashi, S; Miyamoto, K; Nomura, M; Takahashi-Nishioka, T; Tomatsu, S; Yokogawa, K, 2008
)
0.35
" The developed assay method was applied to a pharmacokinetic study in human volunteers following oral administration of 400 mg GFC tablet."( Development and validation of a HPLC method for simultaneous quantitation of gatifloxacin, sparfloxacin and moxifloxacin using levofloxacin as internal standard in human plasma: application to a clinical pharmacokinetic study.
Mullangi, R; Narasu, L; Shankar, BP; Srinivas, N, 2008
)
0.55
" Using the neutropenic murine thigh infection model, we defined the pharmacodynamic profile and property of antofloxacin hydrochloride against Staphylococcus aureus."( Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.
Xiao, XM; Xiao, YH, 2008
)
0.83
"Single-dose pharmacokinetic studies of antofloxacin hydrochloride were carried out in thigh infected mice."( Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.
Xiao, XM; Xiao, YH, 2008
)
0.88
"The PK was linear with similar elimination half-life over the dose range studied."( Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.
Xiao, XM; Xiao, YH, 2008
)
0.61
"In a previous study, levofloxacin 750 mg eradicated 4 ciprofloxacin-resistant isolates of Streptococcus pneumoniae from an in vitro pharmacodynamic model (IVPM)."( Pharmacodynamics of levofloxacin against characterized ciprofloxacin-resistant Streptococcus pneumoniae.
Lister, PD, 2008
)
0.96
" Ciprofloxacin, a carboxyfluoroquinolone, was previously observed to demonstrate the pharmacodynamic interactions with antifungal agents by altering their growth inhibitory activity against Candida albicans and Aspergillus fumigatus."( Comparative pharmacodynamic interaction analysis between ciprofloxacin, moxifloxacin and levofloxacin and antifungal agents against Candida albicans and Aspergillus fumigatus.
Meletiadis, J; Papaioannidou, P; Roilides, E; Sein, T; Stergiopoulou, T; Tsiouris, I; Walsh, TJ, 2009
)
1.11
"The knowledge of the pharmacodynamic interactions between fluoroquinolones and antifungal agents may guide selection and potentially improve the outcome of immunosuppressed patients with concurrent bacterial and fungal infections."( Comparative pharmacodynamic interaction analysis between ciprofloxacin, moxifloxacin and levofloxacin and antifungal agents against Candida albicans and Aspergillus fumigatus.
Meletiadis, J; Papaioannidou, P; Roilides, E; Sein, T; Stergiopoulou, T; Tsiouris, I; Walsh, TJ, 2009
)
0.59
" This bio-analytical method was finally applied to the analysis of samples which have been obtained from patients, participating in a pharmacokinetic study on moxifloxacin."( Pharmacokinetics of fluoroquinolones in critical care patients: A bio-analytical HPLC method for the simultaneous quantification of ofloxacin, ciprofloxacin and moxifloxacin in human plasma.
Boussery, K; Colpaert, K; De Paepe, P; De Smet, J; De Sutter, P; Decruyenaere, J; Van Bocxlaer, J, 2009
)
0.56
" No significant difference in various pharmacokinetic parameters of plasma was observed in healthy calves ( β=0."( Pharmacokinetic studies of levofloxacin after oral administration in healthy and febrile cow calves.
Kumar, S; Kumar, V; Roy, BK; Singh, KK, 2009
)
0.64
"This study aimed to explore the pharmacokinetic features of levofloxacin (LVFX) in Chinese patients with infections and to confirm oral LVFX 500 mg once daily as an optimal treatment regimen based on pharmacokinetic-pharmacodynamic (PK-PD) analysis."( Population pharmacokinetics of oral levofloxacin 500 mg once-daily dosage in community-acquired lower respiratory tract infections: results of a prospective multicenter study in China.
Cao, GY; Huang, JA; Liu, YB; Shi, YG; Si, B; Sun, SH; Wu, XJ; Xia, QM; Xiao, ZK; Xu, JF; Zhang, J; Zhang, YY, 2009
)
0.86
"The pharmacodynamic targets representing 90% probability thresholds for bacterial eradication were determined in patients with complicated urinary tract infections (UTIs) treated with 500mg of levofloxacin every 24h for 7-14 days."( Microbiological outcome of complicated urinary tract infections treated with levofloxacin: a pharmacokinetic/pharmacodynamic analysis.
Arakawa, S; Deguchi, T; Matsumoto, T; Monden, K; Nakane, K; Shimizu, T; Yasuda, M, 2010
)
0.78
"The purpose of the study was to evaluate the pharmacokinetic characteristics of a single, intravenous dose of antofloxacin hydrochloride in healthy Chinese male volunteers."( Pharmacokinetics of antofloxacin hydrochloride, a novel fluoroquinolone, after single-dose intravenous administration in healthy Chinese male volunteers.
Kang, Z; Li, T; Liang, J; Liu, Y; Lu, Y; Wang, J; Xiao, Y; Zhang, M, 2010
)
0.88
" Different pharmacokinetic parameters for both drugs were determined using non-compartmental method."( Interaction study between levofloxacin and omeprazole using urinary pharmacokinetic data.
Azad, MA; Faruquee, CF; Hasnat, A; Parveen, S; Rayhan, I; Ullah, A, 2010
)
0.65
" The purpose of the study was to evaluate the pharmacokinetic characteristics of single and multiple oral doses of antofloxacin hydrochloride in Chinese healthy male volunteers."( Pharmacokinetic study of single and multiple oral dose administration of antofloxacin hydrochloride in healthy male volunteers.
Kang, ZS; Li, TY; Liu, Y; Lü, Y; Xiao, YH; Zhang, M; Zhu, Y, 2011
)
0.81
"The purpose of the study was to evaluate pharmacokinetic characteristics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, during a multiple, intravenous dosing regimen."( Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration.
Kang, Z; Li, T; Liang, J; Liu, Y; Lu, Y; Wang, J; Xiao, Y; Zhang, M, 2011
)
0.91
"To evaluate the pharmacokinetic interactions between theophylline and antofloxacin in vivo and in vitro."( Modulation of pharmacokinetics of theophylline by antofloxacin, a novel 8-amino-fluoroquinolone, in humans.
Cheng, JL; Fan, HW; Liu, HY; Liu, L; Liu, XD; Pan, X; Xiao, DW; Xie, L; Yang, HW, 2011
)
0.85
"Our objectives were to assess the pharmacokinetic interaction and body fluid penetration of ciprofloxacin and levofloxacin."( Population pharmacokinetics and penetration into prostatic, seminal, and vaginal fluid for ciprofloxacin, levofloxacin, and their combination.
Bulitta, JB; Kinzig, M; Landersdorfer, CB; Naber, CK; Naber, KG; Sauber, C; Sörgel, F; Wagenlehner, FM, 2011
)
0.81
" Serum, urine, and body fluid concentrations were determined by high-performance liquid chromatography and analyzed via population pharmacokinetic modeling."( Population pharmacokinetics and penetration into prostatic, seminal, and vaginal fluid for ciprofloxacin, levofloxacin, and their combination.
Bulitta, JB; Kinzig, M; Landersdorfer, CB; Naber, CK; Naber, KG; Sauber, C; Sörgel, F; Wagenlehner, FM, 2011
)
0.59
" This pharmacokinetic interaction was not clinically relevant."( Population pharmacokinetics and penetration into prostatic, seminal, and vaginal fluid for ciprofloxacin, levofloxacin, and their combination.
Bulitta, JB; Kinzig, M; Landersdorfer, CB; Naber, CK; Naber, KG; Sauber, C; Sörgel, F; Wagenlehner, FM, 2011
)
0.59
"Levofloxacin and cyclosporine show different pharmacokinetic properties, but are known to be dose proportional within the therapeutic range."( Assessment of pharmacokinetic proportionality of levofloxacin and cyclosporine over a 100-fold dose range in healthy human volunteers.
Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yu, KS, 2012
)
1.25
"In this study levofloxacin, which is completely absorbed and primarily eliminated renally without modification, showed better pharmacokinetic proportionality than cyclosporine, which is poorly absorbed and extensively metabolized."( Assessment of pharmacokinetic proportionality of levofloxacin and cyclosporine over a 100-fold dose range in healthy human volunteers.
Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yu, KS, 2012
)
0.97
"Despite the important role of fluoroquinolones and the predominant use of ofloxacin for treating multidrug-resistant tuberculosis in South Africa, there are limited data on ofloxacin pharmacokinetics in patients with multidrug-resistant tuberculosis, no ofloxacin pharmacokinetic data from South African patients, and no direct assessment of the relationship between ofloxacin pharmacokinetics and the MIC of ofloxacin of patient isolates."( Population pharmacokinetics and pharmacodynamics of ofloxacin in South African patients with multidrug-resistant tuberculosis.
Chigutsa, E; Harding, J; Kirkpatrick, CM; Mac Kenzie, WR; McIlleron, H; Meredith, S; Moodley, P; Padayatchi, N; Weiner, M; Wiesner, L, 2012
)
0.86
"The present study aimed to investigate the pharmacokinetic variation of ofloxacin based on gender-related difference in the expression of multidrug resistance-associated protein (Abcc2/Mrp2) in rat kidney."( Pharmacokinetic variation of ofloxacin based on gender-related difference in the expression of multidrug resistance-associated protein (Abcc2/Mrp2) in rat kidney.
Li, YQ; Wang, D; Wei, YH; Wu, XA; Zhang, F; Zhang, GQ; Zhang, JP; Zhou, Y, 2012
)
0.9
"We studied the pharmacokinetic and pharmacodynamic parameters of levofloxacin and rifampicin in bone and joint infections."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
0.88
" We then computed the 6 hours post dose area under the concentration-time curve (AUC(0-6h)), the peak plasma concentration (Cmax), the area under the inhibitory concentration curve (AUIC), and the peak-to-minimum-inhibitory-concentration ratio (Cmax/MIC)."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
0.65
"h/l, the average Cmax 10."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
0.65
"The optimal thresholds of pharmacodynamic effectiveness were obtained for most patients with levofloxacin at 500 mg bid."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
0.86
"A series of tetracyclic nitrofuran isoxazoline anti-tuberculosis agents was designed and synthesized to improve the pharmacokinetic properties of an initial lead compound, which had potent anti-tuberculosis activity but suffered from poor solubility, high protein binding and rapid metabolism."( Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
Bruhn, D; Gilliland, JC; Gruppo, V; Lee, RB; Lee, RE; Lenaerts, AJ; Maddox, M; Madhura, DB; McNeil, MR; Meibohm, B; Scherman, MS; Trivedi, A; Yang, L, 2012
)
0.38
" The levofloxacin concentrations were detected by high performance liquid chromatography (HPLC), and the pharmacokinetic parameters were calculated using the 3p97 software program."( Tamsulosin alters levofloxacin pharmacokinetics in prostates derived from rats with acute bacterial prostatitis.
He, HX; He, Y; Qin, GD; Xiao, MZ; Yang, J; Zeng, Y; Zhou, YD, 2013
)
1.14
" Based on pharmacokinetic and pharmacodynamic integration, an oral dose of 10 mg/kg levofloxacin for every 12 h is recommended for a successful clinical effect in quails."( Pharmacokinetics of levofloxacin in Japanese quails (Coturnix japonica) following intravenous and oral administration.
Aboubakr, M, 2012
)
0.91
" Ofloxacin was rapidly distributed from the central to the peripheral compartment as evidenced by a short distribution half-life (0."( Pharmacokinetics, urinary excretion and plasma protein binding of ofloxacin in water buffalo calves (Bubalus bubalis).
Dumka, VK; Ola, AK; Ranjan, B; Sandhu, HS, 2013
)
1.54
" Various pharmacokinetic parameters of RIF significantly differ when administered alone or in combination with OXC and NXC."( Effect of ofloxacin and norfloxacin on rifampicin pharmacokinetics in man.
Barikpoar, E; Brown, S; Ezejiofor, NA; Orisakwe, OE,
)
0.53
" Further studies should determine the optimal pharmacodynamic target for moxifloxacin in a multidrug regimen and clarify safety issues when it is administered at higher doses."( Moxifloxacin population pharmacokinetics and model-based comparison of efficacy between moxifloxacin and ofloxacin in African patients.
Charalambous, S; Chigutsa, E; Denti, P; Harrison, T; Hatherill, M; Jindani, A; McIlleron, HM; Mungofa, S; Simonsson, US; Sirgel, FA; Wiesner, L; Zvada, SP, 2014
)
0.62
" Various pharmacokinetic parameters of INH significantly differed when administered alone or in combination with OXC or with NXC."( Isoniazid Pharmacokinetics in the Presence of Ofloxacin and Norfloxacin Antibiotics.
Anusiem, CA; Barikpoar, E; Brown, SA; Ezejiofor, NA; Orisakwe, OE,
)
0.39
" Drug exposures were lower than those in adults following standard doses and below the proposed pharmacodynamic targets, likely due to more rapid elimination in children."( Pharmacokinetics of ofloxacin and levofloxacin for prevention and treatment of multidrug-resistant tuberculosis in children.
Castel, S; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Norman, J; Schaaf, HS; Thee, S; van der Merwe, PL; Wiesner, L, 2014
)
0.73
"We studied the main pharmacokinetic parameters of ofloxacin when used free and niosomal forms of antibiotic to experimental white mice per os."( [Comparative study of pharmacokinetics of ofloxacin in a free and niosomal forms in experiments on white mice when administered per os].
Kovalev, DA; Kulichenko, AN; Liapustina, LV; Mikhaĭlova, ME; Pisarenko, SV; Siritsa, IuV, 2014
)
0.92
"(S)-(-)-Ofloxacin and (R)-(+)-ofloxacin concentrations in the plasma of Pagrosomus major after drug treatment were detected by chiral high-performance liquid chromatography, and various pharmacokinetic parameters were calculated from these data."( Pharmacokinetic study of ofloxacin enantiomers in Pagrosomus major by chiral HPLC.
Gao, XF; Nie, J; OuYang, XK; Wang, YG; Wu, WJ; Xu, HP; Yang, LY; Yu, D, 2016
)
1.17
" Pharmacokinetic parameters were calculated using noncompartmental analysis."( Pharmacokinetics and Safety of Ofloxacin in Children with Drug-Resistant Tuberculosis.
Castel, S; Dooley, KE; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Seddon, JA; Thee, S; Wiesner, L, 2015
)
0.7
" We aim to compare the culture conversion between new-generation (levofloxacin and moxifloxacin) and old-generation (ciprofloxacin and ofloxacin) fluoroquinolones, develop pharmacokinetic models, and calculate target attainment for levofloxacin and moxifloxacin."( Fluoroquinolones in Drug-Resistant Tuberculosis: Culture Conversion and Pharmacokinetic/Pharmacodynamic Target Attainment To Guide Dose Selection.
Ahmed, S; Al-Shaer, MH; Alghamdi, WA; Alkabab, Y; Alsultan, A; An, G; Banu, S; Barbakadze, K; Cegielski, JP; Heysell, SK; Houpt, E; Kempker, RR; Kipiani, M; Mikiashvili, L; Peloquin, CA, 2019
)
0.75

Compound-Compound Interactions

The efficacy of levofloxacin and dirithromycin, alone and in combination with rifampicin in the treatment of experimental brucellosis was investigated. The antibacterial activity of imipenem combined with norfloxAcin, ciprofloxacIn, or ofloxACin against 43 gram-positive cocci and 53 aerobic gram-negative rods was compared to results obtained with the combination of imIPenem with amikacin.

ExcerptReferenceRelevance
"Multiple injections of ofloxacin (subcutaneous or oral) in combination with a Lactobacillus casei preparation, LC9018 (subcutaneous), in mice infected intravenously with Mycobacterium fortuitum led to a marked delay in the incidence of spinning disease, a lowered incidence of gross renal lesions, and an increase in the rate of elimination of organisms from the kidneys."( Effect of ofloxacin combined with Lactobacillus casei against Mycobacterium fortuitum infection induced in mice.
Saito, H; Sato, K; Tomioka, H, 1990
)
0.99
"Four different sites were randomly selected in each periodontal patient and divided into four group: PT-01-treated site (A), PT-01 treatment combined with scaling (S + A), placebo-treated site (P) and placebo treatment combined with scaling (S + P)."( [Effectiveness of local delivery of ofloxacin using controlled-release strips (PT-01) in periodontal patients. Part 2. Successive delivery system and combination with scaling].
Fukui, M; Hashizume, A; Ikeda, Y; Kobayashi, R; Ogata, C; Ohno, S; Tanaka, S; Teranishi, Y; Ueda, M; Yamamoto, M, 1989
)
0.55
"The in vitro susceptibility of Mycobacterium tuberculosis to new quinolones, ofloxacin and ciprofloxacin, alone and in combination with rifampin or isoniazid, was studied by the agar dilution method."( In vitro susceptibility of Mycobacterium tuberculosis to ofloxacin and ciprofloxacin in combination with rifampin and isoniazid.
Casal, M; González, J; Gutierrez, J; Ruiz, P, 1987
)
0.75
"The antibacterial activity of imipenem combined with norfloxacin, ciprofloxacin, or ofloxacin against 43 gram-positive cocci and 53 aerobic gram-negative rods compared to results obtained with the combination of imipenem with amikacin."( In vitro antibacterial activity of imipenem in combination with newer quinolone derivatives.
Gulden, H; Kern, W; Kurrle, E; Vanek, E, 1988
)
0.51
" Bactericidal titres were determined in sera from volunteers given ofloxacin alone or in combination with fosfomycin or vancomycin."( Bactericidal effect of ofloxacin alone and combined with fosfomycin or vancomycin against Staphylococcus aureus in vitro and in sera from volunteers.
Boussougant, Y; Carbon, C; Dutoit, C; Ichou, F; Weber, P, 1987
)
0.82
" Data are also presented for cefotaxime 2 g every 8 h alone and in combination with ofloxacin."( Role of pharmacokinetics and pharmacodynamics in the design of dosage schedules for 12-h cefotaxime alone and in combination with other antibiotics.
Nix, DE; Schentag, JJ,
)
0.36
"The effects of ofloxacin, clarithromycin, and azithromycin in combination with granulocyte-macrophage colony-stimulating factor (GM-CSF) against Mycobacterium avium-Mycobacterium intracellulare (MAI) were evaluated in an in vitro human macrophage infection model."( Activities of clarithromycin, azithromycin, and ofloxacin in combination with liposomal or unencapsulated granulocyte-macrophage colony-stimulating factor against intramacrophage Mycobacterium avium-Mycobacterium intracellulare.
Bow, LM; Nicolau, DP; Nightingale, CH; Onyeji, CO; Tessier, PR, 1995
)
0.9
"The pharmacodynamic properties of levofloxacin (an optically active isomer of ofloxacin), ofloxacin, and ciprofloxacin, alone and in combination with rifampin, were evaluated over 24 to 48 h against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus (MSSA 1199 and MRSA 494, respectively) in an in vitro infection model."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
0.87
"The antimicrobial effects of ofloxacin against Mycobacterium leprae, either alone or in combination with rifampicin and rifabutin, were studied using mouse foot pad assay technique."( In vivo susceptibility of Mycobacterium leprae to ofloxacin either singly or in combination with rifampicin and rifabutin. Anti-leprosy activity of ofloxacin and ansamycins in mice.
Dhople, AM; Ibanez, MA, 1994
)
0.83
" Its optimal dosage appears to be 400 mg daily, and combination with dapsone and clofazimine does not enhance its activity."( Clinical trial of ofloxacin alone and in combination with dapsone plus clofazimine for treatment of lepromatous leprosy.
Grosset, JH; Ji, B; N'Deli, L; Perani, EG; Petinom, C, 1994
)
0.62
" When combined with one of the three rifamycin analogs, synergism was obtained with KRM-1648 and rifabutin but not with rifampin."( In vitro activity of levofloxacin, singly and in combination with rifamycin analogs, against Mycobacterium leprae.
Dhople, AM; Ibanez, MA, 1995
)
0.6
" Despite the antipseudomonal advantage noted for ciprofloxacin monotherapy, it is unknown whether this advantage is maintained when the fluoroquinolones are used in combination with antipseudomonal beta-lactams such as ceftazidime and piperacillin."( Comparison of the bactericidal activities of ofloxacin and ciprofloxacin alone and in combination with ceftazidime and piperacillin against clinical strains of Pseudomonas aeruginosa.
Klepser, ME; Nicolau, DP; Nightingale, CH; Patel, KB; Quintiliani, R, 1995
)
0.8
" The potential therapeutic activities of these agents both alone and combined with ethambutol were evaluated in a human macrophage test system and in the beige mouse animal test system with MAC strain 101."( Activities of bay Y 3118, levofloxacin, and ofloxacin alone or in combination with ethambutol against Mycobacterium avium complex in vitro, in human macrophages, and in beige mice.
Barbara-Burnham, L; Bermudez, LE; Inderlied, CB; Kolonoski, P; Wu, M; Young, LS, 1996
)
0.59
"In the present study, we evaluated the in vivo anti-Mycobacterium leprae activities of KRM-1648 (KRM) given at long intervals in combination with ofloxacin (OFLX), clofazimine (CFZ), and dapsone (DDS)."( Studies on therapeutic activity of benzoxazinorifamycin KRM-1648 in combination with other antimicrobial agents and biological response modifiers interferon-gamma and granulocyte-macrophage colony-stimulating factor against M. leprae infection in athymic
Maw, WW; Saito, H; Sato, K; Tomioka, H, 1997
)
0.5
" It is concluded that DU-6859a and trovafloxacin are very potent against enterococci, especially when combined with gentamicin."( In vitro activity of quinupristin/dalfopristin and newer quinolones combined with gentamicin against resistant isolates of Enterococcus faecalis and Enterococcus faecium.
Giamarellos-Bourboulis, EJ; Giamarellou, H; Grecka, P; Sambatakou, H, 1998
)
0.3
"We tested three fluoroquinolones (ciprofloxacin, levofloxacin, and trovafloxacin), each combined with each of four beta-lactams (cefoperazone, ceftriaxone, imipenem, and meropenem) for synergy against clinical isolates of nosocomial strains of Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Burkholderia cepacia."( In vitro activity of ciprofloxacin, levofloxacin, and trovafloxacin, alone and in combination with beta-lactams, against clinical isolates of Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Burkholderia cepacia.
Alperstein, P; France, K; Isenberg, HD, 1999
)
0.88
"To evaluate the activity of vancomycin and levofloxacin alone and combined with rifampin against planktonic and sessile cells."( Comparative in vitro activity of vancomycin and levofloxacin in combination with rifampin against planktonic versus sessile cells of Staphylococcus epidermidis.
Kang-Birken, SL, 2000
)
0.82
"The antimicrobial effect of a benzoxazinorifamycin, KRM-1648, either alone or in combination with ofloxacin, was evaluated in vitro against two type strains and six clinical isolates of Mycobacterium ulcerans."( In vitro activity of KRM-1648, either singly or in combination with ofloxacin, against Mycobacterium ulcerans.
Dhople, AM, 2001
)
0.76
"1, 1, 5 and 10 mg/ml), phenylbutazone (1000 microgram/ml) and acetylsalicylic acid (25, 250, 2500 microgram/ml) alone, and combined with 10 mg/ml of ofloxacin on the respiratory burst."( [Effect of anti-inflammatory drugs, alone and combined with ofloxacin, on the respiratory burst of human polymorphonuclear leukocytes].
Cabrera, E; Cantón, E; Martínez, P; Orero, A; Velert, MM, 2001
)
0.75
"The efficacy of two polymyxin-like peptides, KFFKFFKFF and IKFLKFLKFL, alone and combined with levofloxacin, was investigated in a rat model of septic shock."( Therapeutic efficacy of intraperitoneal polymyxin B and polymyxin-like peptides alone or combined with levofloxacin in rat models of septic shock.
Cirioni, O; Ghiselli, R; Giacometti, A; Kamysz, W; Kasprzykowski, F; Mackiewicz, Z; Mocchegiani, F; Orlando, F; Paggi, AM; Saba, V; Scalise, G, 2002
)
0.75
"The synergistic potential of levofloxacin, ofloxacin and ciprofloxacin combined with aztreonam, ceftazidime, or piperacillin was compared using 24 strains of Pseudomonas aeruginosa with varying susceptibility profiles."( In vitro synergy testing of levofloxacin, ofloxacin, and ciprofloxacin in combination with aztreonam, ceftazidime, or piperacillin against Pseudomonas aeruginosa.
Jung, R; Messick, CR; Pendland, SL, 2002
)
0.88
" Only the group treated with quinupristin/dalfopristin combined with levofloxacin or doxycycline showed no evidence of staphylococcal infection."( Quinupristin/dalfopristin bonding in combination with intraperitoneal antibiotics prevent infection of knitted polyester graft material in a subcutaneous rat pouch model infected with resistant Staphylococcus epidermidis.
Cirioni, O; D'Amato, G; Del Prete, M; Ghiselli, R; Giacometti, A; Mocchegiani, F; Orlando, F; Saba, V; Scalise, G, 2002
)
0.55
"The antimicrobial effects of sitafloxacin (DU-6859a) against Mycobacterium leprae, either singly or in combination with either rifampicin, rifabutin or KRM-1648, were studied using a mouse footpad assay technique and the results were compared with those obtained with ofloxacin."( In vivo susceptibility of Mycobacterium leprae to sitafloxacin (DU-6859a), either singly or in combination with rifampicin analogues.
Dhople, AM; Namba, K, 2003
)
0.5
"A rat model was used to investigate the efficacy of linezolid, alone or in combination with levofloxacin and vancomycin, in the prevention of vascular prosthetic graft infection resulting from methicillin-resistant Staphylococcus epidermidis with intermediate resistance to glycopeptides."( Prophylactic efficacy of linezolid alone or combined with levofloxacin and vancomycin in a rat subcutaneous pouch model of graft infection caused by Staphylococcus epidermidis with intermediate resistance to glycopeptides.
Cirioni, O; D'Amato, G; Del Prete, MS; Ghiselli, R; Giacometti, A; Mocchegiani, F; Orlando, F; Saba, V; Scalise, G; Silvestri, C, 2003
)
0.78
" This study was conducted to evaluate the bioequivalence of levofloxacin when administered in a fasting state as compared to when it was administered with a common breakfast of calcium-fortified orange juice and ready-to-eat cereal."( Lack of bioequivalence of levofloxacin when coadministered with a mineral-fortified breakfast of juice and cereal.
Amsden, GW; Johnson, PW; Whitaker, AM, 2003
)
0.85
"The efficacy of levofloxacin and dirithromycin, alone and in combination with rifampicin in the treatment of experimental brucellosis was investigated."( Efficacy of oral levofloxacin and dirithromycin alone and in combination with rifampicin in the treatment of experimental murine Brucella abortus infection.
Arda, B; Gökengin, D; Gürel, O; Tunçel, M; Yaimazhan, T, 2004
)
0.98
"Disposition of uric acid upon administration of ofloxacin (O) alone and in combination with other anti-tuberculosis drugs, rifampicin (R), isoniazid (H) and pyrazinamide (Z) was studied."( Disposition of uric acid upon administration of ofloxacin alone and in combination with other anti-tuberculosis drugs.
Gurumurthy, P; Kumar, AK, 2004
)
0.83
"The in vitro effects of spectinomycin and ceftriaxone, alone or in combination with erythromycin, ofloxacin, and doxycycline, against Chlamydia trachomatis were investigated by the checkerboard method and compared by Ridit (reference identical unit) analysis."( In vitro effects of spectinomycin and ceftriaxone alone or in combination with other antibiotics against Chlamydia trachomatis.
Gong, X; Mabey, D; Shang, S; Wang, Q; Xia, L; Zhang, J; Zhao, J; Zhong, M, 2005
)
0.55
" Drug eruption due to a drug combination appears to be very rare."( Multiple fixed drug eruption due to drug combination.
Hara, H; Yokoyama, A, 2005
)
0.33
"The aim of this study was to evaluate the ability of levofloxacin and ciprofloxacin alone and in combination with either ceftazidime, cefepime, imipenem, piperacillin-tazobactam or amikacin to select for antibiotic-resistant mutants of Pseudomonas aeruginosa and Acinetobacter spp."( In vitro selection of resistance in Pseudomonas aeruginosa and Acinetobacter spp. by levofloxacin and ciprofloxacin alone and in combination with beta-lactams and amikacin.
De Vecchi, E; Drago, L; Gismondo, MR; Nicola, L; Tocalli, L, 2005
)
0.8
" For multi-step studies, MICs were determined after five serial passages on antibiotic-gradient plates containing each antibiotic alone or in combination with levofloxacin or ciprofloxacin."( In vitro selection of resistance in Pseudomonas aeruginosa and Acinetobacter spp. by levofloxacin and ciprofloxacin alone and in combination with beta-lactams and amikacin.
De Vecchi, E; Drago, L; Gismondo, MR; Nicola, L; Tocalli, L, 2005
)
0.75
"Preincubation of pneumococci with sub-MIC concentrations of ceftriaxone (1/16x MIC), cefotaxime (1/8x MIC), and meropenem (1/4x MIC) alone or combined with levofloxacin (1/8x MIC) over 6 h prevents the emergence of levofloxacin-resistant mutants after 96 h of incubation but does not affect the intracellular accumulation of levofloxacin in two penicillin-resistant pneumococcal strains, suggesting a link between the mechanism of action of beta-lactams and the emergence of quinolone-induced resistance in pneumococci."( Preincubation of pneumococci with beta-lactams alone or combined with levofloxacin prevents quinolone-induced resistance without increasing intracellular levels of levofloxacin.
Cottagnoud, M; Cottagnoud, P; Johnson, M; Piddock, L, 2005
)
0.76
"To explore the feasibility of utilizing polymerase chain reaction-single strand conformation polymorphism (PCR-SSCP) analysis combined with Southern blot to detect ofloxacin (OFLX)-resistant Mycobacterium tuberculosis, and figure out the boundary between the OFLX-susceptible and resistant Mycobacterium tuberculosis."( [Polymerase chain reaction-single strand conformation polymorphism analysis combined with nucleic acid hybridization to detect ofloxacin-resistant Mycobacterium tuberculosis mutation selected in vitro].
Li, CY; Li, WM; Ma, Y; Qiu, YQ; Tian, M; Wang, SM; Zhang, JY; Zhang, XX; Zhao, B; Zhao, YL, 2005
)
0.73
" To prove the repeatability of PCR-SSCP combined with Southern blot, 36 clinical isolated OFLX-resistant strains were tested."( [Polymerase chain reaction-single strand conformation polymorphism analysis combined with nucleic acid hybridization to detect ofloxacin-resistant Mycobacterium tuberculosis mutation selected in vitro].
Li, CY; Li, WM; Ma, Y; Qiu, YQ; Tian, M; Wang, SM; Zhang, JY; Zhang, XX; Zhao, B; Zhao, YL, 2005
)
0.53
" Compared with the H(37)Ra, the similar single-stranded shift caused by the single-stranded conformation change was viewed in the 36 clinical isolated OFLX-resistant strains by PCR-SSCP combined with Southern hybridization."( [Polymerase chain reaction-single strand conformation polymorphism analysis combined with nucleic acid hybridization to detect ofloxacin-resistant Mycobacterium tuberculosis mutation selected in vitro].
Li, CY; Li, WM; Ma, Y; Qiu, YQ; Tian, M; Wang, SM; Zhang, JY; Zhang, XX; Zhao, B; Zhao, YL, 2005
)
0.53
"PCR-SSCP analysis combined with Southern blot can clearly distinguish OFLX-susceptible from OFLX-resistant strains."( [Polymerase chain reaction-single strand conformation polymorphism analysis combined with nucleic acid hybridization to detect ofloxacin-resistant Mycobacterium tuberculosis mutation selected in vitro].
Li, CY; Li, WM; Ma, Y; Qiu, YQ; Tian, M; Wang, SM; Zhang, JY; Zhang, XX; Zhao, B; Zhao, YL, 2005
)
0.53
"The mutant prevention concentrations (MPCs) of levofloxacin alone and in combination with ceftazidime, colistin (polymyxin E), meropenem, piperacillin-tazobactam, and tobramycin were established against Pseudomonas aeruginosa."( Mutant prevention concentrations of levofloxacin alone and in combination with azithromycin, ceftazidime, colistin (Polymyxin E), meropenem, piperacillin-tazobactam, and tobramycin against Pseudomonas aeruginosa.
Adam, HJ; Laing, N; Mayer, M; Zhanel, GG, 2006
)
0.86
" To explore strategies to overcome resistance development, we studied the effects of rifalazil in combination with several different antibiotics in an in vitro time-kill model, against both log phase and stationary phase Staphylococcus aureus cells."( Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro.
Murphy, CK; Osburne, MS; Rothstein, DM, 2006
)
0.58
"The objective of this paper was to investigate the in vitro effects of linezolid combined with five antistaphylococcal antibiotics--doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin--upon methicillin-susceptible Staphylococcus aureus (MSSA)."( In vitro activity of linezolid in combination with doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin against methicillin-susceptible Staphylococcus aureus.
Cantón, E; Colombo Gainza, E; Gil Brusola, A; Gobernado, M; Ortiz Estévez, R; Sahuquillo Arce, JM, 2006
)
0.76
"To study the therapeutic efficacy of Longqingpian combined with Levofloxacin on Type IIIA prostatitis."( [Longqingpian combined with levofloxacin highly effective for type IIIA prostatitis].
Cai, X; Huang, YF; Shang, XJ; Teng, WH; Xu, H, 2007
)
0.86
"Longqingpian combined with Levofloxacin is highly effective for Type IIIA prostatitis, by relieving pain and voiding symptoms, decreasing the leukocyte count in EPS and improving the life quality of the patients."( [Longqingpian combined with levofloxacin highly effective for type IIIA prostatitis].
Cai, X; Huang, YF; Shang, XJ; Teng, WH; Xu, H, 2007
)
0.91
" In base to the differences in the kinetic behaviour of ofloxacin with respect to ciprofloxacin and norfloxacin, binary mixtures of the drugs were resolved by using the time-resolved chemiluminescence signals, in combination with first-order partial least-squares (PLS) multivariate calibration."( Resolution of ofloxacin-ciprofloxacin and ofloxacin-norfloxacin binary mixtures by flow-injection chemiluminescence in combination with partial least squares multivariate calibration.
Alañón Molina, A; Durán Merás, I; Jiménez Girón, A; Muñoz de la Peña, A; Murillo, JA, 2007
)
0.95
" When the three FQs were individually combined with CLR in vitro, mild antagonism was observed for 53 to 57% of the tested isolates."( In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
Fukushima, K; Higashiyama, Y; Hirakata, Y; Kohno, S; Kohno, Y; Miyazaki, Y; Ohno, H; Yanagihara, K, 2007
)
0.34
"To evaluate the clinical efficacy of the Chinese medicine Yiqigushen Capsule combined with levofloxacin on type III A prostatitis."( [Yiqigushen capsule combined with levofloxacin highly effective for type III A prostatitis].
Guo, DF; Wang, HP; Zhang, HZ, 2008
)
0.84
"A total of 180 patients with type III A prostatitis were equally randomized into a treatment group, which received Yiqigushen Capsule combined with levofloxacin, and a control group, which was given Yiqigushen Capsule only, both for 4 weeks."( [Yiqigushen capsule combined with levofloxacin highly effective for type III A prostatitis].
Guo, DF; Wang, HP; Zhang, HZ, 2008
)
0.82
"Yiqigushen Capsule combined with levofloxacin is highly effective for type III A prostatitis."( [Yiqigushen capsule combined with levofloxacin highly effective for type III A prostatitis].
Guo, DF; Wang, HP; Zhang, HZ, 2008
)
0.89
"To evaluate the efficacy and safety of corticoid in combination with an antibiotic in the treatment of chronic nonbacterial prostatitis (CNP)."( [Corticoid combined with an antibiotic for chronic nonbacterial prostatitis].
Hou, Y; Lü, C; Wu, ZP; Xiao, N; Yang, MG; Zhao, XK, 2009
)
0.35
"Prednisone in combination with an antibiotic can effectively relieve pain and voiding symptoms, improve QOL and reduce WBC in the EPS of CNP patients, and therefore well deserves to be recommended in clinical application."( [Corticoid combined with an antibiotic for chronic nonbacterial prostatitis].
Hou, Y; Lü, C; Wu, ZP; Xiao, N; Yang, MG; Zhao, XK, 2009
)
0.35
"In this study the bactericidal effect of the N-terminal fragment of the frog skin peptide esculentin-1b [Esc(1-18)] in combination with clinically used antimicrobial agents was evaluated against Stenotrophomonas maltophilia, either in standard conditions (phosphate buffer) or in the presence of human serum."( In vitro bactericidal activity of the N-terminal fragment of the frog peptide esculentin-1b (Esc 1-18) in combination with conventional antibiotics against Stenotrophomonas maltophilia.
Barnini, S; Barra, D; Batoni, G; Brancatisano, FL; Campa, M; Capria, AL; Di Luca, M; Esin, S; Maisetta, G; Mangoni, ML; Pichierri, G, 2009
)
0.35
" (Rubiaceae) alone and in combination with antibiotics (doxycycline and ofloxacin) by means of fractional inhibitory concentration indices (FICI) as well as by the use of time-kill assays against one Gram-positive bacterium (Staphylococcus aureus) and three Gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa) was studied."( In vitro synergistic effect of doxycycline & ofloxacin in combination with ethanolic leaf extract of Vangueria spinosa against four pathogenic bacteria.
Bhattacharjee, I; Chandra, G; Chatterjee, SK, 2009
)
0.85
" spinosa alone and also in combination with antibiotics using the fractional inhibitory concentration (FIC) and time-kill assay method."( In vitro synergistic effect of doxycycline & ofloxacin in combination with ethanolic leaf extract of Vangueria spinosa against four pathogenic bacteria.
Bhattacharjee, I; Chandra, G; Chatterjee, SK, 2009
)
0.61
"Levofloxacin and tobramycin, alone and in combination with cefepime, were investigated for their in vitro activities and post-antibiotic effects (PAEs) on Pseudomonas aeruginosa."( Post-antibiotic effect of levofloxacin and tobramycin alone or in combination with cefepime against Pseudomonas aeruginosa.
Otuk, G; Ozbek, B, 2009
)
1.27
"To investigate the effects of inactivation of CD(4)(+)CD(25)(+) regulatory T cells (Treg) combined with the administration of levofloxacin (LFX) on the cellular immune response of murine tuberculosis."( [The effect of CD4+ CD25+ regulatory T cell inactivation combined with levofloxacin on murine tuberculosis].
Chen, XC; Gou, JZ; Li, MZ; Peng, YZ; Tang, ZJ; Tong, XD; Yue, XH; Zhou, BP, 2009
)
0.79
" One hundred forty-eight cases received levofloxacin and 137 received amikacin, both in combination with ceftazidime."( Empirical therapy with ceftazidime combined with levofloxacin or once-daily amikacin for febrile neutropenia in patients with neoplasia: a prospective comparative study.
Bompolaki, I; Bozionelou, V; Falagas, ME; Kalpadaki, C; Karageorgopoulos, DE; Koutsounaki, E; Mitsikostas, P; Samonis, G; Sgouros, J; Taktikou, V, 2012
)
0.89
"The in vitro antimicrobial activities of usnic acid were evaluated in combination with five therapeutically available antibiotics, using checkerboard microdilution assay against methicillin-resistant clinical isolates strains of Staphylococcus aureus."( In vitro interaction of usnic acid in combination with antimicrobial agents against methicillin-resistant Staphylococcus aureus clinical isolates determined by FICI and ΔE model methods.
Amicosante, G; Bellio, P; Brisdelli, F; Celenza, G; Garbarino, JA; Nicoletti, M; Perilli, M; Piovano, M; Segatore, B; Setacci, D, 2012
)
0.38
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" This method was successfully applied to the drug interaction study of Shuang-huang-lian freeze-dried powder combined with levofloxacin injection after intravenous administration to rats."( Development of an LC-MS method for determination of three active constituents of Shuang-huang-lian injection in rat plasma and its application to the drug interaction study of Shuang-huang-lian freeze-dried powder combined with levofloxacin injection.
Bi, K; Chen, X; Geng, L; Liu, Z; Song, X; Ye, J; Zhao, X, 2012
)
0.77
"Topical application of the gentamicin-collagen sponge seems safe and may improve clinical and microbiological outcomes of diabetic foot infections of moderate severity when combined with standard of care."( Topical application of a gentamicin-collagen sponge combined with systemic antibiotic therapy for the treatment of diabetic foot infections of moderate severity: a randomized, controlled, multicenter clinical trial.
Edmonds, M; Kuss, M; Lipsky, BA; Reyzelman, A; Sigal, F,
)
0.13
" Herein, we developed a fine floating tablet via compression coating of hydrophilic polymer (hydroxypropyl cellulose) combined with effervescent agent (sodium bicarbonate) to achieve simultaneous control of release rate and location of ofloxacin."( Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.
Chen, H; Ma, N; Qi, X; Rui, Y; Wu, Z; Yang, F, 2015
)
0.86
"A green, fast, and efficient pH-induced natural deep eutectic solvent combined with vortex-assisted dispersive liquid-liquid microextraction method (pH-NADES-VA-DLLME) followed by HPLC was established for determination of ofloxacin (OFL), ciprofloxacin (CIP) and enrofloxacin (ENR) in honey."( Determination of quinolone antibiotics in honey by pH-induced natural deep eutectic solvent combined with vortex-assisted dispersive liquid-liquid microextraction.
Liu, J; Qin, F; Xiong, Z; Zhao, C; Zhao, L; Zhu, X, 2022
)
0.91

Bioavailability

Levofloxacin demonstrates good safety, bioavailability and tissue penetration, thus maintaining adequate concentrations at the site of infection. The oral bioavailability is decreased by the coadministration of antacids, but ofl Oxacin does not alter serum theophylline concentrations.

ExcerptReferenceRelevance
" When aluminum hydroxide, ferrous sulfate, and magnesium oxide were coadministered with DR-3355, the relative bioavailability of DR-3355 was decreased to 56, 81, and 78%, respectively, of that for DR-3355 (100 mg) alone."( Effects of antacids, ferrous sulfate, and ranitidine on absorption of DR-3355 in humans.
Aoki, H; Hakusui, H; Okazaki, O; Sakai, O; Shiba, K; Shimada, J, 1992
)
0.28
" The pharmacokinetics of ofloxacin are characterised by almost complete bioavailability (95 to 100%), peak serum concentrations in the range of 2 to 3 mg/L after a 400mg oral dose and an average half-life of 5 to 8h."( Ofloxacin clinical pharmacokinetics.
Bailey, EM; Lamp, KC; Rybak, MJ, 1992
)
2.03
"The relative bioavailability and pharmacokinetics of ofloxacin tablets and a reference oral solution of ofloxacin were compared in 32 normal male subjects using a randomized two-way crossover design."( Bioavailability and pharmacokinetics of oral ofloxacin formulations in normal subjects.
Flor, SC; LeBel, M; Stein, GE; Zinny, M, 1991
)
0.79
" The oral bioavailability is decreased by the coadministration of antacids, but ofloxacin does not alter serum theophylline concentrations."( Ofloxacin.
Scheld, WM; Tunkel, AR, 1991
)
1.95
" These include the high bioavailability from oral administration and the fact that the product is excreted almost entirely by the kidney, primarily as the active parent compound."( Worldwide clinical experience with ofloxacin in urologic cases.
Corrado, ML, 1991
)
0.56
"The bioavailability of ofloxacin after a single dose of one of two tablet formulations (200 or 400 mg) or a liquid formulation (1."( The bioavailability of ofloxacin from several formulations.
Beals, B; Flor, S, 1991
)
0.9
"The pharmacokinetics and bioavailability of ofloxacin in 20 healthy male volunteers were studied in an open-label, randomized, two-way crossover study."( Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers.
Nightingale, CH; Quintiliani, R; Sweeney, KR; Yuk, JH, 1991
)
0.81
"The effects of 15- and 5-ml doses of magnesium-aluminum hydroxide (MAH) and calcium carbonate (CC) antacids, respectively, on the bioavailability of ofloxacin after single oral 400-mg doses of ofloxacin were investigated in a 32-subject, randomized, crossover, open-label study."( Effects of magnesium-aluminum hydroxide and calcium carbonate antacids on bioavailability of ofloxacin.
Flor, S; Guay, DR; Matzke, GR; Opsahl, JA; Tack, K, 1990
)
0.7
"The pharmacokinetic properties of the new fluoroquinolones are characterized by a high volume of distribution, long biological half-life, low serum protein binding, elimination by renal and extrarenal mechanisms with high total and renal clearances, limited biotransformation and moderate to excellent bioavailability after oral administration."( Quinolone pharmacokinetics and metabolism.
Boeckk, M; Borner, K; Deppermann, N; Höffken, G; Koeppe, P; Lode, H, 1990
)
0.28
"Quinolone is reported to interact with caffeine, often resulting in an increase both in the plasma half-life and AUC, a decrease in total plasma clearance, and little change in the absorption rate constant and maximum plasma level."( Pharmacokinetic determination of relative potency of quinolone inhibition of caffeine disposition.
Barnett, G; Carbó, M; de la Torre, R; Segura, J, 1990
)
0.28
" Following oral administration, norfloxacin and ciprofloxacin are well absorbed and the bioavailability of ofloxacin is almost 100%."( The pharmacokinetics of oral quinolones (norfloxacin, ciprofloxacin, ofloxacin).
Alestig, K, 1990
)
0.77
" Ofloxacin was well absorbed orally."( [Efficacy of ofloxacin in treating typhoid fever].
Gu, XJ; Wang, F; Zhang, MF, 1989
)
1.56
" BMY 40062 exhibited longer half-life, higher maximum concentration in serum, greater area under the curve, and better bioavailability in mice after oral dosing than ciprofloxacin."( In vitro and in vivo antibacterial activities of BMY 40062, a new fluoronaphthyridone.
Desiderio, JV; Fung-Tomc, J; Kessler, RE; Tsai, YH; Warr, G, 1989
)
0.47
" A prediction equation is developed under statistical and physiological considerations which correlates both factors with the intestinal absorption rate parameter Kapp."( Prediction of the effect of ofloxacine on intestinal absorption: effect of the body weight and substrate concentration.
Barrio, JP; Gómez, G; Melcón, B; Prieto, JG, 1988
)
0.57
" There were no differences in ofloxacin recovery after oral or intravenous administration, confirming that absolute bioavailability of the oral form is excellent."( Absence of crystalluria and estimation of renal parameters after oral and intravenous ofloxacin as compared to placebo in healthy volunteers.
Grötsch, H; Lorenz, H; Malerczyk, V; Verho, M, 1988
)
0.79
", hydrophobicity and bioavailability including high serum concentrations and easy entry into bacterial cells."( International experiences with ofloxacin, a new quinolone.
Mitsuhashi, S, 1986
)
0.56
" Analysis of ofloxacin after multiple dosing regimens in these patients showed measurable concentrations of the drug in the various tissues examined; hence suggesting a relative good bioavailability of the drug, which presumably reflected the high degree of success rates in these patients."( Pharmacokinetics and tissue distribution of ofloxacin in human subjects during a multiple dose regimen.
Bonaccorsi, S; Carlino, S; De Bernardis, E; Picari, M; Rizza, V, 1988
)
0.91
"The bioavailability of ofloxacin in tonsil tissue, after a single oral dose of 200 mg 2 h before surgery, was evaluated in 14 patients undergoing tonsillectomy for recurrent or chronic infection."( Pharmacokinetic evaluation of ofloxacin in serum and tonsils.
D'Hondt, G; Gordts, B; Van Landuyt, HW, 1988
)
0.87
" Ofloxacin is well absorbed after oral administration."( Ofloxacin: its pharmacology, pharmacokinetics, and potential for clinical application.
Drew, RH; Gallis, HA, 1988
)
2.63
" They are well absorbed after oral administration, and some achieve serum and tissue levels well exceeding the minimal inhibitory concentrations for susceptible bacteria."( Symposium on antimicrobial agents. The quinolones.
Walker, RC; Wright, AJ, 1987
)
0.27
" However, the areas under the serum concentration-time curves (AUC0-28), as also the urinary recoveries did not differ significantly, showing that only the speed of absorption, but not the bioavailability of the tablet is changed in comparison to the oral solution form."( Relative bioavailability of ofloxacin tablets in comparison to oral solution.
Korn, A; Malerczyk, V; Rangoonwala, R; Verho, M, 1987
)
0.57
"The pharmacokinetic properties of the new quinolones are characterised by a high volume of distribution, long biological half-life, low serum protein binding, elimination mainly by the kidneys, high total and renal clearances, limited biotransformation and a moderate to excellent bioavailability after oral administration."( Comparative pharmacokinetics of new quinolones.
Borner, K; Glatzel, P; Höffken, G; Koeppe, P; Lode, H; Olschewski, P; Prinzing, C; Reimnitz, D; Sievers, B; Wiley, R, 1987
)
0.27
"Ofloxacin is a new quinolone-carboxylic acid derivative with a broad spectrum of activity, excellent bioavailability after oral administration and insignificant metabolisation."( [Summarized results of clinical phase II and III studies with ofloxacin (HOE 280) in Europe].
Blomer, R; Bruch, K; Zahlten, RN, 1986
)
1.95
") decreased the bioavailability of LVFX by 15-52%."( Premarketing population pharmacokinetic study of levofloxacin in normal subjects and patients with infectious diseases.
Hori, R; Kagimoto, N; Nomura, H; Okumura, K; Tanigawara, Y, 1995
)
0.54
" The presence of aluminum reduces the absorption rate of this quinolone but does not modify the percentage of the absorbed dose."( Oral absorption of ofloxacin administered together with aluminum.
Dominguez-Gil Hurlé, A; Martínez Cabarga, M; Sánchez Navarro, A, 1994
)
0.62
" In this study, the effect of the Chinese medicines Sho-saiko-to (TJ-9), Rikkunshi-to (TJ-43) and Sairei-to (TJ-114) on the bioavailability of ofloxacin (OFLX) was investigated in seven volunteers in an open, random crossover fashion."( Lack of effect of Chinese medicines on bioavailability of ofloxacin in healthy volunteers.
Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K; Wang, L; Yamaki, K, 1994
)
0.73
" These results strongly suggest that adsorption of quinolones by aluminum hydroxide reprecipitated in the small intestine would play an important role in the reduced bioavailability of quinolones after coadministration with aluminum-containing antacids."( Mechanistic study of inhibition of levofloxacin absorption by aluminum hydroxide.
Aoki, H; Fujisawa, C; Hakusui, H; Kurata, T; Ohshima, Y; Okazaki, O; Tanaka, M, 1993
)
0.56
" Since previous studies have not demonstrated any change in the bioavailability of ofloxacin in infectious disease patients, this study supports the interchangeability of these dosing regimens."( Bioequivalence of oral and intravenous ofloxacin after multiple-dose administration to healthy male volunteers.
Chow, AT; Flor, SC; Rogge, MC, 1993
)
0.78
" Effects of aluminium hydroxide on the oral bioavailability of OFLX and OFLX-PVM were investigated in rabbits."( Effects of aluminium-containing antacid on bioavailability of ofloxacin following oral administration of pivaloyloxymethyl ester of ofloxacin as prodrug.
Hibino, S; Kihira, K; Konishi, T; Maeda, Y; Omoda, K; Takahashi, M; Tsukiai, S, 1993
)
0.53
"Amoxycillin and ofloxacin are both well absorbed after oral administration, despite being hydrophilic."( Lack of effect of amoxycillin on the absorption of ofloxacin.
Alván, G; Hellgren, U; Nilsson-Ehle, I; Paintaud, G, 1993
)
0.88
" These results indicate that the Chinese medicines tested have no significant effect on the rate and extent of bioavailability or renal excretion of LVFX."( Effects of traditional Chinese medicines on pharmacokinetics of levofloxacin.
Hasegawa, T; Muraoka, I; Nabeshima, T; Nadai, M; Takagi, K; Yamaki, K, 1995
)
0.53
"To investigate the regional differences in small intestinal (SI) metabolism and permeability for several compounds and to ascertain the potential significance of these differences on the reported reductions in regional bioavailability in humans."( Determination intestinal metabolism and permeability for several compounds in rats. Implications on regional bioavailability in humans.
Hu, P; Sinko, PJ, 1996
)
0.29
"It has been reported that captopril and ddI demonstrate regional intestinal bioavailability in several species including humans."( Determination intestinal metabolism and permeability for several compounds in rats. Implications on regional bioavailability in humans.
Hu, P; Sinko, PJ, 1996
)
0.29
" Levofloxacin is a fluoroquinolone with excellent bioavailability properties that affords potential use in the treatment of a wide variety of infections caused by Gram-positive organisms such as streptococci."( The comparative antimicrobial activity of levofloxacin tested against 350 clinical isolates of streptococci.
Biedenbach, DJ; Jones, RN, 1996
)
1.11
" The absorption rate from the intestine into the portal system was calculated from the portal-venous difference in the plasma concentration of levofloxacin, considering the distribution of levofloxacin into erythrocytes."( Local absorption kinetics of levofloxacin from intestinal tract into portal vein in conscious rat using portal-venous concentration difference.
Fujieda, Y; Ito, T; Nakagawa, T; Yamaoka, K, 1996
)
0.78
" By considering the bioavailability of levofloxacin in rat, the hepatic extraction ratio in vivo of levofloxacin was estimated to be 30%."( Local absorption kinetics of levofloxacin from intestinal tract into portal vein in conscious rat using portal-venous concentration difference.
Fujieda, Y; Ito, T; Nakagawa, T; Yamaoka, K, 1996
)
0.84
" The mean (95% CI) oral bioavailability was 91% (74 to 109%)."( Pharmacokinetics of oral and intravenous ofloxacin in children with multidrug-resistant typhoid fever.
Bethell, DB; Day, NP; Dung, NM; Dung, NQ; Linh, NT; Loan, HT; MacGowan, AP; McMullin, C; Minh, LT; Tam, DT; Vinh, H; White, LO; White, NJ, 1996
)
0.56
"The properties of ofloxacin such as a new mechanism of action, broad spectrum and high antimicrobial activity, 100-percent bioavailability and rapid penetration to the body tissues, etc."( [Use of ofloxacin in infections which do not readily respond to treatment].
Zalaudek, G, 1996
)
1.06
" We determined if collagen cross-linking affects ofloxacin bioavailability at three different collagen shield dissolution times."( Effect of collagen cross-linking in collagen corneal shields on ocular drug delivery.
Horibe, Y; Kawashima, Y; Kuwano, M, 1997
)
0.55
" The bioavailability of oral levofloxacin approaches 100% and is little affected by the administration with food."( The clinical pharmacokinetics of levofloxacin.
Chow, AT; Fish, DN, 1997
)
0.86
"To determine the levels of two quinolones, ofloxacin and ciprofloxacin, potent broad-spectrum antibiotics with very good oral bioavailability and low minimum inhibitory concentrations (MICs) for most pathogens, in the prostates of patients who underwent transurethral resection of the prostate (TURP) after oral ingestion for surgical prophylaxis."( A comparative study of the distribution of ofloxacin and ciprofloxacin in prostatic tissues after simultaneous oral ingestion.
Cheng, C; Foo, KT; Li, MK; Png, JC; Rekhraj, IR; Tan, E, 1997
)
0.82
" The study reveals that the bioavailability (rate and extent) of levofloxacin was not affected by either age or gender."( Absence of age and gender effects on the pharmacokinetics of a single 500-milligram oral dose of levofloxacin in healthy subjects.
Chien, SC; Chow, AT; Natarajan, J; Nayak, RK; Rogge, MC; Williams, RR; Wong, FA, 1997
)
0.75
" In conclusion, the absorption of levofloxacin was slightly delayed by food, although the overall bioavailability of levofloxacin following a high-fat meal was not altered."( Effects of food and sucralfate on a single oral dose of 500 milligrams of levofloxacin in healthy subjects.
Dix, R; Hafkin, B; Hoh, J; Lee, ID; Lee, LJ, 1997
)
0.8
"5 h and mean absolute bioavailability of > or =99%."( Pharmacokinetic profile of levofloxacin following once-daily 500-milligram oral or intravenous doses.
Cheung, WK; Chien, SC; Chow, AT; Curtin, C; Fowler, CL; Gisclon, LG; Natarajan, J; Rogge, MC; Williams, RR; Wong, F, 1997
)
0.59
" Furthermore, ofloxacin competes with other fluoroquinolones or P-glycoprotein substrates for a common secretory pathway, resulting in an increased rate of absorption for both ofloxacin isomers; this is probably an indirect result of their reduced efflux from the apical side of intestinal cells."( Absorption of ofloxacin isomers in the rat small intestine.
Carbon, C; Colas-Linhart, N; Dautrey, S; Farinotti, R; Rabbaa, L, 1997
)
1.02
" The relative rectal bioavailability (AUC rectal/AUC oral) was 49."( Kinetics of absorption and elimination of ofloxacin in humans after oral and rectal administrations.
Aigbavboa, SO; Akerele, JO; Eboka, CJ; Okor, RS, 1997
)
0.56
" High oral bioavailability allows switching from intravenous to oral therapy without dosage adjustment."( Levofloxacin. Its use in infections of the respiratory tract, skin, soft tissues and urinary tract.
Lamb, HM; Langtry, HD, 1998
)
0.92
" The availability of an intravenous formulation and near-complete oral bioavailability allow ofloxacin to be administered as a sequential regimen without loss of activity."( Ofloxacin. A reappraisal of its use in the management of genitourinary tract infections.
Balfour, JA; Lamb, HM; Onrust, SV, 1998
)
1.96
"Ocular bioavailability of ofloxacin in aqueous humor after oral and topical administration is similar when the drug is applied as described."( Penetration of ofloxacin in human aqueous and vitreous humors following oral and topical administration.
Basci, NE; Batman, C; Bozkurt, A; Cekic, O; Kayaalp, SO; Yasar, U, 1998
)
0.95
" When given orally, bioavailability is greater than 99%, and the drug is highly concentrated in lung tissue and macrophages."( Levofloxacin in the treatment of community acquired pneumonia.
File, TM,
)
0.75
"Median volume of distribution at steady state/systemic bioavailability (V(ss)/F) was significantly smaller in women than in men, although when normalized for total body weight there were no differences."( Effect of gender on the pharmacokinetics of ofloxacin.
Abel, SR; Clark, WR; Mueller, BA; Sowinski, KM, 1999
)
0.56
" It was demonstrated that S/P is a function of the quotient of the rate of absorption and venous plasma drug concentration."( Kinetics of 4-fluoroquinolones permeation into saliva.
Antolic, G; Grabnar, I; Kozjek, F; Mrhar, A; Suturkova, LJ, 1999
)
0.3
"Ocular bioavailability of ofloxacin in SRF after oral and combined administration is equivalent."( Penetration of topical, oral, and combined administered ofloxacin into the subretinal fluid.
Basci, NE; Batman, C; Bozkurt, A; Cekiç, O; Kayaalp, SO; Totan, Y; Yasar, U; Zilelioglu, O, 1999
)
0.85
"Metal ions, which are present in ocular fluids, can significantly decrease the bioavailability of fluoroquinolones."( Effect of two balanced salt solutions on the bioavailability of ofloxacin and ciprofloxacin.
Osato, MS,
)
0.37
"Previous studies have demonstrated a significant reduction in the oral bioavailability of trovafloxacin and ciprofloxacin when administered concomitantly with an intravenous opiate such as morphine."( Lack of interaction between levofloxacin and oxycodone: pharmacokinetics and drug disposition.
Fitzgerald, JF; Grant, EM; Nicolau, DP; Nightingale, C; Quintiliani, R; Zhong, M, 2001
)
0.81
" Bioavailability increase has been ascribed to PEO mucoadhesion and/or increased tear fluid viscosity."( Gel-forming erodible inserts for ocular controlled delivery of ofloxacin.
Burgalassi, S; Chetoni, P; Di Colo, G; Fiaschi, MP; Saettone, MF; Zambito, Y, 2001
)
0.55
"The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid precorneal elimination of the drug may be overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergo a sol-gel transition in the cul-de-sac."( Sustained ophthalmic delivery of ofloxacin from a pH triggered in situ gelling system.
Amin, PD; Cardoza, RM; Srividya, B, 2001
)
0.59
"Levofloxacin, a broad-spectrum fluoroquinolone, may enhance digoxin bioavailability by eliminating intestinal flora that metabolize digoxin."( Absence of a pharmacokinetic interaction between digoxin and levofloxacin.
Chien, SC; Chow, AT; Natarajan, J; Rogge, MC; Williams, RR; Wong, F, 2002
)
1.17
"The purpose of this study was to clarify the contribution of P-glycoprotein to the bioavailability and intestinal secretion of grepafloxacin and levofloxacin in vivo."( Pharmacokinetic role of P-glycoprotein in oral bioavailability and intestinal secretion of grepafloxacin in vivo.
Inui, K; Saito, H; Yamaguchi, H; Yano, I, 2002
)
0.51
"When topical controlled delivery of ophthalmic drugs is realised via erodible inserts, drug bioavailability is maximised, if release is controlled exclusively by insert erosion, since parallel mechanisms which increase the release rate, also increases the dose fraction cleared from the precorneal area by tear fluid draining."( A study of release mechanisms of different ophthalmic drugs from erodible ocular inserts based on poly(ethylene oxide).
Di Colo, G; Zambito, Y, 2002
)
0.31
" Orally administered levofloxacin appears to be well absorbed in selected ICU patients and has pharmacokinetics similar to those of intravenously administered levofloxacin."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.88
" The almost complete (> or =99%) absolute oral bioavailability suggests that a comparable exposure to the iv regimen may be achieved after oral administration."( Pharmacokinetic aspects of levofloxacin 500 mg once daily during sequential intravenous/oral therapy in patients with lower respiratory tract infections.
Brollo, L; Di Qual, E; Dolcet, F; Furlanut, M; Lugatti, E; Pea, F; Talmassons, G, 2003
)
0.61
" The PF-metabolizing activity of intestinal bacteria was reduced to 16% and 33% of normal levels by treatment with AMPC-MET and ofloxacin, respectively, which caused alterations of that degree in the extent of absorption of PF and PM-I, but did not affect their rate of absorption or elimination."( Influence of co-administered antibiotics on the pharmacokinetic fate in rats of paeoniflorin and its active metabolite paeonimetabolin-I from Shaoyao-Gancao-tang.
Akao, T; He, JX; Tani, T, 2003
)
0.52
" Since garenoxacin appeared to be well absorbed following oral administration and concentrations in cartilage tended to be higher than those in plasma, it is unlikely that the low chondrotoxicity in comparison with other quinolones is explained by differences in the pharmacokinetics of these compounds."( Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats.
Baumann-Wilschke, I; Bello, A; Kastner, M; Rahm, U; Stahlmann, R, 2004
)
0.32
" The bioavailability of ofloxacin was 6 times that of ciprofloxacin."( [Aqueous humor penetration of topically applied ofloxacin, ciprofloxacin and tobramycin].
Wu, XD; Yang, YH; Yao, K; Zhang, Z, 2003
)
0.88
" Consequently, the residence time at concentrations higher than the MIC90 and the bioavailability of the antibiotic in the aqueous were increased by about 150 and 240%, respectively, with respect to the reference vehicle."( Effect of chitosan and of N-carboxymethylchitosan on intraocular penetration of topically applied ofloxacin.
Burgalassi, S; Di Colo, G; Nardini, I; Saettone, MF; Zambito, Y, 2004
)
0.54
"Cisplatin-induced ARF differentially modulated the bioavailability and intestinal secretion of quinolones in rats."( Effect of cisplatin-induced acute renal failure on bioavailability and intestinal secretion of quinolone antibacterial drugs in rats.
Inui, K; Saito, H; Yamaguchi, H; Yano, I, 2004
)
0.32
"After the completion of the treatment course, the negative sputum conversion rate in V+D+M treatment protocol group was 84%, significantly higher than that in the control group (42%); the former group showed a focal absorption rate and pulmonary cavity closure rate of 83% and 66%, which were 33% and 26% respectively in the latter."( [Short-term effect of treatment protocol utilizing levofloxacin, pasiniazide and M. Vaccae on multi- drug resistant pulmonary tuberculosis].
Li, SM; Xing, BC; Zheng, XM, 2004
)
0.57
"Levofloxacin has a high bioavailability and a broad antibacterial spectrum which covers the common pathogens found in acute and chronic diabetic foot infections."( Tissue and serum levofloxacin concentrations in diabetic foot infection patients.
Baertsch, U; Born, B; Geiss, HK; Hamann, A; Hoppe-Tichy, T; Kusterer, K; Oberdorfer, K; Swoboda, S; von Baum, H, 2004
)
1.27
" The bioavailability was high (86."( Pharmacokinetics of levofloxacin after single intravenous and repeat oral administration to cats.
Albarellos, GA; Ambros, LA; Landoni, MF, 2005
)
0.64
" The possible roles of small intestinal P-glycoprotein (P-gp) and cytochrome P450 (CYP) in the bioavailability of ofloxacin were also evaluated."( Effects of hepatic fibrosis on ofloxacin pharmacokinetics in rats.
Chen, M; Hu, XL; Liao, ZX; Wang, H, 2006
)
0.83
"Sustained release (SR)-gastroretentive dosage forms (GRDF) enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improve the bioavailability of medications that are characterized by a narrow absorption window."( Development of sustained release gastroretentive drug delivery system for ofloxacin: in vitro and in vivo evaluation.
Chaudhari, S; Chavanpatil, M; Jain, P; Shear, R; Vavia, P, 2005
)
0.56
" By the antibacterial activity and bioavailability sodium furasidin is advantages among the nitrofurans."( [Results of the study on antibiotic resistance emergence among pathogens of community-acquired urinary tract infections in Moscow. Phase I].
Ivanov, DV; Sidorenko, SV, 2005
)
0.33
" We conclude that Bcrp1 is one of the determinants for the bioavailability of fluoroquinolones and their secretion into the milk."( Breast cancer resistance protein (BCRP/ABCG2) transports fluoroquinolone antibiotics and affects their oral availability, pharmacokinetics, and milk secretion.
Alvarez, AI; Merino, G; Molina, AJ; Prieto, JG; Pulido, MM; Schinkel, AH, 2006
)
0.33
"Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window."( Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin.
Chaudhari, S; Chavanpatil, MD; Jain, P; Shear, R; Vavia, PR, 2006
)
0.55
" The oral bioavailability of ofloxacin was 110."( Pharmacokinetics of ofloxacin in broiler chicken.
Kalaiselvi, L; Mathuram, LN; Ramesh, S; Sriram, P; Sriranjani, D, 2006
)
0.95
" The oral bioavailability of levofloxacin is over 99%, enabling simple switching from intravenous to oral therapy during treatment."( Respiratory tract infections: at-risk patients, who are they? Implications for their management with levofloxacin.
Cantón, R; Graninger, W; Lode, H; Milkovich, G, 2006
)
0.83
" Rapid absorption of the drug was also evident by the high value of the absorption rate constant (2."( Pharmacokinetics, urinary excretion and dosage regimen of levofloxacin following a single intramuscular administration in cross bred calves.
Dumka, VK; Srivastava, AK, 2006
)
0.58
" The high bioavailability of levofloxacin allows for rapid step-down from intravenous administration to oral therapy, minimizing unnecessary hospitalization, which may decrease costs and improve patient quality of life."( Levofloxacin for the treatment of community-acquired pneumonia.
File, TM; Lynch, JP; Zhanel, GG, 2006
)
1.24
"In these 2 trials in a selected group of healthy adult male and female volunteers, the ER and IR formulations of ofloxacin displayed a similar rate and extent of bioavailability and comparable safety profiles."( Two open-label, randomized, crossover studies assessing the bioequivalence of ofloxacin administered as immediate-and extended-release formulations in healthy subjects.
Badri, N; Di Spirito, M; DiMarco, M; Ducharme, MP; Marier, JF; Monif, T; Morelli, G; Rampal, A; Tippabhotla, SK, 2006
)
0.77
" However, no published data is available regarding the combined pharmacokinetics and bioavailability of this particular fixed dose combination."( Bioequivalence study of a fixed dose combination of nitazoxanide and ofloxacin in Indian healthy volunteers.
Agarwal, S; Chattaraj, TK; Ghosh, D; Gowda, KV; Pal, TK; Sarkar, AK; Selvan, PS; Solomon, WD, 2007
)
0.57
"Fluoroquinolones are the most commonly used prophylactic antimicrobials for ultrasound-guided transrectal prostate biopsy due to their broad pathogen spectrum, pharmacokinetics, bioavailability and ease of oral administration."( Levofloxacin resistant Escherichia coli sepsis following an ultrasound-guided transrectal prostate biopsy: report of four cases and review of the literature.
Fujisawa, M; Miura, T; Nakano, Y; Shigemura, K; Takenaka, A; Tanaka, K, 2008
)
0.97
"Therapeutic activity, pharmacokinetic and bioavailability on animals (inbred white mouse, rabbits) were evaluated for Ofloxacin-PhPO and Pefloxacin-genova in comparison with innovator products--Tarivid and Abaktal."( [Chemotherapy activity and pharmacokinetics of the fluoroquinolones generics Ofloxacin-PhPO and Pefloxacin-genova].
Bobrov, VI; Borisov, MM; Ptitsina, SN, 2007
)
0.78
" In the bioavailability study, the principal pharmacokinetic parameters showed there were differences between the sustained release pellets and the conventional ofloxacin capsules."( In vitro and in vivo evaluation of ofloxacin sustained release pellets.
Cui, Y; Tang, X; Zhang, Y, 2008
)
0.82
" The bioavailability was high (91."( Characterization of the pharmacokinetic disposition of levofloxacin in stallions after intravenous and intramuscular administration.
Abd El-Aty, AM; Abo El-Sooud, K; Goudah, A; Shim, JH; Shin, HC, 2008
)
0.59
"The poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug may be overcome by the use of in situ gel forming systems that are instilled as drops into the eye and then undergo a sol-gel transition in the cul-de-sac."( Sustained ophthalmic delivery of ofloxacin from an ion-activated in situ gelling system.
Abraham, S; Basavaraj, BV; Bharath, S; Deveswaran, R; Furtado, S; Madhavan, V, 2009
)
0.63
"The fluoroquinolones are currently enjoying extensive worldwide clinical applications because of their good bioavailability and pharmacokinetic profile."( Gender differences on bioavailabity of ofloxacin.
Naseer, R; Riffat, S,
)
0.4
"In Pakistan where the use of antibiotics is more frequent by the general practitioners it is important to elucidate certain dose parameters it is also noticed that side effects are more in females than males so present study is conducted to calculate any differences in bioavailability on the basis of sex."( Gender differences on bioavailabity of ofloxacin.
Naseer, R; Riffat, S,
)
0.4
" Although generic formulations of oral levofloxacin are marketed in Mexico, a literature search did not identify published data concerning the bioavailability of these formulations; these data would be relevant to secure marketing of a test formulation in Mexico."( Bioavailability of two oral formulations of a single dose of levofloxacin 500 mg: an open-label, randomized, two-period crossover comparison in healthy Mexican volunteers.
Burke-Fraga, V; Cariño, L; Fuentes-Fuentes, E; Galan-Herrera, JF; Namur, S; Parra, MG; Poo, JL; Rosales-Sanchez, O, 2009
)
0.86
"The aim of this study was to compare the bioavailability and determine the bioequivalence of a test formulation (an oral tablet containing levofloxacin 500 mg) with its corresponding listed reference-drug formulation in Mexico (a list issued by Mexican Health Authorities)."( Bioavailability of two oral formulations of a single dose of levofloxacin 500 mg: an open-label, randomized, two-period crossover comparison in healthy Mexican volunteers.
Burke-Fraga, V; Cariño, L; Fuentes-Fuentes, E; Galan-Herrera, JF; Namur, S; Parra, MG; Poo, JL; Rosales-Sanchez, O, 2009
)
0.79
" These "in combo" PAMPA data were used to predict the human absolute bioavailability of the ampholytes."( The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
Avdeef, A; Sun, N; Tam, KY; Tsinman, O, 2010
)
0.36
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"Present study was undertaken to evaluate the effect of binders on the bioavailability of the drug."( The effect of binders on the bioavailability of ofloxacin tablets in animal model.
Ahmad, M; Akhtar, N; Khan, HM; Murtaza, G; Rasool, F,
)
0.39
"To reduce the frequency of administration and improve patient compliance, novel levofloxacin sustained-release capsules with suitable in vitro release profiles and good bioavailability were developed."( In vitro and in vivo evaluation of levofloxacin sustained-release capsules.
Huang, SJ; Jiang, SG; Pei, ZQ; Yin, LF; Zhang, Q; Zhao, CJ, 2011
)
0.87
" Unsuccessful in vivo-in vitro correlation was shown in Eudragit® NE30D-coated pellets with a relative bioavailability of only 41."( In vitro and in vivo evaluation of levofloxacin sustained-release capsules.
Huang, SJ; Jiang, SG; Pei, ZQ; Yin, LF; Zhang, Q; Zhao, CJ, 2011
)
0.64
"To assess the feasibility of delivering ofloxacin across the intact tympanic membrane; to compare middle ear bioavailability of ofloxacin after otic and systemic administrations; to determine distribution of otically delivered ofloxacin to other tissues."( Comparison of systemic and otic administration of ofloxacin.
Koulich, E; Pawlowski, KS; Roland, PS, 2010
)
0.88
" This paper is an attempt to compare the bioavailability of two levofloxacin tablet formulations (reference and test) containing 500 mg of levofloxacin."( Bioequivalence study of levofloxacin tablets in healthy Indian volunteers using HPLC.
Chakrabarty, US; Das, A; Dey, G; Mukherjee, J; Nandi, U; Pal, TK; Sahoo, BK; Sarkar, AK, 2011
)
0.9
" In therapy of chronic diseases exacerbations of the respiratory tract, including community-acquired pneumonia, a high oral bioavailability allows to switch from intravenous to oral way of treatment."( [Levofloxacin and other fluoroquinolones in therapy of respiratory tract infections].
Płusa, T, 2011
)
0.93
"In this study levofloxacin, which is completely absorbed and primarily eliminated renally without modification, showed better pharmacokinetic proportionality than cyclosporine, which is poorly absorbed and extensively metabolized."( Assessment of pharmacokinetic proportionality of levofloxacin and cyclosporine over a 100-fold dose range in healthy human volunteers.
Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yu, KS, 2012
)
0.97
" The floating pellets were evaluated for SEM, floating characteristic parameters, in vitro release and bioavailability in New Zealand rabbits."( A floating multiparticulate system for ofloxacin based on a multilayer structure: In vitro and in vivo evaluation.
He, H; Lin, X; Liu, Z; Tang, J; Tang, X; Tao, X; Xu, M; Zhang, C; Zhang, Y, 2012
)
0.65
" Levofloxacin demonstrates good safety, bioavailability and tissue penetration, thus maintaining adequate concentrations at the site of infection."( Levofloxacin for the treatment of respiratory tract infections.
Liapikou, A; Torres, A, 2012
)
1.56
" Its improved bioavailability and safety profile makes the possibility of shorter hospital stays a reality."( Levofloxacin for the treatment of respiratory tract infections.
Liapikou, A; Torres, A, 2012
)
1
" Mean residence time (MRT), mean absorption time (MAT) and bioavailability were 4·26 h, 1·54 h and 69·01%, respectively."( Pharmacokinetics of levofloxacin in Japanese quails (Coturnix japonica) following intravenous and oral administration.
Aboubakr, M, 2012
)
0.69
"In recent years, many pharmaceutical scientists have focused on developing the in situ gel-forming systems to overcome the poor bioavailability and therapeutic response exhibited by conventional ophthalmic solutions due to rapid pre-corneal elimination of the drug."( Comparison of systemic absorption between ofloxacin ophthalmic in situ gels and ofloxacin conventional ophthalmic solutions administration to rabbit eyes by HPLC-MS/MS.
Fan, L; Li, J; Li, L; Li, N; Liu, Z; Ma, L; Okeke, CI; Pang, X; Pi, J; Sun, J; Wang, M; Wu, T; Yin, Z; Zhang, L; Zhang, Q; Zhang, R; Zhao, H; Zhuang, P, 2013
)
0.65
" NXC reduced the extent and rate of absorption of RIF."( Effect of ofloxacin and norfloxacin on rifampicin pharmacokinetics in man.
Barikpoar, E; Brown, S; Ezejiofor, NA; Orisakwe, OE,
)
0.53
" The designed ofloxacin niosomes with span 60 showed good physicochemical properties, good stability, improved pharmacokinetic parameters, prolonged action and improved bioavailability than the commercially available conventional dosage form which might be a potential carrier system to improve the patient compliance and reduce the side effects."( Design and characterization of ofloxacin niosomes.
Balasundaram, J; Dhandayuthapani, B; Natesan, G; Natesan, S; Perumal, P; Ramalingam, N, 2013
)
1.04
" The bioavailability indices of INH in the saliva and plasma were similar in all the groups."( Isoniazid Pharmacokinetics in the Presence of Ofloxacin and Norfloxacin Antibiotics.
Anusiem, CA; Barikpoar, E; Brown, SA; Ezejiofor, NA; Orisakwe, OE,
)
0.39
" Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability."( Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Achar, V; Arora, U; Awasthy, D; Bharath, S; Bheemarao, U; Chinnapattu, M; Coulson, M; de Sousa, SM; Ganguly, S; Gaonkar, S; Ghosh, A; Hameed P, S; Hoffner, S; Humnabadkar, V; Kaur, P; Kumar K N, M; Kumar, CN; Madhavapeddi, P; Manjrekar, P; Menasinakai, S; Mukherjee, K; Nandishaiah, R; Narayan, C; Panduga, V; Patil, V; Puttur, J; Raichurkar, A; Ramya, VK; Reddy, J; Rudrapatana, S; Sambandamurthy, VK; Shanbhag, G; Sharma, S; Sharma, U; Shinde, V; Solapure, S; Waterson, D; Werngren, J, 2014
)
0.4
" It is determined that bioavailability of ofloxacin in the niosomal form is 154% relative to the free form of the antibiotic."( [Comparative study of pharmacokinetics of ofloxacin in a free and niosomal forms in experiments on white mice when administered per os].
Kovalev, DA; Kulichenko, AN; Liapustina, LV; Mikhaĭlova, ME; Pisarenko, SV; Siritsa, IuV, 2014
)
0.93
"The aim of the study was to improve corneal penetration and bioavailability of ofloxacin (OFX) eye preparations."( Improved corneal bioavailability of ofloxacin: biodegradable microsphere-loaded ion-activated in situ gel delivery system.
Ahmed, OA; Hussein, AK; Khaled, KA; Sayed, EG, 2015
)
0.92
" In addition, the oral bioavailability experiment in New Zealand rabbits showed that, the relative bioavailability of the ofloxacin after administrated of floating tablets was 172."( Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.
Chen, H; Ma, N; Qi, X; Rui, Y; Wu, Z; Yang, F, 2015
)
0.89
"The purpose of this investigation is to formulate a gastroretentive sustained drug release system for ofloxacin to improve its retention time, pharmacological activity, bioavailability and therapeutic efficacy in the stomach."( Ofloxacin loaded gellan/PVA nanofibers - Synthesis, characterization and evaluation of their gastroretentive/mucoadhesive drug delivery potential.
Nagar, H; Pruthi, V; Raghuwanshi, N; Singh, H; Srivastava, AK; Vashisth, P, 2017
)
2.11
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Currently, conjunctivitis is treated using ofloxacin eye drop solution, which shows low bioavailability and patient non-compliance."( Ofloxacin laden microemulsion contact lens to treat conjunctivitis.
Huang, C; Li, Y; Yang, X; Zhang, X, 2020
)
2.26
"Currently, bacterial conjunctivitis is managed by multiple antibiotic eye-drop solution, which is highly inefficient due to low ocular bioavailability and frequent dosing."( Ofloxacin-Loaded Niosome-Laden Contact Lens: Improved Properties of Biomaterial for Ocular Drug Delivery.
Liu, J; Wang, X, 2021
)
2.06

Dosage Studied

The pharmacokinetics of levofloxacin, administered in high doses and with extended dosing intervals, was studied in human immunodeficiency virus (HIV)-infected patients. The resulting efficacy for different strains of bacteria suggested that for less sensitive pathogens, a dosage adjustment may be needed.

ExcerptRelevanceReference
" However, the prolonged half-life and enhanced tissue penetration of azithromycin should allow for less frequent dosing and shorter duration of therapy than with erythromycin or clarithromycin."( In vitro activities of azithromycin, clarithromycin, L-ofloxacin, and other antibiotics against Chlamydia pneumoniae.
Hammerschlag, MR; Qumei, KK; Roblin, PM, 1992
)
0.53
" The trough SBAs of the 4 fluoroquinolones suggest that the time interval of administration of CPLX and OFLX should be more than 8 hours, but increase of the dosage or shortening of the time interval between the administrations is recommended for ENX and NFLX."( Comparison of serum bactericidal activity of 4 fluoroquinolones in healthy volunteers.
Liu, YN; Sun, XD; Wang, R; Zhao, HZ, 1992
)
0.28
"The human scalp hair is a useful tissue that retains the past dosage history over a rather long period of time, acting like a "tape-recorder"."( [Establishment of a method to analyze drugs in the hair and its application for determining patient compliance].
Uematsu, T, 1992
)
0.28
" It is concluded that in patients on regular haemodialysis treatment the dosage adjustment employed resulted in safe and therapeutically favourable plasma concentrations."( Multiple dose kinetics of ofloxacin and ofloxacin metabolites in haemodialysis patients.
Borner, K; Kampf, D; Pustelnik, A, 1992
)
0.58
" In comparison with other available quinolones, elimination is more highly dependent on renal clearance, which may lead to more frequent dosage adjustments in patients with impaired renal function."( Ofloxacin clinical pharmacokinetics.
Bailey, EM; Lamp, KC; Rybak, MJ, 1992
)
1.73
" Serial blood samples obtained throughout dosing were assayed for drug concentrations using high-performance liquid chromatography."( Use of nonlinear, mixed-effects modeling for population analysis of ofloxacin: effects of age on oral drug pharmacokinetics.
Brooks, J; Drusano, GL; Flor, S; Yuen, GJ, 1992
)
0.52
"13 ng/ml) after 10 1/2 days of topical dosing were more than 1,000 times lower than those reported after standard oral doses of 300 mg ofloxacin."( Ofloxacin in human serum, urine, and tear film after topical application.
Borrmann, L; Frank, J; Kann, J; Lin, ET; Nista, J; Tang-Liu, DD, 1992
)
1.93
" Although treatment with each quinolone or fenbufen alone at a dosage level tested in mice showed no changes, coadministration of a large dose of all quinolones and fenbufen caused convulsant death."( Interaction of the new quinolone antibacterial agent levofloxacin with fenbufen in mice.
Akahane, K; Furuhama, K; Takayama, S; Tawara, K, 1992
)
0.53
" tuberculosis H37Rv strain, the minimal effective dosage of sparfloxacin, as assessed by survival rate, spleen enlargement and gross lung lesions, was 12."( In vitro and in vivo activities of sparfloxacin (AT-4140) against Mycobacterium tuberculosis.
Grosset, J; Ji, B; Truffot-Pernot, C, 1991
)
0.28
" every 6 h for one day only, while 4 patients with acute peritonitis were treated with this same dosage every 4 h for 3 days, then every 6 h for the next 7 days."( Multiple-dose-kinetics of ofloxacin after intraperitoneal application in CAPD patients.
Borner, K; Conrad, W; Hain, H; Kampf, D, 1991
)
0.58
" The other pharmacokinetic parameters were similar between the two dosage formulations."( Bioavailability and pharmacokinetics of oral ofloxacin formulations in normal subjects.
Flor, SC; LeBel, M; Stein, GE; Zinny, M, 1991
)
0.54
" A proposed protocol for ofloxacin dosage adjustment in chronic renal failure is reported which differs slightly but significantly from that recommended by the manufacturer."( Ofloxacin pharmacokinetics in chronic renal failure and dialysis.
Lameire, N; Lehr, KH; Malerczyk, V; Ringoir, S; Rosenkranz, B; Veys, N, 1991
)
2.03
" three times daily with dosage adjustment according to renal function and body weight (group 2)."( Empiric treatment of serious infections in patients with cancer: randomised comparison of two combinations.
Maiche, AG; Teerenhovi, L, 1991
)
0.28
" The daily dosage was 400 mg to 600 mg, divided into two times."( [Clinical effect and laboratory observation of ofloxacin in the treatment of typhoid fever, bacillary dysentery and gonorrhea].
Jiang, YF; Wang, QN; Zou, QY, 1991
)
0.54
" An extended dosing interval of 24-48 h is recommended, depending upon the degree of renal impairment, when creatinine clearance falls below 50 mL/min."( Pharmacokinetics of ofloxacin in healthy subjects and patients with varying degrees of renal impairment.
Flor, S; Guay, D; Matzke, G; Opsahl, J; Tack, K, 1991
)
0.6
" Ofloxacin was dosed at 400 mg twice daily over a 10-day course of treatment."( Safety of multiple doses of ofloxacin in healthy volunteers.
Beals, BS; Flor, SC; Stein, GE, 1991
)
1.49
" In summary, a once-daily dosing regimen of amikacin 15 mg/kg is practical and probably efficacious and safe in severely infected patients."( Clinical and bacteriological efficacy, and practical aspects of amikacin given once daily for severe infections.
Beaucaire, G; Beuscart, C; Caillaux, M; Chidiac, C; Karp, P; Leroy, O, 1991
)
0.28
" Only in one subject the dosage history could not be deduced from the drug distribution along hair length."( The measurement of ofloxacin in hair as an index of exposure.
Miyazawa, N; Nakashima, M; Uematsu, T, 1991
)
0.61
" Since the AUC in mice treated with ofloxacin 150 mg/kg daily is close to that in man treated with a clinically tolerated dose--600 mg daily--such a dosage may be only moderately effective against human tuberculosis."( Activities of pefloxacin and ofloxacin against mycobacteria: in vitro and mouse experiments.
Grosset, J; Ji, B; Truffot-Pernot, C, 1991
)
0.85
" Ofloxacin has favorable pharmacokinetics with almost 100% bioavailability; peak serum concentrations obtained one to two hours following oral dosing are higher than those achieved with ciprofloxacin."( Ofloxacin.
Scheld, WM; Tunkel, AR, 1991
)
2.63
" The bioavailability (F) of the oral dosage form of ofloxacin was virtually identical to that of the intravenous form (F = 105% +/- 7%)."( Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers.
Nightingale, CH; Quintiliani, R; Sweeney, KR; Yuk, JH, 1991
)
0.8
"In order to reduce the dosage of aminoglycoside in the treatment of patients with complicated urinary tract infections (UTI) in outpatient clinics and to improve cost benefits, we tried both ofloxacin (OFX) treatment and a combination treatment with OFX and a single dose of aminoglycoside (isepamicin)."( Treatment of complicated urinary tract infections with ofloxacin following an aminoglycoside.
Eto, K; Ishii, T; Kumazawa, J; Matsumoto, T; Saito, Y; Sawae, Y; Ueda, S; Yushita, Y, 1991
)
0.72
" The study revealed that concentrations of ofloxacin in serum, bile fluid, and gallbladder tissue after intravenous dosing were adequate against susceptible organisms found in the biliary tract."( Intraoperative concentrations of ofloxacin in serum, bile fluid, and gallbladder wall tissue.
Appleman, MD; Berne, TV; Chin, A; Gill, MA; Heseltine, PN; Okamoto, MP; Sclar, DA; Yellin, AE, 1990
)
0.82
" Dosage adjustments are required, particularly in severe renal failure and for the drugs almost exclusively excreted, in unchanged form, via the renal route."( Pharmacokinetics of quinolones in renal insufficiency.
Borsa-Lebas, F; Dhib, M; Fillastre, JP; Humbert, G; Leroy, A; Moulin, B, 1990
)
0.28
"Antibiotic therapy is directed against bacteria responsible for infectious pathology which are able to resist treatment mainly when the dosage is misadapted."( A new approach to optimal antibiotic dosage regimen by coupling pharmacokinetics and killing curve parameters.
Dellamonica, P; Drugeon, HB; Etesse, H; Garraffo, R; Lapalus, P, 1990
)
0.28
" After a six weeks observation and treatment period, where Ofloxacin was dosed with 20 mg/kg body weight daily with a stomach tube, the animals were sacrificed and their lenses used for biochemical analyses."( Evaluation of a possible cocataractogenic potential of Ofloxacin.
Hockwin, O; Kuhn, UD; Lorenz, M; Wegener, A, 1990
)
0.77
" Single oral dosing of 20 mg/kg of either ofloxacin or ciprofloxacin showed that ofloxacin achieves approximately a four-fold higher peak serum or liver concentration than ciprofloxacin, which may contribute to its better efficacy in this infection model."( In-vivo evaluation of ofloxacin in Salmonella typhimurium infection in mice.
Fu, KP; Hilliard, J; Isaacson, D; McGuire, JL; Rosenthale, ME; Tobia, AJ, 1990
)
0.86
" In a multicenter study in seven Asian countries, 105 mal patients with chlamydial urethritis and 46 male patients with nongonococcal and nonchlamydial urethritis were treated with oral ofloxacin at a dosage of 200 mg twice daily for 5 to 10 days."( Ofloxacin treatment of nongonococcal urethritis. A multi-center study in Asia.
Chang, LS; Daili, SF; Kawada, Y; Lai, C; Lee, JM; Limson, BM; Polnikorn, N; Saito, I, 1990
)
1.91
"Ofloxacin was administered orally at a daily dosage of 300 mg and 600 mg in three divided doses for 14 days to 24 and 60 patients with chronic complicated urinary infections, respectively, in order to evaluate the therapeutic efficacy."( [Clinical evaluation of ofloxacin in the treatment of chronic complicated urinary tract infection].
Hisazumi, H; Kobashi, K; Koizumi, H; Motoi, I; Nagano, K; Nishino, A; Orito, M; Sawaki, M; Shyoda, R; Uchibayashi, T, 1990
)
2.03
" Since no relationship between ofloxacin or pefloxacin kinetics and the usual liver function tests was found, recommended dosage regimens in cirrhotic patients have to be controlled by monitoring plasma drug levels during treatment."( Pharmacokinetics of fluoroquinolones in hepatic failure.
Gaillot, J; Montay, G, 1990
)
0.57
" Dosage adjustment was made for patients in renal failure."( Efficacy of intravenous ofloxacin: a French multicentre trial in 185 patients.
Beaucaire, G; Beuscart, C; Chidiac, C; Leroy, O; Mouton, Y; Senneville, E; Sivery, B; Vincent du Laurier, M, 1990
)
0.59
"A study was made of the plasma and distribution kinetics of ofloxacin administered at a dosage of 400 mg orally to a group of healthy volunteers and a group of patients with renal impairment."( Effect of renal impairment on distribution of ofloxacin.
Domínguez-Gil Hurlé, A; Gomez Sanchez, JC; Martinez Lanao, J; Sanchez Navarro, A; Sanchez Recio, MM; Tabernero Romo, JM; Terreiro Delgado, MM, 1990
)
0.78
" The proposed dosing regimen could be an adequate therapy of peritonitis and exit-site infections in patients on CAPD since levels reached in the dialysate effluent are bactericidal."( Single- and multiple-dose kinetics of ofloxacin in patients on continuous ambulatory peritoneal dialysis (CAPD).
Essers, L; Grabensee, B; Keller, E; Passlick, J; Wonner, R, 1989
)
0.55
" Serum and milk samples were obtained simultaneously at two, four, six, nine, 12, and 24 hours after dosage administration."( Pharmacokinetics of three newer quinolones in pregnant and lactating women.
Aravantinos, D; Gazis, J; Giamarellou, H; Kolokythas, E; Petrikkos, G; Sfikakis, P, 1989
)
0.28
" 64 patients were treated with ofloxacin and 11 with amikacin, dosage regimens of the two drugs were 300 mg and 300-400 mg twice daily."( [Efficacy of ofloxacin in treating typhoid fever].
Gu, XJ; Wang, F; Zhang, MF, 1989
)
0.93
" The pharmacokinetics of the compound indicate that, except for cases of renal impairment, little or no dosage adjustment is necessary."( Pharmacokinetics of ofloxacin. An overview.
Flor, S, 1989
)
0.6
" Dosage of each quinolone was 200 mg twice daily for four days, starting three days prior to the theophylline infusion."( Drug-drug interactions affecting fluoroquinolones.
Guelen, PJ; Janssen, TJ; Vree, TB; Wijnands, GJ, 1989
)
0.28
" The recommendation of some authors that, in general, ofloxacin dosage may be halved in the elderly could not be confirmed."( Pharmacokinetics of a single dose of ofloxacin in healthy elderly subjects using noncompartmental and compartmental models.
Glerum, JH; Jones, RW; Notarianni, LJ; Rademaker, CM; van Dijk, A; Verhoef, J, 1989
)
0.8
"Thirty-four hospitalized patients with various infections: 19 with typhoid fever, 4 with gastroenteritis, 7 with lower respiratory tract infections, 2 with biliary tract infections, 1 with brucellosis and 1 with infection of necrotic ulceration of the feet, were treated with ofloxacin at a daily dosage ranging between 600 and 900 mg orally."( Clinical experience with ofloxacin (DL-8280) in the therapy of various infections.
Altucci, P; Cristiano, P; Iovene, MR; Mandia, L; Morelli, G; Paradisi, F, 1989
)
0.76
" BMY 40062 exhibited longer half-life, higher maximum concentration in serum, greater area under the curve, and better bioavailability in mice after oral dosing than ciprofloxacin."( In vitro and in vivo antibacterial activities of BMY 40062, a new fluoronaphthyridone.
Desiderio, JV; Fung-Tomc, J; Kessler, RE; Tsai, YH; Warr, G, 1989
)
0.47
" The superiority of the triple dosing in chemotherapeutic efficacy of ofloxacin was found to be attributable at least to the longer retention of its pulmonary levels exceeding the antibiotic concentrations."( Chemotherapeutic efficacy of ofloxacin against experimental pneumonia with Pseudomonas aeruginosa in guinea pigs.
Hashimoto, S; Iigo, Y; Ishida, Y; Nakajima, R; Osada, Y; Otani, T; Une, T, 1989
)
0.8
" The data obtained confirm that ofloxacin is active against Chlamydia trachomatis at concentrations achievable with the routine dosage regimen."( In-vitro activity of ofloxacin against Chlamydia trachomatis.
Cevenini, R; Rumpianesi, F; Sambri, V; Xerri, L, 1989
)
0.88
" The therapeutic combination of H2-receptor-antagonists (= H2-RA) and ofloxacin (Tarivid) has shown to heal resistant duodenal ulcers in some preliminary cases, which did not respond to a three month standard dosage treatment with H2-RA."( [Ofloxacin in therapy of "resistant" duodenal ulcer. A pilot study].
Bayerdörffer, E; Kasper, G; Ottenjann, R; Pirlet, T; Sommer, A, 1988
)
1.42
" This study was undertaken at the incubation period, in syphilitic rabbits, using kinetic data obtained in man, after a given dosage of ofloxacin."( [In vivo study of the sensitivity of Treponema pallidum to ofloxacin].
Daubras, M; Ichou, F; Ly, M; Poitevin, M, 1988
)
0.72
" On the basis of these results, a means of determining suitable dosage reduction factors in patients with renal impairment is presented."( Pharmacokinetics of ofloxacin in healthy subjects and patients with impaired renal function.
Höffler, D; Koeppe, P, 1987
)
0.6
" Ofloxacin was administered at a dosage of 600 mg divided into 3 doses for 14 days."( [Studies of clinical efficacy of ofloxacin against male urethritis caused by Chlamydia trachomatis].
Matsuda, T; Okada, K; Yoshida, O, 1988
)
1.47
" These results show that ofloxacin, in a dosage of 300 mg taken orally twice daily for seven days, is an effective treatment for uncomplicated urethritis in men but may not reliably cure chlamydial infections."( A prospective randomized trial of ofloxacin vs. doxycycline in the treatment of uncomplicated male urethritis.
Boslego, JW; Ciak, J; Greenup, R; Hicks, CB; Thomas, RJ; Tramont, EC; Wiener, HA,
)
0.71
" A dosing schedule for the quinolones was proposed on the basis of pharmacokinetic parameters and microbiologic activity."( Pharmacokinetics of the quinolones in volunteers: a proposed dosing schedule.
Andrews, JM; Griggs, D; Wise, R,
)
0.13
" The largest reductions of viable counts in the kidneys at each dosage as compared to the bacterial counts of untreated animals were achieved with coumermycin (3."( Efficacy of coumermycin, ofloxacin and vancomycin against methicillin-resistant Staphylococcus aureus in vitro and in experimental infections of mice.
Breyer, S; Georgopoulos, A; Hirschl, AM; Rotter, ML; Stanek, G, 1988
)
0.58
" Furthermore, there was a broad fluctuation of approximately 80% between the Cmax and Cmin in the plasma levels of the drug during a 12-hour dosing interval."( Pharmacokinetics and tissue distribution of ofloxacin in human subjects during a multiple dose regimen.
Bonaccorsi, S; Carlino, S; De Bernardis, E; Picari, M; Rizza, V, 1988
)
0.54
" Peritoneal effluent ofloxacin levels correlated well with the prevailing serum concentrations of the antibiotic and, except on day 1, the mean peritoneal effluent ofloxacin levels all exceeded 3 mg/l with the second dosing scheme."( Oral treatment of peritonitis in CAPD patients with two dosage regimens of ofloxacin.
Chan, MK; Chan, WW; Chau, PY, 1988
)
0.82
" These results confirm that dosage reduction of ofloxacin is required in haemodialysis patients."( The pharmacokinetics of ofloxacin, desmethyl ofloxacin and ofloxacin N-oxide in haemodialysis patients with end-stage renal failure.
MacGowan, AP; Mackay, IG; Reeves, DS; White, LO, 1988
)
0.84
"3% of ofloxacin after iv dosing could be detected as metabolites in urine."( Comparative pharmacokinetics of intravenous ofloxacin and ciprofloxacin.
Borner, K; Höffken, G; Kirch, A; Koeppe, P; Lode, H; Olschewski, P; Sievers, B, 1988
)
1.02
" Bronchial secretions were aspirated at bronchoscopy between one and 24 h after dosing and blood was collected at the same time."( The penetration of ofloxacin into bronchial secretions.
Bone, M; Javaid, A; Symonds, J; Turner, A, 1988
)
0.6
" A single dosage induced chondrocyte degeneration in the middle zone of the articular cartilage 5 h later and cavity formation 12 and 24 h later."( Effect of ofloxacin on the uptake of [3H]thymidine by articular cartilage cells in the rat.
Kato, M; Onodera, T, 1988
)
0.68
" dosage schedule for enteric fever and UTI due to beta-lactamase-producing bacteria."( In vitro and clinical evaluation of ofloxacin in urinary tract infection and enteric fever.
Srimuang, S; Tanphaichitra, D, 1988
)
0.55
" 667 patients were randomly allocated to 1 of 3 different twice daily dosage regimens: 400 mg (245 patients), 600 mg (211) or 800 mg (211)."( Clinical efficacy of ofloxacin in lower respiratory tract infections. A multicentre study.
Gialdroni Grassi, G; Grassi, C; Mangiarotti, P, 1987
)
0.59
" The dosage of ofloxacin has to be adapted to the stage of chronic renal failure."( [Ofloxacin treatment in nephrologic problem patients with various degrees of chronic renal failure (including dialysis treatment). Preliminary results].
Dörfler, A; Schulz, W, 1986
)
1.53
" Dosage adjustments of ofloxacin in uremic patients are proposed."( Ofloxacin pharmacokinetics in renal failure.
Fillastre, JP; Humbert, G; Leroy, A, 1987
)
2.03
" The authors thus recommend a dosage of 400 mg of ofloxacin three to five hours prior to surgery for middle ear infection."( Tissue concentrations of ofloxacin in the middle ear.
Thorn, V, 1987
)
0.83
" The following ofloxacin dosage regimen is recommended in haemodialysis patients: 200 mg initially, 100 mg loading dose after the first haemodialysis, then 100 mg daily."( Pharmacokinetics of ofloxacin in patients on haemodialysis treatment.
Burkhardt, F; Dörfler, A; Schulz, W; Zichner, M, 1987
)
0.95
"We reviewed, the structure, pharmacokinetic properties, mode of actions, antibacterial spectrum, therapeutic dosage and side effects of fluoroquinolones in this article."( [Fluoroquinolones].
Akalin, E; Baykal, M, 1987
)
0.27
" Each patient had single drug therapy with ofloxacin in a daily dosage of 200 mg taken in the morning on an empty stomach."( [Diffusion of an orally administered single dose of ofloxacin into human bronchial mucus].
Benard, Y; Malbruny, B; Monrocq, N; Morel, C; Vergnaud, M, 1986
)
0.78
"Nine patients with typhoid fever were given ofloxacin in a daily dosage of 400 mg for ten days."( [Treatment of typhoid fever using ofloxacin. Clinical experience and determination of antibiotic diffusion into the mesenteric lymph nodes].
Bru, JP; Croize, J; Fourtillan, JB; Le Noc, P; Leclercq, P; Lefebvre, MA; Micoud, M; Stahl, JP, 1986
)
0.81
" In view of these significant changes in ofloxacin pharmacokinetics found in elderly subjects, we advocate reducing the usual dosage by half."( [Pharmacokinetics of ofloxacin in the elderly (65-85 years) with normal renal function after a single oral dose of 200 mg].
Bryskier, A; Couet, W; Darchis, JP; Fourtillan, JB; Lefebvre, MA; Modai, J; Veyssier, P; Vincent Du Laurier, M, 1986
)
0.86
"Thirteen hospitalized patients with various infections, five with typhoid fever, two with gastroenteritis, four with respiratory tract infection and two with biliary tract infection, were treated with ofloxacin at a daily dosage ranging between 600 and 900 mg orally."( Clinical experience with ofloxacin (DL 8280) in the therapy of various infections: preliminary report.
Altucci, P; Briante, V; Cristiano, P; Leonessa, V; Morelli, G; Paradisi, F, 1986
)
0.76
" We conclude that a single oral dose of ofloxacin in the studied dosage regimens was highly effective and safe in the treatment of uncomplicated gonorrhoea."( Single dose ofloxacin in treatment of uncomplicated gonorrhoea.
Chan, AS; Fung, KK; Ng, TK; Tang, KC, 1986
)
0.92
" Ofloxacin was used at a dosage of 300 mg to 800 mg daily for three to 20 days in 206 cases of various infectious diseases in the otorhinolaryngological field such as otitis media, external otitis, paranasal sinusitis, tonsillitis and pharyngolaryngitis."( Clinical efficacy of ofloxacin in the treatment of otorhinolaryngological infections.
Baba, S, 1986
)
1.5
" It is difficult to generalize their clinical usefulness, since these agents exhibit different pharmacokinetic profiles, antimicrobial activity (with varied minimum inhibitory concentrations among similar organisms), and dosage regimens."( Review of the 4-quinolones.
Eggleston, M; Park, SY, 1987
)
0.27
" In clinical use, the drug was given at a daily dosage of 300-600 mg for 5-21 days."( [Laboratory and clinical study of ofloxacin in the treatment of bacterial prostatitis].
Ando, K; Moriguchi, R; Naide, Y; Suzuki, K; Tamai, H, 1984
)
0.55
" In comparative trials with ofloxacin, levofloxacin, at half the daily dosage of ofloxacin, showed equivalent efficacy and a reduced incidence of adverse effects in the treatment of lower respiratory tract and complicated urinary tract infections."( Levofloxacin. A review of its antibacterial activity, pharmacokinetics and therapeutic efficacy.
Bryson, HM; Davis, R, 1994
)
1.2
" It seems, therefore, that the in vivo activity of LVFX is comparable to that produced by a twofold-greater dosage of OFLO."( In vitro and in vivo activities of levofloxacin against Mycobacterium tuberculosis.
Grosset, J; JI, B; Lounis, N; Truffot-Pernot, C, 1995
)
0.56
" However, the area under the inhibitory serum concentration time-curve (AUIC) may be superior when appropriate dosing intervals are selected."( Role of pharmacokinetics and pharmacodynamics in the design of dosage schedules for 12-h cefotaxime alone and in combination with other antibiotics.
Nix, DE; Schentag, JJ,
)
0.13
" The fluoroquinolones were administered to simulate dosage regimens of 200 mg, 400 mg given intravenously (i."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
0.6
" Population pharmacokinetic parameters are also useful for the individualization of a dosage regimen by means of the Bayesian forecasting method."( Premarketing population pharmacokinetic study of levofloxacin in normal subjects and patients with infectious diseases.
Hori, R; Kagimoto, N; Nomura, H; Okumura, K; Tanigawara, Y, 1995
)
0.54
" Ofloxacin was used primarily to treat tuberculosis (TB), dosed to achieve 2-hour postdose serum concentrations of 8-12 micrograms/ml."( Long-term safety of ofloxacin and ciprofloxacin in the treatment of mycobacterial infections.
Berning, SE; Iseman, MD; Madsen, L; Peloquin, CA, 1995
)
1.52
" Ofloxacin was administered at a dosage of 200 mg three times daily for 7 to 10 days."( Ofloxacin in the treatment of typhoid fever resistant to chloramphenicol and amoxicillin.
Hayat, Z; Khan, MA; Sadick, A,
)
2.48
"Hair samples were obtained 1-5 months after ingestion of the antimicrobial ofloxacin, which had been given for 1 or 3 days at the commencement of haloperidol administration, or when its dosage was reduced."( Using ofloxacin as a time marker in hair analysis for monitoring the dosage history of haloperidol.
Kosuge, K; Nakano, M; Nakashima, M; Nishimoto, M; Sato, H; Uematsu, T, 1994
)
1
" In a dose-response study, treatment with LEV at 100, 200, and 400 mg/kg of body weight was started 1 day after infection and was given daily for 28 days."( Activity of levofloxacin in a murine model of tuberculosis.
Cynamon, MH; Klemens, SP; Rogge, MC; Sharpe, CA, 1994
)
0.64
" Its optimal dosage appears to be 400 mg daily, and combination with dapsone and clofazimine does not enhance its activity."( Clinical trial of ofloxacin alone and in combination with dapsone plus clofazimine for treatment of lepromatous leprosy.
Grosset, JH; Ji, B; N'Deli, L; Perani, EG; Petinom, C, 1994
)
0.62
" Sparfloxacin was more effective than levofloxacin and ofloxacin in both dosing regimens."( In vitro and in vivo activities of sparfloxacin against Mycoplasma pneumoniae.
Irifune, K; Ishida, K; Kaku, M; Mizukane, R; Suyama, N; Takemura, H; Tanaka, H; Tomono, K; Usui, T; Yoshida, R, 1994
)
0.55
" Mean +/- standard deviation levofloxacin pharmacokinetic parameters (by noncompartmental moment method) after multiple dosing were as follows: area under the concentration-time curve, 31."( Pharmacokinetics and safety of levofloxacin in patients with human immunodeficiency virus infection.
Bartlett, JA; Chow, AT; Flor, SC; Gallis, HA; Goodwin, SD; Wong, FA, 1994
)
0.85
"Human scalp hair retains the past dosage history over a rather long period of time, acting as 'tape-recorder'."( Utilization of hair analysis for therapeutic drug monitoring with a special reference to ofloxacin and to nicotine.
Uematsu, T, 1993
)
0.51
" One of five new quinolones was orally administered, before transurethral resection of the prostate, at the dosage of 200 mg three times daily for 3 consecutive days."( Accumulation of new quinolones in the blood of elderly patients.
Abe, Y; Hasuda, A; Morita, M; Nakagawa, H; Suzuki, K,
)
0.13
" Juvenile (4- to 5-week-old) NZW were orally dosed with ofloxacin or pefloxacin (300 mg/kg of body weight for 1 day) or with pefloxacin (300 mg/kg for 7 days)."( Cytofluorometric analysis of chondrotoxicity of fluoroquinolone antimicrobial agents.
Gaudin, C; Hayem, G; Kahn, MF; Levacher, M; Petit, PX; Pocidalo, JJ, 1994
)
0.53
"5 mM) by 20% of the control in the in situ ligated loop experiment, in which partial precipitation of aluminum hydroxide was observed in the dosing solution."( Mechanistic study of inhibition of levofloxacin absorption by aluminum hydroxide.
Aoki, H; Fujisawa, C; Hakusui, H; Kurata, T; Ohshima, Y; Okazaki, O; Tanaka, M, 1993
)
0.56
" Ofloxacin concentrations in plasma were evaluated after 4 days of oral or intravenous (1-h infusion) dosing with a 3-day wash-out period between regimens."( Bioequivalence of oral and intravenous ofloxacin after multiple-dose administration to healthy male volunteers.
Chow, AT; Flor, SC; Rogge, MC, 1993
)
1.47
" These results, together with pharmacokinetic and toxicological data in mice and man, suggest that sparfloxacin may have a higher therapeutic index than ofloxacin in leprosy, and that the tentative standard dosage of 200 mg sparfloxacin daily should be appropriate for a clinical trial."( Sparfloxacin is more bactericidal than ofloxacin against Mycobacterium leprae in mice.
Chan, GP; Franzblau, SG; Parrilla, ML, 1993
)
0.75
" This study was designed to evaluate the additive effect of continuous low dosage or intermittent usual dosage of ofloxacin (OFLX) on EM therapy in patients with sinobronchial syndrome."( Additive effect of continuous low-dose ofloxacin on erythromycin therapy for sinobronchial syndrome.
Fujimura, M; Ishiura, Y; Matsuda, T; Nakatsumi, Y; Nomura, M; Saito, M; Shibata, K, 1995
)
0.77
" Chondrocyte clusters producing glycosaminoglycans were observed 3 weeks after dosing and at later time points."( Quinolone-induced cartilage lesions are not reversible in rats.
Förster, C; Kociok, K; Merker, HJ; Shakibaei, M; Stahlmann, R, 1996
)
0.29
"Effects of intravitreal injection of levofloxacin (LVFX) on the electroretinogram (ERG), visual evoked potential (VEP), and retinal histology were studied in 23 albino and 23 pigmented rabbits to establish the non-toxic intravitreal dosage of LVFX."( [Effects of intravitreal levofloxacin on the rabbit retina].
Kajimura, T; Komatsu, M; Mochizuki, K; Ogata, M; Ohkubo, S; Tanahashi, T; Torisaki, M; Yamashita, Y, 1996
)
0.86
" Dosing modifications and an awareness of possible central nervous system adverse effects are warranted."( Association of a Tourette-like syndrome with ofloxacin.
Reagan, DR; Thomas, RJ, 1996
)
0.55
" However, gastrointestinal adverse events were quite frequent among patients treated with CLARI-MINO, with or without OFLO, and may be attributed to the higher dosage of CLARI or MINO or to the combination of CLARI-MINO plus OFLO."( Bactericidal activity of single dose of clarithromycin plus minocycline, with or without ofloxacin, against Mycobacterium leprae in patients.
Grosset, JH; Jamet, P; Ji, B; Lienhardt, C; Perani, EG; Petinon, C; Sow, S, 1996
)
0.52
" Each dosing was followed by a wash-out period of one week."( Pharmacokinetics of levofloxacin in comparison to the racemic mixture of ofloxacin in man.
Damm, D; Lehr, KH; Malerczyk, V; Verho, M, 1996
)
0.6
" A dose-response analysis showed that levofloxacin was superior to ciprofloxacin for all four isolates at any dose or regimen tested, independent of the methicillin susceptibility of the isolates."( In vivo efficacies of levofloxacin and ciprofloxacin in acute murine hematogenous pyelonephritis induced by methicillin-susceptible and-resistant Staphylococcus aureus strains.
Barrett, JF; Frosco, MB; Kulwich, BA; Licata, L; Melton, JL; Stewart, FP, 1996
)
0.86
" The drug was administered in accordance with 2 regimens: orally in a dose of 400 mg once a day (group I) and intravenously in a dose of 200 mg twice a day for 2 to 4 days followed by the drug oral use in the same dosage for 6 to 8 days (group II)."( [Clinical and pharmacokinetic evaluation of ofloxacin under various regimens of administration in patients with bronchopulmonary infections].
Belousov, OB; Efremenkova, OV; Gutkin, AB; Sokolov, AV; Tishchenkova, IF, 1996
)
0.56
" After that period the drug was used orally in the same dosage for 4 to 6 days."( [Comparative evaluation of the effectiveness of ofloxacin in comprehensive treatment of acute inflammatory diseases of the uterus and uterine appendages].
Denisova, EN; Evseev, AA; Savel'eva, GM, 1996
)
0.55
" For the first 3 to 5 days in the present study ofloxacin was administered in a dose of 200 mg twice a day followed by its oral use in the same dosage for 3 to 5 days."( [Outlook and experience in using ofloxacin in urology].
Derevianko, II; Kotliarova, GA; Siniukhin, VN, 1996
)
0.83
" In group III ofloxacin was used in the same dosage but in combination with some other antibiotics."( [Treatment of Flexner's dysentery with ofloxacin].
Kulikov, VP; Rakhmanova, AG, 1996
)
0.92
" Clinafloxacin at higher dosage (45 mg/kg/d) resulted in a decrease in myeloid progenitors in BM."( Enhanced hematopoiesis in sublethally irradiated mice treated with various quinolones.
Fabian, I; Gruss, T; Kletter, Y; Shalit, I; Weiss, K, 1997
)
0.3
" Test fluoroquinolones were administered orally at 1 h (single dose) or at 1 and 3 h (divided dose) postinfection, with 10 infected mice used for each of six concentrations of each fluoroquinolone tested (1 to 40 mg/kg of body weight) in each dosing regimen."( In vivo oral efficacy of levofloxacin for treatment of systemic Pseudomonas aeruginosa infections in a murine model of septicemia.
Amaratunga, DJ; Barrett, JF; Frosco, MB; Yagel, SK, 1996
)
0.59
" The dosage of prednisolone was increased, and amikacin was injected to treat pneumonia that had developed in the right lung."( [Legionella pneumonia successfully treated despite late diagnosis].
Takazakura, E; Tsuji, H, 1997
)
0.3
" Plasma levofloxacin concentrations were monitored for 36 h after levofloxacin dosing on day 1, immediately prior to the morning doses on days 3 to 9, and for 72 h after dosing on day 10."( Pharmacokinetics and safety of oral levofloxacin in human immunodeficiency virus-infected individuals receiving concomitant zidovudine.
Chien, SC; Chow, AT; Hendrix, CW; Rogge, MC; Williams, RR, 1997
)
0.96
" To verify intraocular penetration, ten rabbits received identical dosing schedules followed by HPLC measurement of aqueous and vitreous drug concentrations at 1, 4, 8, 12, and 24 hours following dose completion."( Retinal safety of oral and topical ofloxacin in rabbits.
Callina, C; Cohen, RG; Lahav, M; Raizman, M, 1997
)
0.57
"To evaluate the levels of ofloxacin (Ocuflox) in human corneal tissue in patients exposed to various dosing regimens and application methods."( Corneal tissue levels of topically applied ofloxacin.
Gonzales, J; Johns, S; Price, FW; Whitson, WE,
)
0.69
" Patients were placed into one of two study groups of 20 each based on dosing regimen and application method."( Corneal tissue levels of topically applied ofloxacin.
Gonzales, J; Johns, S; Price, FW; Whitson, WE,
)
0.39
"Corneal tissue concentrations of Ocuflox were elevated significantly by varying drug application methods and dosing schedules before PKP."( Corneal tissue levels of topically applied ofloxacin.
Gonzales, J; Johns, S; Price, FW; Whitson, WE,
)
0.39
" Levofloxacin at 500 mg or placebo was administered orally or intravenously as a single dose on day 1; daily oral or intravenous dosing resumed on days 4 to 10."( Pharmacokinetic profile of levofloxacin following once-daily 500-milligram oral or intravenous doses.
Cheung, WK; Chien, SC; Chow, AT; Curtin, C; Fowler, CL; Gisclon, LG; Natarajan, J; Rogge, MC; Williams, RR; Wong, F, 1997
)
1.14
" A HPLC method was developed for determination of both antibiotics in ocular aqueous humor and plasma in order to optimize dosage for safe surpassing minimal inhibitory concentration in the humor compartment."( Simultaneous quantification of cefotaxime, desacetylcefotaxime, ofloxacine and ciprofloxacine in ocular aqueous humor and in plasma by high-performance liquid chromatography.
Breithaupt, A; Breithaupt, H; Gehrke, R; Kraemer, HJ, 1997
)
0.54
"5 and 6 h after dosing and the drug was still detectable in plasma 48 h after dosing (0."( Quinolone-induced arthropathy: exposure of magnesium-deficient aged rats or immature rats, mineral concentrations in target tissues and pharmacokinetics.
Förster, C; Günther, T; Lozo, E; Merker, HJ; Schwabe, R; Stahlmann, R; Vormann, J; Zippel, U, 1997
)
0.3
" In study period 1, 750 mg of levofloxacin or a placebo was administered orally as a single dose on day 1, followed by a washout period on days 2 and 3; dosing resumed for days 4 to 10."( Double-blind evaluation of the safety and pharmacokinetics of multiple oral once-daily 750-milligram and 1-gram doses of levofloxacin in healthy volunteers.
Callery-D'Amico, SV; Chien, SC; Chow, AT; Fowler, CL; Nayak, R; Williams, RR; Wong, FA, 1998
)
0.79
" In mouse experiments, the activity of a single dose of the combination OFLO-MINO was dosage related; the higher dosage of the combination displayed bactericidal activity which was significantly inferior to that of a single dose of RMP, whereas the lower dosage did not exhibit a bactericidal effect."( Bactericidal activity of a single-dose combination of ofloxacin plus minocycline, with or without rifampin, against Mycobacterium leprae in mice and in lepromatous patients.
Diderot, V; Grosset, J; Ji, B; Lienhardt, C; Perani, E; Sow, S, 1998
)
0.55
" Dosing regimens were: every 30 min, 60 min, or a single drop applied at 9 h PI."( Effectiveness of ciprofloxacin-polystyrene sulfonate (PSS), ciprofloxacin and ofloxacin in a Staphylococcus keratitis model.
Engel, LS; Green, LC; Hill, JM; Moreau, JM; O'Callaghan, RJ, 1998
)
0.62
" Starting from 10(7) CFU/ml, the bacterial count was determined serially during the exposure to LVFX present at concentrations automatically simulated to its clinically achievable urinary levels at the recommended dosage (100 mg 3 times daily)."( Bactericidal effect of levofloxacin on strains with equal susceptibility in an in vitro urinary bladder model.
Hirose, T; Matsukawa, M; Mikami, M; Nishimura, M; Sano, M; Takahashi, S; Tsukamoto, T,
)
0.43
" We conclude that the type of dialyzer used has to be taken into account in dosage recommendations for antimicrobial therapy in hemodialysis patients."( Ofloxacin clearance during hemodialysis: a comparison of polysulfone and cellulose acetate hemodialyzers.
Burgmann, H; El Menyawi, I; Hörl, WH; Kletzmayr, J; Kovarik, J; Rosenkranz, AR; Thalhammer, F; Traunmüller, F, 1998
)
1.74
" High oral bioavailability allows switching from intravenous to oral therapy without dosage adjustment."( Levofloxacin. Its use in infections of the respiratory tract, skin, soft tissues and urinary tract.
Lamb, HM; Langtry, HD, 1998
)
0.92
" In many cases dose and intervals were based on WHO protocol, however smaller dosage was used in some cases."( [Chemotherapy of Hansen's disease in Japan--present status].
Goto, M; Kitajima, S; Miyagi, S; Takizawa, H, 1998
)
0.3
" Compared with ciprofloxacin and the earlier quinolone agents, levofloxacin has an improved pharmacokinetic profile that allows convenient once-daily dosing in either an oral or parenteral formulation."( Levofloxacin: a therapeutic review.
Garrison, MW; Schoonover, L; Wimer, SM,
)
1.08
" Standard antibiotic dosing regimens which simulated the pharmacokinetic profile observed in humans were used."( Pharmacodynamic comparisons of levofloxacin, ciprofloxacin, and ampicillin against Streptococcus pneumoniae in an in vitro model of infection.
Lacy, MK; Lu, W; Nicolau, DP; Nightingale, CH; Quintiliani, R; Tessier, PR; Xu, X, 1999
)
0.58
"25 mL in children with chronic suppurative otitis media and perforated tympanic membrane, with serial sampling of otorrhea and serum up to 8 hours after dosing and middle ear mucosa up to 2 hours after dosing."( Ofloxacin otic solution in patients with otitis media: an analysis of drug concentrations.
Furuta, S; Katsuda, K; Kiyota, R; Miyazaki, Y; Nobori, T; Ohyama, M; Ueno, K, 1999
)
1.75
" For the 6 bacterial strains isolated from the middle ear, the highest minimum inhibitory concentration of ofloxacin was covered by otorrhea drug concentrations measured at up to 8 hours after dosing in some patients."( Ofloxacin otic solution in patients with otitis media: an analysis of drug concentrations.
Furuta, S; Katsuda, K; Kiyota, R; Miyazaki, Y; Nobori, T; Ohyama, M; Ueno, K, 1999
)
1.96
" aeruginosa with varying quinolone susceptibility, we constructed sigmoidal dose-response curves for AUC(0-6."( The antibacterial efficacy of levofloxacin and ciprofloxacin against Pseudomonas aeruginosa assessed by combining antibiotic exposure and bacterial susceptibility.
Holt, HA; MacGowan, AP; Wootton, M, 1999
)
0.58
" SBA was tested in vitro by a microtitration method 15 min before dosing and at 1, 4, 8 and 12 h after drug absorption."( Levofloxacin: serum bactericidal activity against methicillin-resistant Staphylococcus aureus isolates.
Benoit, C; Bigot, C; Carbon, C; Decré, D; Maubert, B; Muller-Serieys, C, 1999
)
0.92
"The objective of the current study was to evaluate the bactericidal activity of levofloxacin against Streptococcus pneumoniae at concentrations equivalent to those present in serum after a po dosage of 500 mg."( Bactericidal activity of levofloxacin against Streptococcus pneumoniae in an in-vitro model simulating serum pharmacokinetic parameters.
Schwärzel, R; Shah, PM, 1999
)
0.82
"The aim of this study was to compare the bactericidal efficacy of levofloxacin and ofloxacin against Streptococcus pneumoniae at different dosage regimens for both agents."( Pharmacodynamics of levofloxacin and ofloxacin against Streptococcus pneumoniae.
Bauernfeind, A, 1999
)
0.85
" A greater number of infections were eradicated by levofloxacin than by cefuroxime axetil: infections were eradicated in 68% of patients receiving the 500 mg dosage and in 63% of those taking 250 mg levofloxacin, whereas the eradication rate with the comparator drug was much lower (48%)."( Clinical effectiveness of levofloxacin in patients with acute purulent exacerbations of chronic bronchitis: the relationship with in-vitro activity.
Davies, BI; Maesen, FP, 1999
)
0.84
" The dosing regimen of each drug that yielded serum levels in mice which mimic human therapeutic concentrations of the drugs, were designed."( Comparative efficacies of levofloxacin and ciprofloxacin against Streptococcus pneumoniae in a mouse model of experimental septicaemia.
Bui, KQ; Nicolau, DP; Nightingale, CH; Onyeji, CO; Owens, RC; Quintiliani, R, 1999
)
0.59
"The pharmacokinetics of levofloxacin, administered in high doses and with extended dosing intervals, was studied in human immunodeficiency virus (HIV)-infected patients."( Pharmacokinetics and safety of high-dose and extended-interval regimens of levofloxacin in human immunodeficiency virus-infected patients.
Baird, B; Chow, AT; Fowler, CL; Masur, H; Natarajan, J; Piscitelli, SC; Spooner, K; Walker, RE; Williams, RR, 1999
)
0.83
" The dosage was 500 mg once or twice a day depending on the studies."( [Levofloxacin in the treatment of community-acquired pneumococcal pneumonia].
Léophonte, P; Veyssier, P, 1999
)
0.86
" Good tolerability of the various ofloxacin dosing regimens in both the adult and pediatric patients was shown."( [The safety of ofloxacin].
Efremenkova, OV; Kapranov, NI; Litvinov, DV; Postnikov, SS; Semykin, SIu; Sokolov, AV, 1999
)
0.94
" pneumoniae, with standard dosing resulting in area under the concentration-time curve/MIC ratios and peak concentration/MIC ratios that resulted in 99."( Activities of trovafloxacin, gatifloxacin, clinafloxacin, sparfloxacin, levofloxacin, and ciprofloxacin against penicillin-resistant Streptococcus pneumoniae in an in vitro infection model.
Hershberger, E; Rybak, MJ, 2000
)
0.54
" Dose-response experiments with two topoisomerase IV mutants that confer clinical resistance to quinolones (GrlA(Ser80Phe) and GrlA(Glu84Lys)) indicate that resistance is caused by a decrease in both drug affinity and efficacy."( Action of quinolones against Staphylococcus aureus topoisomerase IV: basis for DNA cleavage enhancement.
Anderson, VE; Gootz, TD; Kaczmarek, FS; Osheroff, N; Zaniewski, RP, 2000
)
0.31
" It would be reasonable to propose the 500 mg twice daily dosage for severe community-acquired pneumonia warranting intensive care hospitalization in accordance with the criteria of the ERS Task Force Report."( [Treatment of community-acquired pneumonia with levofloxacin: 500 mg once a day or 500 mg twice a day?].
Bru, JP; Zuck, P,
)
0.38
" The present study was focused on the impact of ofloxacin on rat testicular DNA ploidy in a dose-response relationship using an image analysis technique on testicular sections following Fuelgen DNA staining."( The impact of ofloxacin on rat testicular DNA: application of image analysis.
Abd-Allah, AR; Gannam, BB; Hamada, FM, 2000
)
0.92
" Experiments simulated variable peak serum concentrations, but clinically relevant half-lives and dosing intervals."( In vitro characterization of fluoroquinolone concentration/MIC antimicrobial activity and resistance while simulating clinical pharmacokinetics of levofloxacin, ofloxacin, or ciprofloxacin against Streptococcus pneumoniae.
Demasters, TA; Madaras-Kelly, KJ, 2000
)
0.51
" In cases where a fever does not decrease through dosage of an antibiotic such as ofloxacin after about 3 days, half of the standard dose of Mao-bushi-saishin-to for 7 days should be considered as a complementary therapy."( Effect of Mao-bushi-saishin-to on infection of ofloxacin resistant bacteria and of unknown origin.
Kamei, T; Tomioka, H; Toriumi, Y, 2000
)
0.79
" Average length of stay (LOS), hospital costs, death rate, age, and ratio of oral to intravenous dosage administration were analyzed."( Experiences at a large teaching hospital with levofloxacin for the treatment of community-acquired pneumonia.
Clark, LC; Davis, CW, 2000
)
0.56
" Plasma OFLX concentration-time course collected from the highest dosage showed a convex decline, indicating a capacity-limited process in drug elimination (Michaelis-Menten elimination)."( Non-linear pharmacokinetics of ofloxacin after a single intravenous bolus dose in pigs.
Ikenoue, N; Kokue, E; Shimoda, M; Son, DS; Tagawa, Y, 2000
)
0.59
" An understanding of pharmacodynamic principles is essential; it forms the scientific basis for the design of dosing strategies that maximize clinical efficacy and minimize toxicity."( Antimicrobial pharmacodynamics.
Ambrose, PG; Grasela, D; Owens, RC, 2000
)
0.31
" Further multiple-dose studies are required to enable dosage recommendations to be made for patients receiving renal replacement therapy with CVVH."( Single-dose pharmacokinetics of levofloxacin during continuous veno-venous haemofiltration in critically ill patients.
Locker, GJ; Losert, H; Schmid, R; Staudinger, T; Thalhammer, F; Thalhammer-Scherrer, R; Traunmüller, F, 2001
)
0.59
" The twice daily dosing regimen encourages better patient adherence to therapy, which is likely to improve treatment efficacy."( Efficacy of ofloxacin and other otic preparations for acute otitis media in patients with tympanostomy tubes.
Goldblatt, EL, 2001
)
0.69
"4 (100%), respectively, over the dosing period."( Streptococcus pneumoniae response to repeated moxifloxacin or levofloxacin exposure in a rabbit tissue cage model.
Bui, KQ; Mattoes, H; McNabb, J; Nicolau, DP; Nightingale, CH; Quintiliani, R; Xuan, D; Zhong, M, 2001
)
0.55
" In the face of rising MICs (as is occurring worldwide with Streptococcus pneumoniae), close attention to appropriate dosing and concentration above the MIC may delay and potentially even prevent antibiotic resistance."( What have we learned from pharmacokinetic and pharmacodynamic theories?
Gilliland, KK; Paladino, JA; Schentag, JJ, 2001
)
0.31
" The penetration of levofloxacin averaged 53% for the 7 mg/kg dosage group, 76% for the 10."( Cerebrospinal fluid penetration and pharmacokinetics of levofloxacin in an experimental rabbit meningitis model.
Dash, AK; Destache, CJ; Larsen, C; Owens, H; Pakiz, CB, 2001
)
0.86
"A dosage schedule of levofloxacin 250 mg qd with a 500 mg loading dose seems appropriate for anuric patients during CVVHF."( Pharmacokinetics of levofloxacin during continuous veno-venous hemofiltration.
Bucher, M; Hansen, E; Jakob, W; Kees, F; Lemberger, P, 2001
)
0.93
" For levofloxacin, plasma samples were obtained at steady state during a 24-h dosing interval."( Pharmacokinetic evaluation of oral levofloxacin in human immunodeficiency virus-infected subjects receiving concomitant antiretroviral therapy.
Cadeo, B; Carosi, G; Fiocchi, C; Marchetti, F; Regazzi, MB; Signorini, L; Viale, P; Villani, A; Villani, P, 2001
)
1.02
" The adverse effects disappeared after the dosage was reduced and the theophylline serum concentration decreased; however, there was no change in theophylline clearance."( Effect of levofloxacin on theophylline clearance during theophylline and clarithromycin combination therapy.
Enomoto, H; Hasegawa, A; Kawana, H; Kitada, M; Kuriyama, T; Nakamura, H; Ohmori, S; Ohtsuka, T, 2001
)
0.68
" Therefore, the purpose of this study was to compare the effectiveness of standard once per day dosing of oral levofloxacin with a standard parenteral antibiotic regimen (nafcillin four times daily) for the treatment of experimental MSSA osteomyelitis in rabbits."( Comparative evaluation of oral levofloxacin and parenteral nafcillin in the treatment of experimental methicillin-susceptible Staphylococcus aureus osteomyelitis in rabbits.
Calhoun, JH; Mader, JT; Shirtliff, ME, 2001
)
0.8
" With the resistant isolates, the MICs for ciprofloxacin, gatifloxacin, grepafloxacin, levofloxacin, and trovafloxacin were above the maximal serum drug concentrations reported for standard dosage regimens."( Fluoroquinolone-resistant Streptococcus pneumoniae associated with levofloxacin therapy.
Drlica, K; Mariano, N; Rahal, JJ; Rahman, N; Segal-Maurer, S; Urban, C; Zhao, X, 2001
)
0.8
"We have assessed levofloxacin penetration in cerebrospinal fluid (CSF) and the liquor-to-plasma ratio (C(L)/C(P)) at 2 hours after dosing in 5 patients with spontaneous acute bacterial meningitis."( Cerebrospinal fluid penetration of levofloxacin in patients with spontaneous acute bacterial meningitis.
Baraldo, M; Furlanut, M; Giobbia, M; Pea, F; Scotton, PG; Vaglia, A, 2001
)
0.91
" Sequential therapy is easily administered due to its high oral bioavailability, and the dosing schedule can be a convenient once-daily dose."( Optimal treatment strategies for acute exacerbations of chronic bronchitis: high-risk patients.
Norrby, SR, 2001
)
0.31
"Thirty-one cases were randomly assigned to two drug regimens using WHO dosage schedules: (i) regimen A (n = 15): isoniazid, rifampicin and ethambutol for 2 months, followed by isoniazid and rifampicin for a further 7 months; and (ii) regimen B (n = 16): isoniazid, pyrazinamide, ethambutol and ofloxacin for 2 months, followed by isoniazid, ethambutol and ofloxacin for a further 10 months."( Safety of an ofloxacin-based antitubercular regimen for the treatment of tuberculosis in patients with underlying chronic liver disease: a preliminary report.
Agarwal, SR; Nandeesh, HP; Saigal, S; Sarin, SK, 2001
)
0.86
" Although clinical trials have shown that gemifloxacin is effective for the treatment of uncomplicated urinary tract infections, whether an oral dosage of 320 mg of gemifloxacin once daily is also adequate for the treatment of complicated urinary tract infections has yet to be confirmed."( Urinary excretion and bactericidal activities of gemifloxacin and ofloxacin after a single oral dose in healthy volunteers.
Bygate, EA; Fairless, AJ; Hammer, M; Kinzig-Schippers, M; Machka, K; Naber, CK; Naber, KG; Sauber, C; Sörgel, F, 2001
)
0.55
" Gatifloxacin should be avoided in the same patient population, and the recommended dosage of 400 mg/day should not be exceeded."( Rates of torsades de pointes associated with ciprofloxacin, ofloxacin, levofloxacin, gatifloxacin, and moxifloxacin.
Frothingham, R, 2001
)
0.57
"Marked extracorporeal elimination of levofloxacin occurs, requiring a dosage adjustment that can be calculated from the characteristics of CVVH and CVVHDF."( Pharmacokinetics of levofloxacin during continuous venovenous hemodiafiltration and continuous venovenous hemofiltration in critically ill patients.
Boos, C; Bruch, HP; Guenter, SG; Iven, H; Muhl, E, 2002
)
0.89
"The main pharmacokinetic parameters af ter the first dosing were as follows: Cmax was (2."( Pharmacokinetics of multiple intravenous instillation of levofloxacin in Chinese healthy subjects.
Li, JT; Li, MN; Li, TY; Liu, Y; Lu, Y; Zhang, JW; Zhang, L; Zhang, YL, 2002
)
0.56
"To probe the pharmacokinetic basis for the use of levofloxacin for complicated skin and skin-structure infections (SSSIs) at a once-daily dosage of 750 mg by investigating its penetration into skin tissue."( Penetration of levofloxacin into skin tissue after oral administration of multiple 750 mg once-daily doses.
Chen, A; Chow, AT; Fowler, C; Lattime, H; Morgan, N; Williams, RR; Wong, F, 2002
)
0.9
" Since this dosing regimen does not reflect the therapeutic situation, we studied the effects of a 5- or 7-day treatment with ofloxacin at lower oral doses (10, 30, and 100 mg/kg twice a day [b."( Synergistic effect of ofloxacin and magnesium deficiency on joint cartilage in immature rats.
Lozo, E; Riecke, K; Schwabe, R; Stahlmann, R; Vormann, J, 2002
)
0.84
" Many of the fluoroquinolone agents have once-daily dosing regimens, enhancing patient adherence."( The expanding role of fluoroquinolones.
Schaeffer, AJ, 2002
)
0.31
" Given the severity of some of the adverse events, a better understanding of dosing and clearer guidelines for monitoring therapy are imperative if these drugs are to be prescribed together."( Adverse events associated with pyrazinamide and levofloxacin in the treatment of latent multidrug-resistant tuberculosis.
Dolovich, LR; Holbrook, A; Loeb, M; Papastavros, T; Whitehead, L, 2002
)
0.57
" A higher dosage of sequential levofloxacin 750mg once daily proved as effective as intravenous ticarcillin/clavulanic acid (+/- oral switch to amoxicillin/clavulanic acid) in the treatment of complicated skin and skin structure infections."( Levofloxacin: an updated review of its use in the treatment of bacterial infections.
Figgitt, DP; Hurst, M; Lamb, HM; Scott, LJ, 2002
)
1.22
" Animals were killed on Days 2, 3, 4, 5 or 8 (the dosing day was designated as Day 1), and the incidence of micronucleus in the epidermis was determined."( In vivo photochemical micronucleus induction due to certain quinolone antimicrobial agents in the skin of hairless mice.
Furuhama, K; Itoh, S; Katoh, M, 2002
)
0.31
"Most integral endpoints of antimicrobial effect, including area between the control growth and time-kill curves (ABBC), area above the curve (AAC) and area under the time-kill curve (AUBC) are determined over a dosing interval (tau), regardless of the actual effect duration."( AUC/MIC relationships to different endpoints of the antimicrobial effect: multiple-dose in vitro simulations with moxifloxacin and levofloxacin.
Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2002
)
0.52
"05) from those observed after intravenous dosing in the same patients; other pharmacokinetic parameters were similar."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.58
"The dosage regimen of intravenous levofloxacin 500 mg once/day appears adequate for most pathogens found in critically ill patients with normal renal function."( Pharmacokinetics of intravenous and oral levofloxacin in critically ill adults in a medical intensive care unit.
Abraham, E; Fish, DN; Rebuck, JA, 2002
)
0.85
"This in vitro study evaluated the pharmacodynamic performance of levofloxacin using different dosing strategies against both a levofloxacin-sensitive (MIC = 1 mg/liter) and -resistant (MIC = 16 mg/liter) strain of Streptococcus pneumoniae."( Microbiologic effectiveness of time- or concentration-based dosing strategies in Streptococcus pneumoniae.
Gunderson, B; Hovde, LB; Ibrahim, KH; Ross, G; Rotschafer, JC; Wright, DH, 2002
)
0.55
" Owing to a concern regarding noncompliance and the adverse effect of bleeding, warfarin dosage was adjusted in one patient even though his first INR value was in the high end of the therapeutic range (2."( Effect of levofloxacin coadministration on the international normalized ratios during warfarin therapy.
Burrows, MM; Enlow, AM; Greenwood, MC; Kilpatrick, DM; Lower, DL; Yamreudeewong, W, 2003
)
0.69
" AUC0-t/MIC was strongly associated with bacterial kill throughout the dosing interval."( AUC(0-t)/MIC is a continuous index of fluoroquinolone exposure and predictive of antibacterial response for Streptococcus pneumoniae in an in vitro infection model.
Ariano, RE; Harding, GK; Iacovides, H; Sun, S; Zelenitsky, SA, 2003
)
0.32
" Area under the concentration-time curve (AUC(tau)) over the 12-hour dosage interval was about 30-40% lower than in healthy volunteers (33."( Pharmacokinetics and pharmacodynamics of intravenous levofloxacin in patients with early-onset ventilator-associated pneumonia.
Baldassarre, M; Brollo, L; Cusenza, A; Di Qual, E; Furlanut, M; Pea, F, 2003
)
0.57
" Dosing regimens and consequent drug exposures that amplify or suppress the emergence of resistant bacterial subpopulations were identified and prospectively validated."( Application of a mathematical model to prevent in vivo amplification of antibiotic-resistant bacterial populations during therapy.
Bachhawat, R; Bush, K; Deziel, MR; Drusano, GL; Dudley, MN; Freeman, C; Jumbe, N; Kahn, JB; Leary, R; Liu, W; Louie, A; Miller, MH; Tam, VH, 2003
)
0.32
" For example, the cost implications of using manufacturers' recommendations for dosing in patients with renal dysfunction may be important, depending on the distribution of various levels of renal function within a patient population."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Also, costs of failing to adjust dosing regimens for decreased renal function were determined."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Costs potentially incurred by failing to adjust dosing for renal function were substantial."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
"Formulary decisions can be facilitated by considering factors such as patient characteristics and related dosing in addition to simple acquisition costs."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Objectives of this study are to determine the pharmacokinetics and dialytic clearance of levofloxacin and develop dosing strategies in these patients."( Levofloxacin pharmacokinetics in ESRD and removal by the cellulose acetate high performance-210 hemodialyzer.
Hamburger, RJ; Kays, MB; Lucksiri, A; Mueller, BA; Scott, MK; Sowinski, KM, 2003
)
1.16
"Direct measurement of the concentration of antimicrobial agents in bronchial epithelial lining fluid (ELF) would allow for a more informed approach to appropriate dosing of antimicrobial agents for respiratory tract infections."( Bronchoscopic microsampling method for measuring drug concentration in epithelial lining fluid.
Ishizaka, A; Nishimura, M; Ogura, S; Oh-hara, T; Yamazaki, K, 2003
)
0.32
" Recent reports demonstrate enhanced activity associated with a higher 750 mg dosage of levofloxacin."( Comparative antimicrobial activity of levofloxacin and ciprofloxacin against Streptococcus pneumoniae.
Garrison, MW, 2003
)
0.81
" In classical fractionated dose-response studies with animals, it is difficult to differentiate between the AUC/MIC ratio and the peak/MIC ratio because of colinearity."( Pharmacodynamics of levofloxacin and ciprofloxacin in a murine pneumonia model: peak concentration/MIC versus area under the curve/MIC ratios.
Fraschini, F; Mattina, R; Mouton, JW; Scaglione, F, 2003
)
0.63
" Plasma samples were collected prior to dosing and for up to 48 hours after."( Lack of bioequivalence of levofloxacin when coadministered with a mineral-fortified breakfast of juice and cereal.
Amsden, GW; Johnson, PW; Whitaker, AM, 2003
)
0.61
" The areas under the concentration-time curves during the 12-h dosing interval (AUC(0-tau)s) were 47."( Levofloxacin disposition in cerebrospinal fluid in patients with external ventriculostomy.
Benetton, C; Furlanut, M; Nascimben, E; Pavan, F; Pea, F; Scotton, PG; Vaglia, A, 2003
)
0.94
"The impact of the pharmacokinetic/pharmacodynamic (PK/PD) parameters (the 24h area under the concentration-time curve [AUC24h]/minimum inhibitory concentration [MIC] and maximum concentration in serum [Cmax]/MIC ratio) after single oral dosing of gatifloxacin on its bactericidal activity and resistance selectivity against quinolone-susceptible clinical isolates of Streptococcus pneumoniae J-69 was investigated using an in vitro PK model."( The effect of pharmacokinetic/pharmacodynamic (PK/PD) parameters of gatifloxacin on its bactericidal activity and resistance selectivity against clinical isolates of Streptococcus pneumoniae.
Ebisu, H; Fukuda, H; Kishii, R; Takei, M, 2003
)
0.32
"In treating SARS, ICWM was superior to the treatment with western medicine alone in aspects of improving clinical symptom, promoting recovery of immune function and absorption of lung inflammation, decreasing the dosage of hormone used and shortening the therapeutic course."( [Controlled clinical study on 49 patients of SARS treated by integrative Chinese and Western medicine].
Jiao, Q; Wang, BG; Zhang, RL, 2003
)
0.32
" Additional groups of rats were orally dosed with 600 mg/kg ofloxacin and ciprofloxacin."( Concentrations of the des-F(6)-quinolone garenoxacin in plasma and joint cartilage of immature rats.
Baumann-Wilschke, I; Bello, A; Kastner, M; Rahm, U; Stahlmann, R, 2004
)
0.57
" In a second study, two dosage regimens of sitafloxacin were compared with placebo in Oriental subjects."( A randomized controlled trial (volunteer study) of sitafloxacin, enoxacin, levofloxacin and sparfloxacin phototoxicity.
Dawe, RS; Ferguson, J; Ibbotson, SH; Sanderson, JB; Thomson, EM, 2003
)
0.55
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.9
" With dosing regimens B and C, levofloxacin concentrations in the aqueous humor were above the MIC90 for most common ocular pathogens, including Staphylococcus and Streptococcus species."( An in vivo study comparing the ocular absorption of levofloxacin and ciprofloxacin prior to phacoemulsification.
Bucci, FA, 2004
)
0.85
" for ventilator associated pneumonia to evaluate if this high dosage regimen might ensure appropriate exposure in the treatment of severe UTIs in ICU patients."( Urinary pharmacokinetics and theoretical pharmacodynamics of intravenous levofloxacin in intensive care unit patients treated with 500 mg b.i.d. for ventilator-associated pneumonia.
Baldassarre, M; Brollo, L; Di Qual, E; Furlanut, M; Nascimben, E; Pavan, F; Pea, F, 2003
)
0.55
"To determine the steady-state, extracellular, and intracellular pulmonary disposition of moxifloxacin (MXF), levofloxacin (LEVO), and azithromycin (AZI) relative to that of the plasma over a 24-h dosing interval."( Steady-state intrapulmonary concentrations of moxifloxacin, levofloxacin, and azithromycin in older adults.
Braman, S; Capitano, B; Mattoes, HM; Nicolau, DP; O'Brien, A; Shore, E; Sutherland, C, 2004
)
0.77
"0 micro g/mL) throughout the dosing interval."( Steady-state intrapulmonary concentrations of moxifloxacin, levofloxacin, and azithromycin in older adults.
Braman, S; Capitano, B; Mattoes, HM; Nicolau, DP; O'Brien, A; Shore, E; Sutherland, C, 2004
)
0.56
" The once daily dosage regimen is more applicable, convenience and has better compliance."( An open label, randomized comparative study of levofloxacin and amoxicillin/clavulanic acid in the treatment of purulent sinusitis in adult Thai patients.
Bunnag, C; Dhiraputra, C; Fooanant, S; Jareoncharsri, P; Srifuengfung, S; Tunsuriyawong, P; Voraprayoon, S, 2004
)
0.58
" g(-1) at 24 h after dosing and declined slowly with a terminal half-life of 468."( Absorption, distribution and excretion of 14C-levofloxacin after single oral administration in albino and pigmented rats: binding characteristics of levofloxacin-related radioactivity to melanin in vivo.
Ono, C; Tanaka, M; Yamada, M, 2004
)
0.58
" Periodic and continuous ECGs were recorded before and after subjects were dosed with placebo and increasing doses of levofloxacin (500 mg, 1000 mg, 1500 mg) that included doses twice the maximum recommended dose of 750 mg in a double-blind, randomized, four-period, four-sequence crossover trial."( Measuring the effects of supratherapeutic doses of levofloxacin on healthy volunteers using four methods of QT correction and periodic and continuous ECG recordings.
Chien, S; Goodman, DB; Natarajan, J; Noel, GJ; Padmanabhan, M; Solanki, B, 2004
)
0.78
" Based on the range of clinical indications, safety profile, local susceptibility, cost, and dosing convenience, levofloxacin was chosen over ciprofloxacin and gatifloxacin as the sole fluoroquinolone."( Drug costs and bacterial susceptibility after implementing a single-fluoroquinolone use policy at a university hospital.
Armitstead, JA; Empey, KL; Evans, ME; Martin, C; Ofotokum, I; Rapp, RP, 2004
)
0.53
" Areas between the control growth and the time--kill curves (ABBC in single dose simulations and the sum of ABBCs determined after the first, second and third dosing in multiple dose simulations--ABBC(1+2+3)) were higher with ABT492 than levofloxacin."( ABT492 and levofloxacin: comparison of their pharmacodynamics and their abilities to prevent the selection of resistant Staphylococcus aureus in an in vitro dynamic model.
Arzamastsev, AP; Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2004
)
0.87
"Ofloxacin was administered to six male goats intravenously (5 mg/kg) to determine its kinetic behavior, tissue residue, in vitro plasma protein binding and to compute a rational dosage regimen."( Pharmacokinetics, tissue residue and plasma protein binding of ofloxacin in goats.
Baruah, H; Khonikor, HN; Roy, DC; Roy, RK, 2004
)
2.01
"The aqueous penetration of the commercial preparations of the fluoroquinolone antibiotics ofloxacin, ciprofloxacin, levofloxacin, and gatifloxacin were compared following topical dosing in a rabbit model."( Aqueous penetration of gatifloxacin and levofloxacin into the rabbit aqueous humor following topical dosing.
Blanchard, J; Lane, LC; Levine, JM; Noecker, RJ; Rapedius, M; Snyder, RW, 2004
)
0.81
" The concentration and the extent of accumulation of radioactivity not only in melanin-containing ocular tissues but also in other non-pigmented ocular tissues, such as retina, after chronic oral administration of 14C-levofloxacin once daily for 84 days were much lower than those after multiple dosing with 14C-chloroquine under the same conditions."( Comparative assessment of ocular tissue distribution of drug-related radioactivity after chronic oral administration of 14C-levofloxacin and 14C-chloroquine in pigmented rats.
Takashina, H; Tanaka, M; Tsutsumi, S, 2004
)
0.71
" This is one of the first studies to demonstrate a significant effect of a computerized intervention on dosing route within an antibiotic class."( Oral quinolones in hospitalized patients: an evaluation of a computerized decision support intervention.
Arbogast, PG; Bansal, P; Hargrove, F; Hulgan, T; Kernodle, DS; Miller, RA; Rosenbloom, ST; Talbert, DA, 2004
)
0.32
" Pharmacokinetics of levofloxacin simulated after 500 mg, 750 mg and 1000 mg once daily dosing resulted in levofloxacin volume of distribution: elderly patients = younger patients, while levofloxacin clearance was: elderly patients < younger patients."( Pharmacodynamic target attainment analysis against Streptococcus pneumoniae using levofloxacin 500 mg, 750 mg and 1000 mg once daily in plasma (P) and epithelial lining fluid (ELF) of hospitalized patients with community acquired pneumonia (CAP).
Chan, CK; Hoban, DJ; Marras, TK; Noreddin, AM; Sanders, K; Zhanel, GG, 2004
)
0.85
" To provide dosing guidance for children, 3 single-dose, multicenter pharmacokinetic studies were conducted in 85 children in 5 age groups: 6 months to <2 years, 2 to <5 years, 5 to <10 years, 10 to <12 years, and 12 to 16 years."( Levofloxacin pharmacokinetics in children.
Blumer, JL; Bocchini, JA; Bradley, JS; Chien, S; Kearns, GL; Maldonado, S; Natarajan, J; Noel, GJ; Wells, TG, 2005
)
0.95
" The percentage of patients who required a warfarin dosage adjustment based on the post-INR (secondary outcome measure) was 41% (9 of 22 patients) in the levofloxacin group and 33% (7 of 21 patients) in the felodipine group."( Retrospective evaluation of a possible interaction between warfarin and levofloxacin.
Anderson, HG; McCall, KL; Scott, JC, 2005
)
0.76
"A standard dosage regimen of 500 mg/day was administered to nine Caucasian patients included in the study, irrespective of their demographic characteristics."( Pharmacokinetics and pharmacodynamics of levofloxacin in intensive care patients.
Alvarez Lerma, F; Colino Gandarillas, CI; Domínguez-Gil, A; Menacho, YA; Sánchez Navarro, A, 2005
)
0.59
"The aim was to confirm which was the better regimen for second-line therapy after treatment failure with a standard triple therapy in Japan, a high dosage of levofloxacin- or metronidazole-based therapy."( Levofloxacin- versus metronidazole-based rescue therapy for H. pylori infection in Japan.
Aoyama, N; Kasuga, M; Matsumoto, Y; Miki, I; Mitani, T; Miyachi, H; Morita, Y; Shirasaka, D; Tamura, T; Toyoda, M; Watanabe, Y, 2005
)
1.15
" Dosing regimens for gatifloxacin were 400 mg once daily (qd) administered to younger patients (<65 years) and gatifloxacin 200 mg qd to elderly patients (> or =65 years)."( Comparison of gatifloxacin and levofloxacin administered at various dosing regimens to hospitalised patients with community-acquired pneumonia: pharmacodynamic target attainment study using North American surveillance data for Streptococcus pneumoniae.
Hoban, DJ; Noreddin, AM; Zhanel, GG, 2005
)
0.61
" Serum levofloxacin disposition after intravenous and oral dosing was best fitted to a bicompartmental and a monocompartmental open models with first-order elimination, respectively."( Pharmacokinetics of levofloxacin after single intravenous and repeat oral administration to cats.
Albarellos, GA; Ambros, LA; Landoni, MF, 2005
)
1.04
" The ECL was satisfactorily applied to the determination of the two FQs in dosage form and urine sample."( Electrochemiluminescence of terbium (III)-two fluoroquinolones-sodium sulfite system in aqueous solution.
Chen, SL; Ding, F; Liu, Y; Zhao, HC, 2006
)
0.33
" Efforts should be directed at modifying hospital policies for dosing of levofloxacin and DTCCs to prevent coadministration."( Coadministration of oral levofloxacin with agents that impair its absorption: potential impact on emergence of resistance.
Barton, TD; Fishman, NO; Lautenbach, E; Quain, RD; Weiner, MG, 2005
)
0.85
" Levofloxacin dosage adjustments based on sex should be considered on an individual basis."( Pharmacokinetics of intravenously administered levofloxacin in men and women.
Goldman, M; Kays, MB; Lagvankar, S; Mueller, BA; Overholser, BR; Sowinski, KM, 2005
)
1.14
"Sustained release (SR)-gastroretentive dosage forms (GRDF) enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal (GI) tract and improve the bioavailability of medications that are characterized by a narrow absorption window."( Development of sustained release gastroretentive drug delivery system for ofloxacin: in vitro and in vivo evaluation.
Chaudhari, S; Chavanpatil, M; Jain, P; Shear, R; Vavia, P, 2005
)
0.56
"Levofloxacin is a fluoroquinolone antimicrobial agent for which pharmacodynamic relationships between the maximum serum antibiotic concentration (Cmax)/minimum inhibitory concentration (MIC) ratio and/or the area under the serum concentration-time curve during a 24-h dosing period (AUC(0-24))/MIC ratio and clinical and/or microbiological outcomes have been developed."( Pharmacodynamics of levofloxacin in patients with acute exacerbation of chronic bronchitis.
Blasi, F; Cazzola, M; Donnarumma, G; Marchetti, F; Matera, MG; Sanduzzi, A; Tufano, MA, 2005
)
1.26
" By using a simulated animal pharmacokinetic profile, a once-daily dosing regimen that provided a human-equivalent exposure failed to sterilize the cultures."( Effective antimicrobial regimens for use in humans for therapy of Bacillus anthracis infections and postexposure prophylaxis.
Basset, J; Bush, K; Byrne, WR; Deziel, MR; Drusano, GL; Heine, H; Kao, M; Kelly, M; Louie, A; Miller, L, 2005
)
0.33
" The unbound AUC/MIC ratio revealed that levofloxacin used in the described manner was borderline sufficient for the treatment of nosocomial pneumonia caused by Klebsiella pneumoniae and insufficient for the treatment of pneumonia caused by Pseudomonas aeruginosa, because the breakpoint of 30 to 40 for AUC/MIC could not be reached by the conventionally used dosage schema in our post-CS setting."( In vivo measurement of levofloxacin penetration into lung tissue after cardiac surgery.
Burgmann, H; Hutschala, D; Jaksch, P; Mayer-Helm, BX; Müller, M; Skhirtladze, K; Tschernko, EM; Wisser, W; Wolner, E; Zuckermann, A, 2005
)
0.89
" pneumoniae, MPC results were below susceptible breakpoints and within clinically achievable and sustainable drug concentrations for >24 hours of the dosing interval against."( Comparison of the minimum inhibitory, mutant prevention and minimum bactericidal concentrations of ciprofloxacin, levofloxacin and garenoxacin against enteric Gram-negative urinary tract infection pathogens.
Blondeau, JM; Hansen, GT, 2005
)
0.54
"The aim of this work is to provide a methodology to predict the potential efficacy of standard dosage schedules established for antimicrobials when used in clinical practice and administered to patients with different demographic characteristics."( [Pharmacokinetic/pharmacodynamic analysis to optimize antibacterial treatments: prediction of efficacy by using Montecarlo simulation techniques].
Sánchez Navarro, A, 2005
)
0.33
"Compare two dosage strengths of levofloxacin in the treatment of acute bacterial sinusitis."( A trial of high-dose, short-course levofloxacin for the treatment of acute bacterial sinusitis.
Anon, J; Kahn, J; Khashab, M; Paglia, M; Poole, M; Xiang, J, 2006
)
0.88
" The safety profile of the 2 dosage strengths was similar."( A trial of high-dose, short-course levofloxacin for the treatment of acute bacterial sinusitis.
Anon, J; Kahn, J; Khashab, M; Paglia, M; Poole, M; Xiang, J, 2006
)
0.6
" Recommendations for agent selection, agent concentration, length of treatment, dosing schedule, and methods of irrigation are presented."( Evidence-based recommendations for antimicrobial nasal washes in chronic rhinosinusitis.
Elliott, KA; Stringer, SP,
)
0.13
" dosing of levofloxacin (81%[95% CI: 78%-89%]vs 84%[95% CI: 66%-97%])."( Levofloxacin-based triple therapy versus bismuth-based quadruple therapy for persistent Helicobacter pylori infection: a meta-analysis.
Chey, WD; Kim, HM; Saad, RJ; Schoenfeld, P, 2006
)
1.32
" Adherence to the prescribed regimen is affected by a number of variables including dosing interval, treatment duration, adverse effects, and palatability in pediatric patients."( Value of short-course antimicrobial therapy in community-acquired pneumonia.
Blasi, F; Tarsia, P, 2005
)
0.33
"Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window."( Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin.
Chaudhari, S; Chavanpatil, MD; Jain, P; Shear, R; Vavia, PR, 2006
)
0.55
" This subgroup analysis attempted to compare the safety and efficacy of a short-course levofloxacin regimen with traditional levofloxacin dosing for PSI Class III/IV patients."( Levofloxacin 750-mg for 5 days for the treatment of hospitalized Fine Risk Class III/IV community-acquired pneumonia patients.
Kahn, JB; Khashab, MM; Shorr, AF; Tennenberg, AM; Xiang, JX, 2006
)
1.18
" These differences can pose challenges in developing appropriate dosing guidelines."( Do intensive care patients need an individualized dosing regimen for levofloxacin?
Barth, J; Hochhaus, G; Jäger, D; Kaufmann, S; Tayab, ZR, 2006
)
0.57
" For patients with higher levofloxacin clearance, the resulting efficacy for different strains of bacteria (expressed as free AUC/MIC ratios) suggested that for less sensitive pathogens, a dosage adjustment may be needed."( Do intensive care patients need an individualized dosing regimen for levofloxacin?
Barth, J; Hochhaus, G; Jäger, D; Kaufmann, S; Tayab, ZR, 2006
)
0.86
" This may have significant implications in the clinical setting for identifying optimal dosage regimens for ICU patients."( Do intensive care patients need an individualized dosing regimen for levofloxacin?
Barth, J; Hochhaus, G; Jäger, D; Kaufmann, S; Tayab, ZR, 2006
)
0.57
" Three males and three female Rhesus monkeys were dosed with a single oral dose of 14C-levofloxacin at 15 mg kg-1 (2 MBq kg-1)."( Pharmacokinetics, metabolism, excretion and plasma protein binding of 14C-levofloxacin after a single oral administration in the Rhesus monkey.
Bottacini, M; Hemeryck, A; Kao, M; Kelley, MF; Macpherson, D; Mamidi, RN, 2006
)
0.78
"5 points above the INR before fluoroquinolone use; major or minor bleeding events; requirement for vitamin K administration; warfarin dosage reduction or withholding doses; and warfarin-related hospital, emergency, or urgent care admissions or visits."( Anticoagulation-related outcomes in patients receiving warfarin after starting levofloxacin or gatifloxacin.
Cole, J; Mathews, S; Ryono, RA, 2006
)
0.56
" Both the dosage forms follow Higuchi model for release from formulations."( Formulation and development of gastroretentive drug delivery system for ofloxacin.
Ali, J; Ali, M; Hasan, S, 2006
)
0.57
"Given similar adverse event profiles and the advantages of higher dose therapy, including shorter courses of therapy and potential impact on preventing resistance, clinicians should consider utilizing the 750 mg dose of levofloxacin when choosing between dosage strengths for treatment of indicated infections."( Comparison of the adverse event profiles of levofloxacin 500 mg and 750 mg in clinical trials for the treatment of respiratory infections.
Kahn, JB; Khashab, MM; Xiang, J, 2006
)
0.78
" The value of dosing of antimicrobial agents based on MPC thresholds results in a rapid reduction in viable cells--even at higher inocula which are more reflective of organism burden in pneumonia."( Application of two methods to determine killing of Streptococcus pneumoniae by various fluoroquinolones.
Blondeau, JM; Blondeau, LD; Borsos, S; Hesje, C, 2006
)
0.33
" Computer simulations to match plasma concentration profile, area under the concentration-time curve (AUC), and time above MIC for a human oral dose of 500 mg levofloxacin once a day identified a dosing regimen in rhesus monkeys that would most closely match human exposure: 15 mg/kg followed by 4 mg/kg administered 12 h later."( Pharmacokinetic considerations and efficacy of levofloxacin in an inhalational anthrax (postexposure) rhesus monkey model.
Barnewall, R; Bush, K; Chien, S; Drusano, GL; Estep, J; Hemeryck, A; Kao, LM; Kelley, MF; Minton, N; Olson, PH; Thalacker, FW, 2006
)
0.78
"The mutant selection window hypothesis, originally based on agar plate assays, may lead to new antimicrobial dosing strategies that severely restrict the acquisition of resistance."( The mutant selection window in rabbits infected with Staphylococcus aureus.
Cui, J; Drlica, K; Liu, Y; Tong, W; Wang, R; Zhao, X, 2006
)
0.33
" It can be concluded that overall the doses of the two tested fluoroquinolones may be considered equivalent with regard to treatment of complicated urinary tract infections, although the recommended dosing is twice daily for ciprofloxacin and once daily for levofloxacin."( Concentrations in plasma, urinary excretion and bactericidal activity of levofloxacin (500 mg) versus ciprofloxacin (500 mg) in healthy volunteers receiving a single oral dose.
Kinzig-Schippers, M; Naber, KG; Sörgel, F; Wagenlehner, FM; Weidner, W, 2006
)
0.75
" Area under the concentration time curve to minimum inhibitory concentration (AUC/MIC) values for tigecycline ranged from 79 to 158 microg h/mL and tigecycline concentrations remained above the MIC (T>MIC) throughout the simulated dosing interval."( In vitro activity of tigecycline against quinolone-resistant Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci.
Garrison, MW; Nuemiller, JJ, 2007
)
0.34
" Standard levofloxacin dosing (especially monotherapy) is unlikely to produce maximum therapeutic effectiveness."( Levofloxacin pharmacokinetics in adult cystic fibrosis.
Boyle, MP; Brass-Ernst, L; Diener-West, M; Lee, CKK; Noschese, M; Zeitlin, PL, 2007
)
1.33
" and the possible emergence of resistant bacterial strains in a ten rats group receiving levofloxacin at the dosage of 10mg/kg one a day for 5 consecutive days."( [Changes in intestinal microflora following levofloxacin administration in laboratory animals].
Ciarcia, R; Esposito, S; Ianniello, F; Leone, S; Lucisano, A; Noviello, S, 2005
)
0.81
"A rapid and sensitive reverse phase high performance liquid chromatographic (RP-HPLC) method for the analysis of levofloxacin from bulk materials, dosage formulations and human serum is described."( Optimization of levofloxacin analysis by RP-HPLC using multivariate calibration technique.
Arayne, MS; Siddiqui, FA; Sultana, N, 2007
)
0.88
" The purpose of this paper is to review the concepts pertinent to drug removal by hemodialysis and discuss the issues related to these new dialysis techniques and how they may have a impact on drug removal and the design of dosing regimens."( Drug dosing considerations in alternative hemodialysis.
Decker, BS; Mueller, BA; Sowinski, KM, 2007
)
0.34
" pylori treatment: effectiveness (>80%), simplicity (twice-daily dosing and excellent compliance) and safety (low incidence of adverse effects)."( First-line triple therapy with levofloxacin for Helicobacter pylori eradication.
Fernández-Bermejo, M; Gisbert, JP; González-García, G; Mateos-Rodríguez, JM; Molina-Infante, J; Pérez-Gallardo, B; Prieto-Bermejo, AB; Robledo-Andrés, P, 2007
)
0.62
"To identify the optimal dosage of levofloxacin to eradicate persistent Helicobacter pylori when triple therapy with amoxicillin, clarithromycin, and omeprazole fails."( Levofloxacin-containing triple therapy to eradicate the persistent H. pylori after a failed conventional triple therapy.
Chang, WL; Chen, WY; Cheng, HC; Sheu, BS; Wu, JJ; Yang, HB, 2007
)
1.23
" According to these findings, anuric critically ill patients who are undergoing EDD should be treated with the standard dosage of moxifloxacin (400 mg/d intravenously)."( Pharmacokinetics of moxifloxacin and levofloxacin in intensive care unit patients who have acute renal failure and undergo extended daily dialysis.
Czock, D; de Groot, K; Fliser, D; Hafer, C; Haller, H; Hüsig-Linde, C; Keller, F; Kielstein, JT; Kuse, E; Langhoff, A; Schöpke, T; Swoboda, S, 2006
)
0.6
" Included studies also had to meet 3 minimum criteria: evaluation of clinically relevant dosing regimens, use of rigorous study methods, and provision of mean (SD) values for the pharmacokinetic parameters of interest."( Simulated comparison of the pharmacodynamics of ciprofloxacin and levofloxacin against Pseudomonas aeruginosa using pharmacokinetic data from healthy volunteers and 2002 minimum inhibitory concentration data.
Burgess, DS; Hall, RG, 2007
)
0.59
" Improper dosage adjustment based on renal function was not associated with higher rates of hypoglycemia and hyperglycemia for either drug."( Effects of gatifloxacin and levofloxacin on rates of hypoglycemia and hyperglycemia among elderly hospitalized patients.
Graves, J; Lodise, T; Lomaestro, B; Miller, C; Mohr, JF; Smith, RP, 2007
)
0.63
" For eradication, European, Canadian, and American guidelines recommend a regimen consisting of a proton pump inhibitor, clarithromycin, and metronidazole or amoxicillin dosed twice daily for at least 7 days."( An alternative salvage regimen for Helicobacter pylori-resistant patients with heart failure.
Cantu, M; Ferguson, D; Page, RL, 2008
)
0.35
" no change in warfarin dosing in 40 chronically anticoagulated patients initiating trimethoprim-sulfamethoxazole (TMP-SMX) or levofloxacin."( Impact of preemptive warfarin dose reduction on anticoagulation after initiation of trimethoprim-sulfamethoxazole or levofloxacin.
Ahmed, A; Fay, WP; Kaus, CA; Stephens, JC, 2008
)
0.76
" An expectant strategy consisting of no change in warfarin dosing with short-term INR follow-up appears reasonable in patients treated with levofloxacin."( Impact of preemptive warfarin dose reduction on anticoagulation after initiation of trimethoprim-sulfamethoxazole or levofloxacin.
Ahmed, A; Fay, WP; Kaus, CA; Stephens, JC, 2008
)
0.76
"Information about the elimination and the adequate dosing of levofloxacin during renal replacement therapy is scarce."( Clearance of levofloxacin by an in vitro model of continuous venovenous hemodialysis (CVVHD).
Drewelow, B; Mueller, SC; Siewert, S, 2007
)
0.92
" Based on the pharmacokinetic parameters, an appropriate intravenous dosage regimen for levofloxacin would be 5 mg/kg repeated at 24 h intervals when prescribed with paracetamol in calves."( Disposition kinetics and dosage regimen of levofloxacin on concomitant administration with paracetamol in crossbred calves.
Dumka, VK, 2007
)
0.82
"A simple, rapid, and accurate high-performance thin-layer chromatography (HPTLC) method is described for the simultaneous determination of levofloxacin hemihydrate and ornidazole in tablet dosage form."( Validated HPTLC method for simultaneous estimation of levofloxacin hemihydrate and ornidazole in pharmaceutical dosage form.
Bari, SB; Chepurwar, SB; Fursule, RA; Shirkhedkar, AA; Surana, SJ, 2007
)
0.79
" Multivariate analysis demonstrated that lack of downward dosage adjustment based on creatinine clearance (odds ratio [OR] 10."( Prevalence of and risk factors for dysglycemia in patients receiving gatifloxacin and levofloxacin in an outpatient setting.
LaPlante, KL; Mersfelder, TL; Quilliam, BJ; Ward, KE, 2008
)
0.57
" Lack of downward fluoroquinolone dosage adjustment for renal function, presence of diabetes, and treatment with insulin or sulfonylureas each independently increased the risk of dysglycemia."( Prevalence of and risk factors for dysglycemia in patients receiving gatifloxacin and levofloxacin in an outpatient setting.
LaPlante, KL; Mersfelder, TL; Quilliam, BJ; Ward, KE, 2008
)
0.57
" In patients with these risk factors, especially among people with a combination of said risk factors - which is frequently the case with nephrologic and dialysis patients, especially -, fluoroquinolones should be administered only after critical evaluation and with a dosage that is adapted to renal function."( [Fluoroquinolone-induced Achilles tendon rupture].
Maurin, N, 2008
)
0.35
" To prevent the emerging of resistance resulting from its abuse, an optimal method and dosage are needed."( Population pharmacokinetics of levofloxacin as prophylaxis for febrile neutropenia.
Fujimoto, Y; Kanbayashi, Y; Matsumoto, Y; Morimoto, Y; Nomura, K; Taniwaki, M, 2008
)
0.63
" is predicted to be the most effective dosage and method."( Population pharmacokinetics of levofloxacin as prophylaxis for febrile neutropenia.
Fujimoto, Y; Kanbayashi, Y; Matsumoto, Y; Morimoto, Y; Nomura, K; Taniwaki, M, 2008
)
0.63
" Our findings suggest the re-evaluation of clinical dosing schemas of antibiotic therapy in a variety of diseases associated with atelectasis formation."( The impact of perioperative atelectasis on antibiotic penetration into lung tissue: an in vivo microdialysis study.
Hutschala, D; Kinstner, C; Mayer-Helm, BX; Müller, M; Skhirtladze, K; Tschernko, E; Wisser, W; Zeitlinger, M, 2008
)
0.35
" A hollow-fiber infection model (HFIM) simulating various clinical (fluctuating concentrations over time) dosing exposures was used to selectively validate our quantitative assessment of the combined killing effect."( Quantitative assessment of combination antimicrobial therapy against multidrug-resistant Acinetobacter baumannii.
Chang, KT; Hou, JG; Kwa, AL; Ledesma, KR; Lim, TP; Nikolaou, M; Prince, RA; Quinn, JP; Tam, VH, 2008
)
0.35
"Being a sustained release dosage form, pellets allow ofloxacin to exhibit improved release and absorption profiles."( In vitro and in vivo evaluation of ofloxacin sustained release pellets.
Cui, Y; Tang, X; Zhang, Y, 2008
)
0.87
" The efficacy of the rifampin-levofloxacin combination is not significantly improved by the dosage of levofloxacin."( Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Euba, G; Gudiol, F; Murillo, O; Pachón, ME; Tubau, F; Verdaguer, R, 2008
)
0.87
" Azithromycin use was associated with more nausea in the 30 min after dosing (azithromycin group, 8% of patients; levofloxacin group, 1% of patients; Pp."( Azithromycin and loperamide are comparable to levofloxacin and loperamide for the treatment of traveler's diarrhea in United States military personnel in Turkey.
Frenck, RW; Johnston, JR; Monteville, MR; Putnam, SD; Riddle, MS; Rockabrand, DM; Sanders, JW; Tribble, DR; Ulukan, S, 2007
)
0.8
" Although nausea after dosing is uncommon, it is more frequently associated with azithromycin than with levofloxacin."( Azithromycin and loperamide are comparable to levofloxacin and loperamide for the treatment of traveler's diarrhea in United States military personnel in Turkey.
Frenck, RW; Johnston, JR; Monteville, MR; Putnam, SD; Riddle, MS; Rockabrand, DM; Sanders, JW; Tribble, DR; Ulukan, S, 2007
)
0.81
" The methods developed were applied successfully to the determination of the subject drugs in their pharmaceutical dosage forms with good precision and accuracy compared to official and reported methods as revealed by t- and F-tests."( Study of fluorescence characteristics of the charge-transfer reaction of quinolone agents with bromanil.
Chen, XF; Li, WY; Xuan, CS, 2009
)
0.35
"The manuscript describes validated reversed-phase column high-performance liquid chromatographic (RP-HPLC) and first-derivative UV spectrophotometric methods for the estimation of levofloxacin (LFX) and ornidazole (ORNI) in combined dosage forms."( Development and validation of column high-performance liquid chromatographic and derivative spectrophotometric methods for determination of levofloxacin and ornidazole in combined dosage forms.
Patel, NJ; Patel, PU; Patel, SA; Prajapati, AM; Vaghmasi, JB,
)
0.52
"This is the first study to measure AH levels of levofloxacin after postoperative pulsed dosing in humans."( Increased anterior chamber penetration of topical levofloxacin 0.5% after pulsed dosing in cataract patients.
Gardner, S; Geldsetzer, K; Lokkila, J; Ropo, A; Seal, D; Stenevi, U; Sundelin, K, 2009
)
0.85
" Therapy was initiated at 2 h postinoculation with 5-640 mg/kg per d fractionated for different dosing regimens."( Pharmacokinetics/pharmacodynamics of antofloxacin hydrochloride in a neutropenic murine thigh model of Staphylococcus aureus infection.
Xiao, XM; Xiao, YH, 2008
)
0.61
" However, dosage and length of levofloxacin-based regimens have not been established."( Second-line levofloxacin-based triple schemes for Helicobacter pylori eradication.
Di Caro, S; Franceschi, F; Gasbarrini, A; La Rocca, E; Mariani, A; Masci, E; Raimondo, D; Testoni, A; Thompson, F, 2009
)
0.98
" Dosage of levofloxacin did not affect the eradication rates (77."( Second-line levofloxacin-based triple schemes for Helicobacter pylori eradication.
Di Caro, S; Franceschi, F; Gasbarrini, A; La Rocca, E; Mariani, A; Masci, E; Raimondo, D; Testoni, A; Thompson, F, 2009
)
1.07
"1% dosing approach the calculated value was 116 microg/cm2."( Cleaning validation of ofloxacin on pharmaceutical manufacturing equipment and validation of desired HPLC method.
Ali, SS; Arayne, MS; Sajid, SS; Sultana, N,
)
0.44
"Emerging evidence suggests that current fluoroquinolone dosing strategies may be inadequate to treat bloodstream infections caused by organisms classified as sensitive."( Effect of differences in MIC values on clinical outcomes in patients with bloodstream infections caused by gram-negative organisms treated with levofloxacin.
Defife, R; Feinglass, JM; Postelnick, MJ; Scarsi, KK; Scheetz, MH, 2009
)
0.55
"5% eyedrops with the classic, more frequent dosing in patients with bacterial conjunctivitis."( Clinical and microbiological efficacy of levofloxacin administered three times a day for the treatment of bacterial conjunctivitis.
Kaminska, A; Szaflik, J; Szaflik, JP,
)
0.39
"5% levofloxacin eyedrops three times daily to each eye for 5 days (experimental dosage group), or every 2 hours on days 1 and 2, and then every 4 hours on days 3-5 (up to four times per day) (classic dosage group)."( Clinical and microbiological efficacy of levofloxacin administered three times a day for the treatment of bacterial conjunctivitis.
Kaminska, A; Szaflik, J; Szaflik, JP,
)
0.87
"3% in classic dosage group, p=0."( Clinical and microbiological efficacy of levofloxacin administered three times a day for the treatment of bacterial conjunctivitis.
Kaminska, A; Szaflik, J; Szaflik, JP,
)
0.39
" Subsequent studies should be performed to evaluate antibiotic resistance, doses, dosing intervals, duration of treatment, and safety of these two regimes."( Failure of Helicobacter pylori treatment after regimes containing clarithromycin: new practical therapeutic options.
Coelho, L; Moretzsohn, L; Sanches, B; Vieira, G, 2008
)
0.35
" Concentrations of all agents are predicted to exceed the MPC for ATCC 49226 for the entire dosage interval, while concentrations of moxifloxacin alone will exceed the MPC for m-49226."( Evaluation of the mutant selection window for fluoroquinolones against Neisseria gonorrhoeae.
Allen, GP; Hankins, CD, 2009
)
0.35
" The proposed method has been applied for the analysis of ofloxacin and ornidazole both individually and in a combined dosage tablet formulation."( Simultaneous determination of ofloxacin and ornidazole in pharmaceutical preparations by capillary zone electrophoresis.
Aboul-Enein, HY; Ali, AS; Elbashir, AA; Saad, B; See, KL, 2009
)
0.89
" In case of macrolides higher dosage is indicated, because there is a risk of clinical failure at lower doses."( [Voice on the treatment of ureaplasmas infections].
Biernat-Sudolska, M; Drzewiecki, A; Rojek-Zakrzewska, D, 2009
)
0.35
" The superiority of aerosol dosing over systemic dosing was demonstrated in models of both acute and chronic lung infection."( Efficacy of aerosol MP-376, a levofloxacin inhalation solution, in models of mouse lung infection due to Pseudomonas aeruginosa.
Dudley, MN; Griffith, DC; Miller, CE; Nolan, TG; Sabet, M; Senekeo-Effenberger, K, 2009
)
0.63
"The objective of current study was to develop a validated specific stability indicating reversed-phase liquid chromatographic method for the quantitative determination of levofloxacin as well as its related substances determination in bulk samples, pharmaceutical dosage forms in the presence of degradation products and its process related impurities."( A validated stability-indicating RP-HPLC method for levofloxacin in the presence of degradation products, its process related impurities and identification of oxidative degradant.
Chandrasekhar, KB; Lalitha Devi, M, 2009
)
0.79
"The efficacy of drug candidates is frequently limited by their inability to reach the target site of action, especially when they are administered through conventional dosage forms or drug delivery systems."( Ofloxacin targeting to lungs by way of microspheres.
Harsha, S; R, C; Rani, S, 2009
)
1.8
" The results indicate that LVFX dosage adjustment should be individualized on the basis of the CL(cr), especially in those with CL(cr) less than 50 ml/min."( Population pharmacokinetics of oral levofloxacin 500 mg once-daily dosage in community-acquired lower respiratory tract infections: results of a prospective multicenter study in China.
Cao, GY; Huang, JA; Liu, YB; Shi, YG; Si, B; Sun, SH; Wu, XJ; Xia, QM; Xiao, ZK; Xu, JF; Zhang, J; Zhang, YY, 2009
)
0.62
" This study concluded that the dosage regimen of LVFX 500 mg once daily was effective and tolerable for the treatment of LRTIs and UTIs."( Clinical evaluation of oral levofloxacin 500 mg once-daily dosage for treatment of lower respiratory tract infections and urinary tract infections: a prospective multicenter study in China.
Chen, BY; Ding, GH; Duan, J; Gu, JM; Guo, DY; Hao, QL; Huang, HH; Huang, JA; Li, HY; Li, QH; Liu, A; Lü, XJ; Ma, H; Ren, ZY; Shen, HH; Shi, MH; Si, B; Sun, SH; Sun, TY; Wu, GM; Xia, QM; Xiao, W; Xiao, ZK; Xiu, QY; Yang, HF; Yang, HP; Yao, WZ; Ying, KJ; Yu, YS; Yue, HM; Zhang, W; Zhang, YY; Zheng, HG, 2009
)
0.64
" Different dosing regimens were simulated to match adult exposure (area under the concentration-time curve from 0 to 24 h at steady state, maximum concentration of drug in serum at steady state, and minimum concentration of drug in serum at steady state) following the approved adult dose of 500 mg once a day."( Pharmacometrics-based dose selection of levofloxacin as a treatment for postexposure inhalational anthrax in children.
Chien, S; Li, F; Nandy, P; Noel, GJ; Tornoe, CW, 2010
)
0.62
" These results, including in vitro antibacterial activity against clinical isolates and therapeutic efficacy of a humanized dosing regimen, provide good evidence to support the use of LVFX at 500 mg once a day for treating patient with legionnaires disease."( [Therapeutic efficacy of levofloxacin against a model of replicable Legionella pneumophila lung infection in DBA/2 mice].
Fujikawa, K; Karibe, Y; Kashimoto, Y; Kurosaka, Y; Namba, K; Otani, T; Uoyama, S; Yamaguchi, K, 2009
)
0.65
" Subjects were dosed every 2 hours while awake and 4 and 6 hours after retiring (Days 1-3) and four times daily while awake (Days 4-14)."( Tear concentration and safety of levofloxacin ophthalmic solution 1.5% compared with ofloxacin ophthalmic solution 0.3% after topical administration in healthy adult volunteers.
Holdbrook, M; Krebs, W; Rinehart, M; Walters, T, 2010
)
0.64
"3% ophthalmic solution after topical dosing in human eyes."( [Human aqueous humor levels of levofloxacin 0.5%, gatifloxacin 0.3% and levofloxacin 0.3% ophthalmic solution after topical dosing].
Chen, WJ; Huang, XD; Yao, K; Yuan, JQ; Zhang, Z, 2009
)
0.63
" Subsequently, a neutropenic murine pneumonia model with simulated clinical dosing exposures was used to validate our quantitative assessment of combined killing."( Quantitative assessment of combination antimicrobial therapy against multidrug-resistant bacteria in a murine pneumonia model.
Hou, J; Ledesma, KR; Prince, RA; Singh, R; Tam, VH; Yuan, Z, 2010
)
0.36
" The proposed procedure was applied successfully for the detection of the investigated drugs in their pharmaceutical dosage forms, in spiked plasma, spiked urine, and urine samples, with good precision and accuracy."( Determination of ofloxacin and gatifloxacin by mixed micelle-mediated cloud point extraction-fluorimetry combined methodology.
Du, LM; Wu, H; Zhao, GY, 2010
)
0.7
"0 hours after the dosing of ofloxacin tablets to 24 rabbits and analyzed by high performance liquid chromatography."( The effect of binders on the bioavailability of ofloxacin tablets in animal model.
Ahmad, M; Akhtar, N; Khan, HM; Murtaza, G; Rasool, F,
)
0.68
" A biphasic extended release profile at an appropriate dose can inhibit the biofilm growth for four days, therefore reducing the dosing frequency."( Antibacterial efficacy of inhalable levofloxacin-loaded polymeric nanoparticles against E. coli biofilm cells: the effect of antibiotic release profile.
Chang, MW; Cheow, WS; Hadinoto, K, 2010
)
0.63
" In particular, the deeper knowledge of kinetic-dynamic characteristics has allowed to highlight that high dosage approach in short term therapy might reveal as extremely interesting in a setting of critical patients."( [PK/PD profile and post-marketing surveillance of levofloxacin].
Pea, F, 2009
)
0.6
"A questionnaire regarding what antitubercular drugs, their dosage and for how long was asked to attending faculty in an International Conference on musculoskeletal infections."( A survey of prescribing pattern for osteoarticular tuberculosis: orthopaedic surgeons' and infectious disease experts' perspective.
Agarwal, A; Arora, A; Kumar, S, 2009
)
0.35
" To overcome these problems of conventional dosage form, novel drug delivery systems are explored like nanoparticles."( Biodegradable levofloxacin nanoparticles for sustained ocular drug delivery.
Ali, A; Aqil, M; Bhatnagar, A; Gupta, H; Khar, RK; Mittal, G, 2011
)
0.71
" In the CCB, the pharmacokinetics of different ofloxacin dosing regimens were simulated."( Novel in vitro pharmacodynamic model simulating ofloxacin pharmacokinetics in the treatment of Pseudomonas aeruginosa biofilm-associated infections.
Elkhatib, WF; Noreddin, AM, 2009
)
0.87
" aeruginosa biofilm and the shedding planktonic cells in response to different ofloxacin dosing regimens were not parallel and this may explain the non-coincidence of microbiological and clinical outcomes with biofilm associated infections."( Novel in vitro pharmacodynamic model simulating ofloxacin pharmacokinetics in the treatment of Pseudomonas aeruginosa biofilm-associated infections.
Elkhatib, WF; Noreddin, AM, 2009
)
0.84
" The single method thus developed is applied for the quantification of levofloxacin both in aqueous humour as well as pharmaceutical dosage forms (i."( A single reversed-phase UPLC method for quantification of levofloxacin in aqueous humour and pharmaceutical dosage forms.
Ali, A; Aqil, M; Chander, P; Gupta, H; Khar, RK, 2010
)
0.83
" Aerosol administration of levofloxacin as in the form of the investigational formulation MP-376 results in higher concentrations in lung tissues that are higher than those that can be attained with oral or intravenous dosing of levofloxacin."( Levofloxacin reduces inflammatory cytokine levels in human bronchial epithelia cells: implications for aerosol MP-376 (levofloxacin solution for inhalation) treatment of chronic pulmonary infections.
Dudley, MN; Griffith, DC; Lomovskaya, O; Sabet, M; Tarazi, Z; Tsivkovskii, R, 2011
)
1.28
" This trial is based on the hypothesis that current anti-mycobacterial treatment schedules for TBM are not potent enough and that outcomes will be improved by increasing the CSF penetrating power of this regimen by optimising dosage and using additional drugs with better CSF penetration."( Intensified treatment with high dose rifampicin and levofloxacin compared to standard treatment for adult patients with tuberculous meningitis (TBM-IT): protocol for a randomized controlled trial.
Bang, ND; Caws, M; Chau, TT; Day, J; Dung, NH; Farrar, J; Heemskerk, D; Merson, L; Olliaro, P; Pouplin, T; Wolbers, M; Yen, NT, 2011
)
0.62
" Accumulating elimination rate of antofloxaxin from urine within 120 hours after the last dosing was 60."( Pharmacokinetic study of single and multiple oral dose administration of antofloxacin hydrochloride in healthy male volunteers.
Kang, ZS; Li, TY; Liu, Y; Lü, Y; Xiao, YH; Zhang, M; Zhu, Y, 2011
)
0.6
"Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing levofloxacin as the only active pharmaceutical ingredient (API) are reviewed."( Biowaiver monographs for immediate release solid oral dosage forms: levofloxacin.
Barends, DM; Cristofoletti, R; Dressman, JB; Fernandes, EF; Junginger, HE; Koeppe, MO; Kopp, S; Midha, KK; Shah, VP; Stavchansky, S; Storpirtis, S, 2011
)
0.79
" We had previously developed a mathematical modelling framework to describe the dynamics of bacterial populations under the effect of antimicrobials, which could facilitate the design of optimal dosing regimens."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
" Based on the best-fit model parameters, the likelihood of resistance development associated with various dosing regimens was predicted."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
"Bacterial regrowth and resistance development were observed with suboptimal dosing regimens."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
"Our model was found to be reasonable in characterizing biphasic killing of fluoroquinolones and predicting dosing regimens to suppress resistance development."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
" C3H/HeOuJ mice were dosed by oral gavage with diclofenac (DF), APAP, AMAP, OFLX, MET, or CMZ."( Oral exposure to drugs with immune-adjuvant potential induces hypersensitivity responses to the reporter antigen TNP-OVA.
Bleumink, R; Boon, L; Fiechter, D; Hassing, I; Kwast, LM; Ludwig, IS; Pieters, RH, 2011
)
0.37
"The purpose of the study was to evaluate pharmacokinetic characteristics of antofloxacin hydrochloride, a new fluoroquinolone antibiotic, during a multiple, intravenous dosing regimen."( Pharmacokinetics of antofloxacin hydrochloride in healthy male subjects after multiple intravenous dose administration.
Kang, Z; Li, T; Liang, J; Liu, Y; Lu, Y; Wang, J; Xiao, Y; Zhang, M, 2011
)
0.91
" This was despite a longer duration of treatment at a higher dosage in patients infected with isolates with an MIC≥0."( The influence of reduced susceptibility to fluoroquinolones in Salmonella enterica serovar Typhi on the clinical response to ofloxacin therapy.
Baker, S; Campbell, JI; Chinh, NT; Farrar, JJ; Hien, TT; Parry, CM; Vinh, H; Wain, J, 2011
)
0.58
"Being controlled release dosage forms, tablets allow an improved absorption and release profiles of Ofloxacin."( Formulation and in vitro evaluation of ofloxacin-ethocel controlled release matrix tablets prepared by wet granulation method: influence of co-excipients on drug release rates.
Ahmad, K; Hussain, A; Jan, SU; Khan, GM; Rehman, A; Shah, K; Shah, S, 2011
)
0.85
" An in vitro infection model was used to simulate free pulmonary fluctuating concentrations expected after multiple dosing regimens of both drugs in humans or constant multiples of the minimum inhibitory concentration."( Pharmacokinetic/pharmacodynamic modelling of the bactericidal activity of free lung concentrations of levofloxacin and gatifloxacin against Streptococcus pneumoniae.
Dalla Costa, T; de Andrade, C; Tasso, L, 2011
)
0.58
" Due to the high antibiotic dosage requirement in anti-biofilm therapy, the most suitable formulation for this purpose is the antibiotic nanoparticles themselves, instead of the more extensively studied antibiotic-loaded nano-carriers, which often exhibit low drug loading."( Green preparation of antibiotic nanoparticle complex as potential anti-biofilm therapeutics via self-assembly amphiphile-polyelectrolyte complexation with dextran sulfate.
Cheow, WS; Hadinoto, K, 2012
)
0.38
" Using a similar dosing selection pressure, the emergence of levofloxacin resistance was delayed in a strain with acrAB deleted compared to the isogenic parent."( Temporal interplay between efflux pumps and target mutations in development of antibiotic resistance in Escherichia coli.
Hu, M; Ledesma, KR; Singh, R; Swick, MC; Tam, VH; Yang, Z; Zechiedrich, L, 2012
)
0.62
"The series is part of an ongoing randomised controlled trial assessing rechallenge dosing following TB-associated cutaneous ADR."( Multiple drug hypersensitivity reactions to anti-tuberculosis drugs: five cases in HIV-infected patients.
Dheda, K; Lehloenya, RJ; Todd, G; Wallace, J, 2012
)
0.38
"We performed plasma dosage for each antibiotic in patients with a bone and joint infection requiring treatment with a levofloxacin and rifampicin combination."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
0.85
" Just after dosing of OFLX, hindlimb unloading was performed for 0, 2, 4, or 8 h by a tail-suspension method."( Effect of body-weight loading onto the articular cartilage on the occurrence of quinolone-induced chondrotoxicity in juvenile rats.
Goto, K; Goto, M; Imaoka, M; Jindo, T; Kikuchi, I; Suzuki, T; Takasaki, W, 2013
)
0.39
"Levofloxacin dosing regimens with low AUC/MIC ratios select for efflux pump overexpression, leading to fluoroquinolone resistance."( Comparative antibacterial effects of moxifloxacin and levofloxacin on Streptococcus pneumoniae strains with defined mechanisms of resistance: impact of bacterial inoculum.
Bowker, KE; Garvey, MI; Macgowan, AP; Noel, AR; Tomaselli, SG, 2013
)
1.26
" Patients were administered LVFX 500mg, orally, once a day and the dosage period was seven days."( [Efficacy and safety of levofloxacin to non-gonorrheal urethritis].
Hosobe, T; Kato, T; Onodera, S; Onoe, Y; Yoshida, M, 2012
)
0.68
" Moreover, in this study, smart control over the pH conditions of the oxidation system via different modes of Oxone dosage resulted in the selective degradation of the functional sites of OFX molecule, where it was shown that the SO4 (-•)-driven destruction of the quinolone moiety of OFX molecule favored the neutral pH conditions."( Oxidation of ofloxacin by Oxone/Co(2+): identification of reaction products and pathways.
Feng, J; Pi, Y; Song, M; Sun, J, 2014
)
0.77
" The designed ofloxacin niosomes with span 60 showed good physicochemical properties, good stability, improved pharmacokinetic parameters, prolonged action and improved bioavailability than the commercially available conventional dosage form which might be a potential carrier system to improve the patient compliance and reduce the side effects."( Design and characterization of ofloxacin niosomes.
Balasundaram, J; Dhandayuthapani, B; Natesan, G; Natesan, S; Perumal, P; Ramalingam, N, 2013
)
1.04
" (99m)Tc-Ofloxacin served as a good tracer for studying the pharmacokinetics of three controlled release mucoadhesive dosage forms by gamma scintigraphy studies."( Preparation and evaluation of three mucoadhesive dosage forms using (99m)Tc-Ofloxacin.
Chakraborti, CK; Mukherjee, A; Sahoo, S; Samuel, G; Sarma, HD, 2014
)
1.05
"To prolong the residence time of dosage forms within gastrointestinal trace until all drug released at desired rate was one of the real challenges for oral controlled-release drug delivery system."( Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent.
Chen, H; Ma, N; Qi, X; Rui, Y; Wu, Z; Yang, F, 2015
)
0.68
" It is not known whether the current internationally recommended pediatric dosage of 15 to 20 mg/kg of body weight achieves exposures reached in adults with tuberculosis after a standard 800-mg dose (adult median area under the concentration-time curve from 0 to 24 h [AUC0-24], 103 μg · h/ml)."( Pharmacokinetics and Safety of Ofloxacin in Children with Drug-Resistant Tuberculosis.
Castel, S; Dooley, KE; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Seddon, JA; Thee, S; Wiesner, L, 2015
)
0.7
"Two sensitive, accurate, and precise spectrophotometric methods have been developed and validated for the simultaneous estimation of ofloxacin (OFX), clotrimazole (CLZ), and lignocaine hydrochloride (LGN) in their combined dosage form (ear drops) without prior separation."( Simultaneous Estimation of Ofloxacin, Clotrimazole, and Lignocaine Hydrochloride in Their Combined Ear-Drop Formulation by Two Spectrophotometric Methods.
Bodiwala, K; Kalyankar, G; Marolia, B; Patel, Y; Prajapati, P; Shah, S, 2017
)
0.96
" The aim of our study was to establish the kinetics of dissolution rate process of ofloxacin optical isomers (S-(-) and R-(+)-ofloxacin) from solid oral dosage forms using flow-through cell method (USP 4 method)."( STUDY OF OFLOXACIN ENANTIOMERS DISSOLUTION FROM SELECTED SOLID DOSAGE FORMS USING HIGH PERFORMANCE CAPILLARY ELECTROPHORESIS METHOD.
Kokot, ZJ; Lulek, J; Milanowski, B; Urbaniak, B, 2017
)
1.1
"The effect of AT on QT interval prolongation may not have been significant at the dosage of 400 mg."( Relationship between antofloxacin concentration and QT prolongation and estimation of the possible false-positive rate.
He, YC; Huang, JH; Li, LJ; Li, YF; Liang, LY; Wang, K; Xu, FY; Yang, J; Zheng, QS, 2020
)
0.87
"Bacterial regrowth was observed under exposure to clinically relevant dosing regimens in the dynamic in vitro infection model."( Quantification of persister formation of Escherichia coli leveraging electronic cell counting and semi-mechanistic pharmacokinetic/pharmacodynamic modelling.
Kloft, C; Michelet, R; Seeger, J, 2021
)
0.62
" The mimicked dosing regimens did not eradicate the resistant isolates and enhanced persister formation to a strain-specific extent."( Quantification of persister formation of Escherichia coli leveraging electronic cell counting and semi-mechanistic pharmacokinetic/pharmacodynamic modelling.
Kloft, C; Michelet, R; Seeger, J, 2021
)
0.62
" Monte-Carlo simulations were used to evaluate the probability of target attainment (PTA) of different dosing regimens."( Development of a dosing-adjustment tool for fluoroquinolones in osteoarticular infections: The Fluo-pop study.
Arvieux, C; Bellissant, E; Comets, E; Fily, F; Foulquier, JB; Huten, D; Jullien, V; Laviolle, B; Lemaitre, F; Petitcollin, A; Polard, JL; Revest, M; Tattevin, P; Tron, C; Verdier, MC, 2021
)
0.62
" The fast capillary action of the porous structure enabled controllable loading and sustained release of ofloxacin and bovine albumin at a high loading dosage of 79."( Fabrication of "Spongy Skin" on Diversified Materials Based on Surface Swelling Non-Solvent-Induced Phase Separation.
Fang, Y; Huang, WP; Ji, J; Qian, HL; Ren, KF; Wang, J; Xu, ZK; Yu, WJ; Zou, LY, 2021
)
0.84
" The optimal removal for ozone dosing range was nitrate (9."( Efficient removal of ibuprofen and ofloxacin pharmaceuticals using biofilm reactors for hospital wastewater treatment.
Ahmed, S; Alam, SS; Ali, I; Bokhari, A; Farooqi, IH; Khan, AH; Khan, NA; Mubashir, M, 2022
)
1
" Recently, the combination of nanomaterial-loaded antibiotics with photothermal therapy showed the efficient antibacteria ability under a low dosage of antibiotics."( Ofloxacin-loaded HMPB NPs for Klebsiella pneumoniae eradication in the surgical wound with the combination of PTT.
Fan, J; Liu, B; Liu, T; Liu, X; Tang, D; Tong, C; Yang, X; Yang, Y; Zhong, G; Zhong, X, 2022
)
2.16
" The Day-1 dosing rates for ciprofloxacin and ofloxacin should be considered separately, and the regimes suggested in published guidelines and case studies may need be re-considered in light of the findings of this review."( The clinical treatment of bacterial keratitis: A review of drop instillation regimes.
Essex, RW; Maddess, T; Pearce, JG, 2022
)
1
"Uniformity of dosage unit (UDU) test is widely used to assess the quality, safety, and effectiveness of dosage forms in unit doses."( Measurement uncertainty for < 905 > Uniformity of Dosage Units tests using Monte Carlo and bootstrapping methods - Uncertainties arising from sampling and analytical steps.
Lourenço, FR; Martins, MT, 2024
)
1.44
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (5)

ClassDescription
3-oxo monocarboxylic acid
N-methylpiperazine
N-arylpiperazine
oxazinoquinolineAny organic heterotricyclic compound based on a skeleton comprised of an oxazine ring fused onto a quinoline system.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency112.20200.003245.467312,589.2998AID2517
Chain A, HADH2 proteinHomo sapiens (human)Potency17.55950.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency17.55950.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency17.39550.177814.390939.8107AID2147
Chain A, Ferritin light chainEquus caballus (horse)Potency31.62285.623417.292931.6228AID2323
thioredoxin reductaseRattus norvegicus (Norway rat)Potency29.75060.100020.879379.4328AID488772; AID588453; AID588456
TDP1 proteinHomo sapiens (human)Potency19.76110.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.56480.011212.4002100.0000AID1030
EWS/FLI fusion proteinHomo sapiens (human)Potency20.93100.001310.157742.8575AID1259252; AID1259253
arylsulfatase AHomo sapiens (human)Potency4.25621.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency32.57330.035520.977089.1251AID504332
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency14.14060.001815.663839.8107AID894
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency32.64270.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency79.43283.548119.542744.6684AID743266
flap endonuclease 1Homo sapiens (human)Potency37.68580.133725.412989.1251AID588795
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency19.95260.251215.843239.8107AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)566.50000.11007.190310.0000AID1449628; AID1473738
DNA gyrase subunit AEscherichia coli K-12IC50 (µMol)1.50000.02390.56295.2300AID530379
DNA gyrase subunit BEscherichia coli K-12IC50 (µMol)1.50000.00500.43985.2300AID530379
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.505710.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.497310.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.498810.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.504610.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.506510.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.505710.0000AID71980; AID71981
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50 (µMol)28.00000.01502.467610.0000AID530368
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)28.00000.01503.477310.0000AID530368
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)1,414.03200.00091.901410.0000AID161281; AID243151; AID408340; AID576612; AID755684
GABA theta subunitRattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)IC50 (µMol)55.50000.00010.507510.0000AID71980; AID71981
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
streptokinase A precursorStreptococcus pyogenes M1 GASEC50 (µMol)3.69400.06008.9128130.5170AID1902
AlbuminHomo sapiens (human)Kd12.00000.08933.31358.0000AID557095
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
STE24Saccharomyces cerevisiae (brewer's yeast)AC501.95001.95006.687011.8600AID488815
CAAX prenyl proteaseSaccharomyces cerevisiae S288CAC50100.00001.079017.990668.9400AID488788
TrypsinSus scrofa (pig)AC509.26403.340016.705077.2200AID488789
DNA gyrase subunit AEscherichia coli K-12CC250.20000.20000.35000.5000AID530391
DNA gyrase subunit BEscherichia coli K-12CC250.20000.20000.35000.5000AID530391
DNA gyrase subunit BMycobacterium tuberculosis H37RvCC257.00002.00004.50007.0000AID530380
DNA gyrase subunit AMycobacterium tuberculosis H37RvCC257.00002.00004.50007.0000AID530380
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (75)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit AEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit AEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
response to antibioticDNA gyrase subunit AEscherichia coli K-12
chromosome organizationDNA gyrase subunit AEscherichia coli K-12
negative regulation of DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit BEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit BEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit BEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
response to antibioticDNA gyrase subunit BEscherichia coli K-12
chromosome organizationDNA gyrase subunit BEscherichia coli K-12
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (50)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
DNA bindingDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit AEscherichia coli K-12
protein bindingDNA gyrase subunit AEscherichia coli K-12
ATP bindingDNA gyrase subunit AEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit AEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit AEscherichia coli K-12
identical protein bindingDNA gyrase subunit AEscherichia coli K-12
DNA bindingDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit BEscherichia coli K-12
protein bindingDNA gyrase subunit BEscherichia coli K-12
ATP bindingDNA gyrase subunit BEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit BEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit BEscherichia coli K-12
metal ion bindingDNA gyrase subunit BEscherichia coli K-12
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
chromosomeDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
cytosolDNA gyrase subunit AEscherichia coli K-12
membraneDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit AEscherichia coli K-12
chromosomeDNA gyrase subunit BEscherichia coli K-12
cytoplasmDNA gyrase subunit BEscherichia coli K-12
cytosolDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit BEscherichia coli K-12
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1631)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID447218Antibacterial activity against Listeria monocytogenes ATCC 15313 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID562930Antimicrobial activity against Clostridium difficile CD07-259 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID209087Compound was tested for inhibition of the gram-negative organism Streptococcus faecalis MGH-21986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID127505In vitro antibacterial activity against glucose nonfermenter Moraxella bovis P-71011990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID391988Antibacterial activity against Staphylococcus aureus RN4220 containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1163980Antimycobacterial activity against isoniazid, rifampicin, ofloxacin and kanamycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 clinical isolate after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1230207Antibacterial activity against Bacillus cereus N258 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID530388Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB N464S mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID562782Antimicrobial activity against Chlamydia trachomatis L2/oflR harboring ompA gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID70428Compound was tested for antibacterial activity against gram negative Escherichia coli ML47071998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID510156Antimicrobial activity against Staphylococcus aureus ATCC 35218 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID1368746Antibacterial activity against Escherichia coli MTCC 443 at 1 ug/ml under overnight incubation condition by paper disc method2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Synthesis and biological evaluation of 1-amino isochromans from 2-bromoethyl benzaldehyde and amines in acid medium.
AID200881Tested in vitro against Salmonella Typhimurium IID971 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID563502Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 71 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID371460Antimicrobial activity against Bacillus subtilis ATCC 6633 after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID64885Tested for inhibitory activity against DNA gyrase supercoiling in Escherichia coli (KL-16)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID524824Antibacterial activity against erythromycin resistant Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID1230227Antibacterial activity against Enterococcus gallinarum N489 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID572525Antimicrobial activity against qnrS-positive Salmonella enterica serovar Corvallis isolate s2017 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID531337Antibacterial activity against MeXAB-OprM deficient Pseudomonas aeruginosa TNP077 selected after 1.0 ug/ml of azithromycin by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID371464Antimicrobial activity against Klebsiella pneumoniae RSHM 574 after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID1193922Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID428985Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 104 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID733008Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 1 hr at 37 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID128018Compound was tested for Therapeutic effects on systemic infections on mice by peroral administration1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID395361Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID532981Antibacterial activity against Escherichia coli DH5alpha2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID1331878Antibacterial activity against Salmonella enterica ATCC 140282017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID206437In vitro antibacterial activity against clinical isolates of Staphylococcus aureus 18773 (gram-positive) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID1695812Antibacterial activity against Escherichia coli assessed as inhibition zone at 1 mg/ml measured after overnight incubation by disc diffusion method2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID1324013Permeability of the compound at 100 ug/ml after 16 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID293582Antibacterial activity against Klebsiella pneumoniae isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1274482Antibacterial activity against Escherichia coli JM 109 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID287371Antibacterial activity against Escherichia coli after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID203039Minimum inhibitory concentration required in vitro against Shigella1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID207258Tested in vitro for antibacterial activity against Staphylococcus aureus (FDA 209P JC-1)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1743440Antibacterial activity against Mycobacterium smegmatis measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID520423Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU18 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID1516026Antibacterial activity against Acinetobacter baumannii AB1901 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID572516Antimicrobial activity against qnrS-positive Salmonella enterica serovar Montevideo isolate s2944 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID530424Antimicrobial activity against Borrelia burgdorferi harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID164395Antimicrobial activity against the Pseudomonas aeruginosa K 799/61 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID322314Antibacterial activity against CTX-M group 1 enzyme producing Escherichia coli isolates assessed as percent resistant isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID1224525Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID498787Antimicrobial activity against ciprofloxacin-susceptible Streptococcus pyogenes harboring Asp91/Asn mutation in parC gene at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID352091Antimicrobial activity against Escherichia coli ATCC 25922 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID530384Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID540227Volume of distribution at steady state in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID163228Compound was tested for antibacterial activity against gram negative Proteus vulgaris No.331998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID1662846Antibacterial activity against Staphylococcus aureus ATCC 209p2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID1823665Apparent permeability across basolateral to apical side in human Caco-2 cells at 5 uM measured every 15 mins for 1 hr by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID316447Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 by agar dilution method2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID530383Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A, I85V, F96W and P101M mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID70860Compound was tested for inhibition of the gram-negative organism Escherichia cloacae HA 26461986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID429013Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT60 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID562927Antimicrobial activity against Clostridium difficile ATCC 43603-M1 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID164709Compound was tested for inhibition of the gram-negative organism Pseudomonas aeruginosa UI-181986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1653574Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.375 ug/ml in presence of 0.05 ug/ml rifabutin measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID562797Antimicrobial activity against Chlamydia trachomatis L2/tetR1 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1577333Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 9449/2007 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID572511Antimicrobial activity against Salmonella enterica serovar Typhimurium isolate s2878 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID562928Antimicrobial activity against Clostridium difficile ATCC 43603 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID550048Antibacterial activity against Escherichia coli assessed as inhibition of visible growth after 48 hrs by agar dilution method2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Conventional and microwave assisted synthesis of 2-oxo-4-substituted aryl-azetidine derivatives of benzotriazole: a new class of biological compounds.
AID1167608Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis XDR-TB after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
AID563228Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1274479Antibacterial activity against Bacillus subtilis ATCC 6633 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID1331879Antimycobacterial activity against Mycobacterium smegmatis MC2 1552017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID581497Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrB D500N mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID530409Antimicrobial activity against Mycobacterium tuberculosis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1230214Antibacterial activity against Enterococcus durans CIP 104999 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1485937Permeability of the compound in PBS/EtOH after 16 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1570739Antimicrobial activity against Listeria monocytogenes clinical isolate at 5 ug/disk incubated for 20 +/- 4 hrs by agar disk diffusion method2019Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21
Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1907629Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC2858 incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1331872Antibacterial activity against vancomycin-resistant Enterococcus2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID144565Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium smegmatis ATCC 19420 by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID530245Antimicrobial activity against apaH deficient Escherichia coli K-12 BW-25113 assessed as survival rate at 5 ug/ml after 6 hrs by time kill analysis2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Role of global regulators and nucleotide metabolism in antibiotic tolerance in Escherichia coli.
AID352095Antimicrobial activity against ceftriazone-resistant Bacillus subtilis after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID679031TP_TRANSPORTER: inhibition of DNP-SG uptakee (DNP-SG: 1 uM, OFLX: 10000 uM) in bile canalicular membrane vesicles from SD rat1998The Journal of pharmacology and experimental therapeutics, Mar, Volume: 284, Issue:3
Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats.
AID203167Tested in vitro against Serratia marcescens IAM1184 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID520871Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU57 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID9222Activity against Acinetobacter calcoaceticus (AC54)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID1377751Effective permeability of the compound after 2.5 hrs at 25 degC by PAMPA assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID371462Antimicrobial activity against Escherichia coli ATCC 25922 after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID1743467Inhibition of DNA gyrase in Escherichia coli ATCC 25922 assessed as elongation of bacterial cells at 2 ug/ml measured after 1.5 hrs by DAPI/FM 4-64 staining based confocal fluorescence microscopic analysis2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID694231Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID1138550In vivo antibacterial activity against Staphylococcus aureus in New zealand rabbit keratitis model assessed as suppression of conjuctival congestion, conjuctival chemosis, infiltration, operative ulcer area and depth at 3 mg/ml administered topically ever2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Haloemodin as novel antibacterial agent inhibiting DNA gyrase and bacterial topoisomerase I.
AID1653556Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.375 ug/ml in presence of 0.0062 ug/ml KRM-1648 measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID445446Oral bioavailability in human2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID385166Antimicrobial activity against Enterococcus faecalis by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID532988Antibacterial activity against Klebsiella aerogenes NCIM 22812010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID532987Antibacterial activity against Pseudomonas aeruginosa NCIM 5029 in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID1412154Bactericidal activity against methicillin-resistant Staphylococcus aureus 15 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID322316Antibacterial activity against CTX-M group 9 enzyme producing Escherichia coli isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID95540Tested in vitro for antibacterial activity against Klebsiella pneumoniae (B54)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID535837Antimicrobial activity against Pseudomonas aeruginosa GP20KT21 harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID562783Antimicrobial activity against Chlamydia suis S45/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1435653Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 7357/1998 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID69782Antibacterial activity against Escherichia coli (H560)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID429017Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG7 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID424879Antimicrobial activity against multidrug-resistant Enterobacter cloacae E705 bearing qnrB10 gene with aac(6)-IId-aadA1a integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID429022Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG152 harboring DNA gyrase A S83F and D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID67531Inhibition of growth of Entero. cloacae1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID557096Binding affinity to human alpha-1-acid glycoprotein assessed as compound binding sites level by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID209225In vitro antibacterial activity against Streptococcus faecalis 24731990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID1516028Antibacterial activity against Pseudomonas aeruginosa 25349 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID206368Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus faecalis MGH-21990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID581502Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA D94A mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID542140Antimicrobial activity against Salmonella enterica HN-GSS2007-0.033 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID1378880Effective permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID542146Antimicrobial activity against Escherichia coli DH10B harboring pBR322 with Salmonella enterica HN-GSS-2007-057 qnrS1 gene by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID1557280Antibacterial activity against Pseudomonas aeruginosa by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID559366Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID581500Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrB A90V and T539P mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID203037Minimum bactericidal concentration required in vitro against Shigella1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID209061In vitro antibacterial activity against Streptococcus epidermis 81990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID581510Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrB A90V and D500A mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1557279Antibacterial activity against Escherichia coli by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID656233Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1557287Antibacterial activity against Enterococcus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID563225Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1653573Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.75 ug/ml in presence of 0.2 ug/ml rifampin measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID133980In vivo protective dose (PD50) in mice against Escherichia coli Vogel when administered subcutaneously1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID395365Antibacterial activity against Listeria monocytogenes ATCC 15313 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID205965Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus aureus UC-761990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID352837Antimicrobial activity against Aspergillus fumigatus NCIM 902 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID70947In vitro antibacterial activity against clinical isolates of Escherichia coli 15 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID1412149Antibacterial activity against Staphylococcus epidermidis ATCC 35984 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID1502712Antimycobacterial activity against Mycobacterium avium isolate MAV3 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID574808Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 horboring rpoB S531L, katG R463L/E217G, gyrA D94N/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID562241Antimycobacterial activity against Mycobacterium smegmatis grown in carbon-limited broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID279820Antimicrobial activity against Mycobacterium tuberculosis H3Rv on day 72007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID563031Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1301203Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis harbouring Beijing genotype with combination of mutations of Ser 53-Leu 315 and Ser-Thr in rpoB and katG genes after 10 days by micro broth dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides.
AID1230244Antibacterial activity against Staphylococcus haemolyticus CIP 8156 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID530619Antimicrobial activity against Tropheryma whipplei harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1188153Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID1743471Inhibition of DNA gyrase in Mycobacterium smegmatis assessed as segmentation of bacterial cells at 2 ug/ml measured after 6 hrs by DAPI/FM 4-64 staining based confocal fluorescence microscopic analysis2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID530410Antimicrobial activity against Mycobacterium fortuitum harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID207385Inhibition of growth of Staphylococcus aureus (sensitive)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID67215Compound was tested for antibacterial activity against gram positive Enterococcus faecalis 13731998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID559579Antimicrobial activity against Parachlamydia acanthamoebae infected in Acanthamoeba castellanii amoeba cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID396101Antibacterial activity against Pseudomonas aeruginosa OCR1 overexpressing mexAB by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID530413Antimicrobial activity against Bacillus subtilis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1463957Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 4 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID530422Antimicrobial activity against Ehrlichia chaffeensis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559561Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID162775In vitro minimum inhibitory concentration against Pseudomonas aeruginosa (ATCC 27853)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID316451Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse spleen assessed as viable organisms at 50 mg/kg, ip after 35 days relative to control2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID530617Antimicrobial activity against Mycobacterium tuberculosis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID529671Antimicrobial activity against azide-resistant Escherichia coli J53 by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
ISEcp1-mediated transposition of qnrB-like gene in Escherichia coli.
AID530426Antimicrobial activity against Staphylococcus aureus harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID206283In vitro antibacterial activity against Staphylococcus aureus 209P JC-11990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID562939Effect on fbp69 gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID43924Compound was tested for antibacterial activity against gram negative Burkholderia cepacia 231998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID562784Antimicrobial activity against Chlamydia trachomatis J/6276/rifR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID562245Antimycobacterial activity against Mycobacterium smegmatis grown in nitrogen -limited broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID562788Antimicrobial activity against Chlamydia muridarum MoPn/rifRoflR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID523002Cytotoxicity against human 5637 cells assessed as mild induction of cell death by LDH release assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID349880Permeability across porcine brain lipid coated polyvinylidene fluoride membrane by PAMPA2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID563055Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1309353Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 24 hrs by microbroth dilution method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.
AID534424Antibacterial activity against Mycobacterium bovis BCG-Pasteur2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID557093Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID557094Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 1.6% gamma globulin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID521968Antibacterial activity against Campylobacter sp. assessed as resistance breakpoint by CLSI method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID563043Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID524825Antibacterial activity against erythromycin susceptible Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID563032Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1743462Antitubercular activity against Mycobacterium tuberculosis XDR measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID68846In vitro minimum inhibitory concentration against Escherichia coli KC-141993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID406846Antibacterial activity against Escherichia coli TOP10 containing pS1A plasmid expressing quinolone resistance determinant QnrB4 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1171213Antibacterial activity against tolC-deficient Escherichia coli2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID151536Tested in vitro against Pseudomonas aeruginosa IFO3445 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1152758Antimycobacterial activity against wild-type Mycobacterium tuberculosis H37Rv ATCC 27294 after 16 to 18 days by BACTEC 7H12B microdilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1672289Antibacterial activity against Escherichia coli assessed as bacterial growth inhibition after 24 hrs by CLSI protocol based broth microdilution assay
AID1823666Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco-2 cells at 5 uM measured every 15 mins for 1 hr by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID563040Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1695811Antibacterial activity against Pseudomonas aeruginosa assessed as inhibition zone at 1 mg/ml measured after overnight incubation by disc diffusion method2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID131700Effective dose against Escherichia coli KC14 strain in mouse1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID1230225Antibacterial activity against Enterococcus faecium N823 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID70926In vitro antibacterial activity against Escherichia coli P-51011990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID535838Antimicrobial activity against wild-type Pseudomonas aeruginosa GP20 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID530403Antimicrobial activity against Borrelia burgdorferi harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID562242Antimycobacterial activity against Mycobacterium smegmatis grown in nitrogen -limited broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID295112Antibacterial activity against Bacillus cereus ATCC 7064 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID574589Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 obtained from pus of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID406845Antibacterial activity against Escherichia coli TOP10 containing pS1B plasmid expressing quinolone resistance determinant QnrS1 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID498188Antibacterial activity against Stenotrophomonas maltophilia MBS108 containing both chromosomally and plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID572513Antimicrobial activity against Salmonella enterica serovar Mbandaka isolate s2159 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID293583Antibacterial activity against Pseudomonas aeruginosa isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1421886Effective permeability of the compound at 25 ug/ml after 18 hrs by BBB-PAMPA method2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID1562257Antimycobacterial activity against Mycobacterium smegmatis atR2 assessed as decrease in drug resistance development at 2 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID1435650Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID206643Tested for in vitro for antibacterial activity against 16 clinical isolated of methicillin-resistant Staphylococcus aureus1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID1174112Antimycobacterial activity against isoniazid, rifampin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1478786Permeability of the compound at 200 uL after 16 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors.
AID391987Antibacterial activity against Staphylococcus aureus RN4220 containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1743457Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Asp-94-Gly mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID433403Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID563048Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID164385Antibacterial activity against Pseudomonas aeruginosa (UI-18)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1347980Permeability of the compound in PBS/EtOH at 100 ug/ml after 12 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID530615Antimicrobial activity against Streptococcus pneumoniae harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1264447Permeability of the compound by PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID293590Antibacterial activity against Bacillus subtilis ATCC 6633 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1230212Antibacterial activity against Enterococcus casseliflavus N487 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID405120Antimicrobial activity against Escherichia coli TOP10 harbouring p0 plasmid expressing pCR-BluntII-TOPO2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID1152777Antimycobacterial activity against 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID117675Median protective dose against Escherichia coli, determined in acute, lethal systemic infection in female charles river CD-1 mice (sc)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID563017Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID433400Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID498190Antibacterial activity against Stenotrophomonas maltophilia MBS82 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID205546Minimum inhibitory concentration (MIC) against Staphylococcus aureus ATCC 137092003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Antibacterial activity of quinolone-macrocycle conjugates.
AID1730991Antitubercular activity against drug susceptible Mycobacterium tuberculosis V4207 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID563046Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563219Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425069Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae M7943 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID316445Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID1653575Antimicrobial activity against Mycobacterium leprae assessed as fractional inhibitory concentration index at 0.375 ug/ml in presence of 0.0125 ug/ml KRM-1648 measured at 4 weeks2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID542147Antimicrobial activity against Escherichia coli DH10B harboring pBR322 with Salmonella enterica HN-GSS-2007-057 qnrD gene by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID1230243Antibacterial activity against Staphylococcus epidermidis CIP 53124 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID396097Antibacterial activity against Staphylococcus aureus K1758-P by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID765109Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition at 2 ug/mL relative to control2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID530616Antimicrobial activity against Mycobacterium smegmatis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1113447Antibacterial activity against Proteus vulgaris assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID1174108Antimycobacterial activity against isoniazid, rifampin, ethambutol, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID532038Antimicrobial activity against azide-resistant Escherichia coli DH5alpha TrfPS012 harboring PMQR determinant qnrB22 by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID581509Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1653552Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.75 ug/ml in presence of 0.1 ug/ml rifampin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID563503Antimicrobial activity against cetylpyridinium chloride-sensitive Serratia marcescens 79 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID532982Antibacterial activity against Escherichia coli W3110 in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID52937Compound was tested for antibacterial activity against gram negative Citrobacter freundii KP-291998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID94051Tested in vitro against Klebsiella pneumoniae PCI-602 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID295121Antibacterial activity against Micrococcus luteus La 2971 at 5 ug by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID425072Antimicrobial activity against Escherichia coli DH10B expressing pCRQB10 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID563027Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID450458Antibacterial activity against Bacillus subtilis after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID559358Antimicrobial activity against compound-resistant Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID562829Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID696005Permeability of the compound after 4 hrs by PAMPA assay2012European journal of medicinal chemistry, Dec, Volume: 58Microwave-assisted synthesis of hydroxyphenyl nitrones with protective action against oxidative stress.
AID162914In vitro antibacterial activity against clinical isolates of Proteus morganii 27 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID530405Antimicrobial activity against Staphylococcus aureus harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID352089Antimicrobial activity against Klebsiella pneumoniae RSHM 574 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID406844Antibacterial activity against Escherichia coli TOP10 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID559552Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1823664Apparent permeability across apical to basolateral side in human Caco-2 cells at 5 uM measured every 15 mins for 1 hr by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID1113448Antibacterial activity against Escherichia coli assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID122923Minimum inhibitory concentration against gram-positive MI, Micrococcus luteus ATCC 9341.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID520873Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU69 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID450460Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID1167550Permeability of the compound in 70:30 PBS:EtOH by PAMPA-BBB assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1743461Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Asp-94-Gly/gyrB Asp-500-Asn mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1349194Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Natural product inspired library synthesis - Identification of 2,3-diarylbenzofuran and 2,3-dihydrobenzofuran based inhibitors of Chlamydia trachomatis.
AID1502710Antimycobacterial activity against Mycobacterium avium isolate MAV1 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID763998Antibacterial activity against Staphylococcus aureus ATCC 6538P assessed as diameter of inhibition zone at 1 mg/ml after 24 hrs by cup diffusion method (Rvb = 15 mm)2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.
AID562798Antimicrobial activity against Chlamydia muridarum MoPn/tetR14 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID428998Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1516020Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID542148Antimicrobial activity against Escherichia coli DH10B harboring p2007057 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID445445Permeability at pH 6.5 by PAMPA method2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
The permeation of amphoteric drugs through artificial membranes--an in combo absorption model based on paracellular and transmembrane permeability.
AID164712Compound was tested for its minimal inhibitory constant against Gram-negative microorganism Pseudomonas aeruginosa E-2 (Pa(E))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID532035Antimicrobial activity against azide-resistant Escherichia coli J53 TrcPS012 harboring PMQR determinant qnrB22 by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID559364Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1705959Effective permeability of compound at 100 ug/ml incubated for 20 hrs by PAMPA-BBB assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID78715Inhibition constant against DNA Gyrase isolated from Micrococcus luteus1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID1360040Antimicrobial activity against Escherichia coli after 18 to 20 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID206890Antibacterial activity against Staphylococcus aureus UC761988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID532033Antimicrobial activity against Citrobacter werkmanii PS012 expressing PMQR determinant qnrB22 gene by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID428990Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 45 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID498781Antimicrobial activity against mild ciprofloxacin-resistant Streptococcus pyogenes by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID164703Compound was tested for antibacterial activity against gram negative Pseudomonas aeruginosa PAO11998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID1662849Bactericidal activity against Bacillus cereus2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID562931Antimicrobial activity against Clostridium difficile 6269 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID205651Compound was tested for antibacterial activity against gram positive Staphylococcus aureus JS-11998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID41268In vitro minimum inhibitory concentration against Bacteroides fragilis (ATCC 25285)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID395360Antibacterial activity against Klebsiella pneumoniae UC57 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID530406Antimicrobial activity against Enterococcus faecalis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1055941Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 16 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID656231Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID164702Compound was tested for antibacterial activity against gram negative Pseudomonas aeruginosa KP-2541998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID535833Antimicrobial activity against Pseudomonas aeruginosa GP62KT41 harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID542141Antimicrobial activity against Salmonella enterica HN-GSS2007-0.056 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID279821Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 12007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID559578Antimicrobial activity against Waddlia chondrophila ATCC VR-1470 infected in Vero cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID559367Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID209279Antimicrobial activity against the streptococcus pyogenes EES 61 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID572147Antimicrobial activity against AcrAB-deficient Escherichia coli AG100AX harboring pBADomeganorM plasmid containing Neisseria gonorrhoeae multidrug efflux pump NorM after 18 to 24 hrs by two fold dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
AID324747Antibacterial activity against Mycobacterium leprae at 5 ug/mL after 11 to 18 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID1171217Antibacterial activity against wild-type Pseudomonas aeruginosa2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1743458Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Gly-88-Cys mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1412156Bactericidal activity against methicillin-resistant Staphylococcus epidermidis 57 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID206174Tested for in vitro for antibacterial activity against 16 clinical isolated of methicillin-resistant Staphylococcus aureus1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID1907643Antibiofilm activity against methicillin-resistant Staphylococcus aureus ATCC2858 assessed as minimal biofilm eradication concentration incubated for 24 hrs by crystal violet staining based assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID143122Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium tuberculosis clinical isolate 1104 by 90%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID1463956Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 1 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID70735Evaluated for minimum inhibitory concentration against gram-negative bacteria Escherichia coli Vogel1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID428994Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate ipt 32 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID133813Compound was evaluated for protective dose against the Streptococcus aureus UC-76 lethal infection following po administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID563050Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID198343Tested in vitro against Staphylococcus aureus FDA209P JC-1 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID352833Antimicrobial activity against Rhodotorula rubra NCIM 3174 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID208131In vitro minimum inhibitory concentration against Streptococcus pneumoniae (ATCC 6301)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID1557295Cmax in human at 0.4 g, po bid2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID205596In vitro minimum inhibitory concentration against gram-positive Se, Staphylococcus epidermidis IAM 1296.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID665368Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate at 10 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID498782Antimicrobial activity against ciprofloxacin-susceptible Streptococcus pyogenes harboring Asp91/Asn mutation in parC gene by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID563012Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID423635Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs2009Journal of natural products, Apr, Volume: 72, Issue:4
Terpenoids from Toona ciliata.
AID1331871Antibacterial activity against methicillin-resistant Staphylococcus aureus2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID1173784Inhibition of Mycobacterium tuberculosis DNA gyrase using relaxed pBR322 as substrate after 30 mins by supercoiling assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID581504Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA D94N mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID63896Activity against Enterobacter aerogenes (ATCC 13048)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID428993Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 51 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID316449Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35801 infected CD1 mouse lungs assessed as viable organisms at 50 mg/kg, ip after 35 days relative to control2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID151670Minimum inhibition concentration against Pseudomonas aeruginosa U-31 strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID733007Inhibition of Mycobacterium leprae DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 2 hrs at 30 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID163048Inhibition of growth of Proteus rettgeri1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID563338Induction of Cwp84 protease expression in Clostridium difficile CD196 M1 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1662848Antibacterial activity against Bacillus cereus2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID563337Induction of Cwp84 protease expression in Clostridium difficile CD196 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID78688Inhibitory concentration in supercoiling inhibition Escherichia coli DNA gyrase assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID581506Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA G88A mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID510170Antimicrobial activity against Enterococcus faecalis ATCC 29212 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID1171215Antibacterial activity against wild-type Escherichia coli2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID427197Membrane permeability dissolved in PBS/EtOH (70:30) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID352621Antimicrobial activity against Salmonella Typhimurium NCIM 2501 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID1274481Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID1437026Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by agar dilution method2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Development of gallic acid formazans as novel enoyl acyl carrier protein reductase inhibitors for the treatment of tuberculosis.
AID559359Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID151530Tested in vivo against Pseudomonas aeruginosa E-2 in mice after peroral dose of drug with 0.5% sodium carboxy methyl cellulose1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1224521Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID530408Antimicrobial activity against Mycobacterium smegmatis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559564Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1193921Inhibition of Mycobacterium smegmatis DNA GyrB domain assessed as inhibition of inorganic phosphate release after 100 mins at room temperature by ATPase assay2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID352629Antimicrobial activity against Pseudomonas aeruginosa NCIM 2200 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1557286Antibacterial activity against Streptococcus pyogenes by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1173786Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID133979In vivo protective dose (PD50) in mice against Escherichia coli Vogel when administered perorally1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID428900Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation assessed as complete cell killing at 4 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID131401Oral efficacy against Streptococcus pyogenes A65 on Systemic Infections in Mice1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID1511118Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID581494Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrA D94G mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID287379Antibacterial activity against Pseudomonas aeruginosa after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID28899Calculated partition coefficient (clogP)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID117674Median protective dose against Escherichia coli, determined in acute, lethal systemic infection in female charles river CD-1 mice (po)1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID574790Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID209067Antibacterial activity against Streptococcus faecalis MGH-21988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID1331876Antibacterial activity against Klebsiella pneumoniae ATCC 277362017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1055939Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 20 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID71794Percentage of GABA-induced chloride currents with 10e-4 M 4-biphenylacetic acid1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID209462In vitro antibacterial activity against Streptococcus pyogenes A651990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID164704In vitro minimum inhibitory concentration against gram-negative Pa(E), Pseudomonas aeruginosa E-2.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID429023Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG168 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID562945Upregulation of cwp84 gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID165055In vitro antibacterial activity against clinical isolates of Pseudomonas aeruginosa 2437 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID40925Tested in vitro against Bacillus subtilis ATCC 6633 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID70564Compound was tested for in vitro antibacterial activity (minimum inhibition concentration) against gram-negative Ec(K), Escherichia coli KC-14.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID563224Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID293589Antibacterial activity against Escherichia coli ATCC 25922 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID574809Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 horboring rpoB H526Y, katG D329A/R463L, gyrA D94G/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID209730Inhibition of growth of Streptococcus pneumonia1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID1557284Antibacterial activity against Staphylococcus aureus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1188156Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 100 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID572523Antimicrobial activity against qnrS-positive Salmonella enterica serovar Corvallis isolate s2052 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1352674Effective permeability at 25 ug/ml after 16 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1174110Antimycobacterial activity against isoniazid, rifampin, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID563332Upregulation of fbp68 gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1295091Tuberculostatic activity against multi-drug resistant Mycobacterium tuberculosis isolates assessed as induction of penetration size stunting incubated for 10 days by vertical diffusion method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
AID1309354Antimycobacterial activity against Mycobacterium avium after 24 hrs by microbroth dilution method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.
AID285684Antimicrobial activity against Pseudomonas aeruginosa PAO1 with pvdS mutation after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID562800Antimicrobial activity against Chlamydia trachomatis F/70/rifR-tetR harboring rpoB gene and tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1743442Antibacterial activity against Mycobacterium marinum measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID530379Inhibition of Escherichia coli DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559361Antimicrobial activity against compound-resistant Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID530402Antimicrobial activity against Bacteroides fragilis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID429033Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT76 harboring wild type DNA gyrase A by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1230223Antibacterial activity against Enterococcus faecium N507 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID428995Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate ipt 33 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID530348Antimicrobial activity against azide-resistant Escherichia coli J53 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID1193920Inhibition of Mycobacterium tuberculosis DNA GyrA/B heterotetramer assessed as inhibition of pBR322 supercoiling after 30 mins by gel electrophoresis2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID530421Antimicrobial activity against Helicobacter pylori harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID534344Antimicrobial activity against Burkholderia pseudomallei Bp174 harboring mini-Tn7T-bpeR+ after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID71980Inhibition of [3H]muscimol binding to GABA A receptor 4-biphenylacetic acid at 10 e-4 M1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID1188155Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID532985Antibacterial activity against Escherichia coli MG16552010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID563018Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559362Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID530378Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA M74I and A83S mutant/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID531336Antibacterial activity against MeXAB-OprM deficient Pseudomonas aeruginosa TNP077 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID530411Antimicrobial activity against Tropheryma whipplei harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID293588Antibacterial activity against Pseudomonas aeruginosa ATCC 25853 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID429034Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation assessed as decrease in viable count at 4 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1163982Cytotoxicity against mouse RAW264.7 cells at 50 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID656227Antimycobacterial activity against isoniazid-, rifampin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID535836Antimicrobial activity against wild-type Pseudomonas aeruginosa GP37 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID450459Antibacterial activity against Serratia marcescens after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID164396Antimicrobial activity against the Pseudomonas aeruginosa K 799/WT by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID447216Antibacterial activity against Proteus vulgaris ATCC 8427 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID559576Antimicrobial activity against Waddlia chondrophila ATCC VR-1470 infected in Acanthamoeba castellanii amoeba cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID433404Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID687497Clearance in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID542145Antimicrobial activity against Escherichia coli DH10B harboring pBR322 with Salmonella enterica HN-GSS-2007-057 qnrA1 gene by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID733004Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB G89C mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID1730995Antitubercular activity against extensively drug resistance Mycobacterium tuberculosis R506 XDR by MABA2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID510157Antimicrobial activity against cephalosporin-resistant Acinetobacter baumannii by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID285682Antimicrobial activity against wild type Pseudomonas aeruginosa PAO1 after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID405121Antimicrobial activity against Escherichia coli TOP102007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID562244Antimycobacterial activity against Mycobacterium smegmatis grown in carbon-limited broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID1279155Permeability of the compound at 25 ug/ml at pH 7.4 after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID295100Antibacterial activity against Staphylococcus aureus ATCC 6538 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID534337Antimicrobial activity against Burkholderia pseudomallei Bp216 harboring mini-Tn7T after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID1907630Antibacterial activity against Escherichia coli incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID69619Antibacterial activity against Escherichia coli H5601988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID94363In vitro antibacterial activity against Klebsiella pneumoniae K-19661992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID530394Antimicrobial activity against Haemophilus influenzae harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID208737Minimum inhibitory concentration required in vitro against Streptococcus D1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID322313Antibacterial activity against CTX-M group 1 enzyme producing Escherichia coli isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID295097Antibacterial activity against Escherichia coli ATCC 11230 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID498191Antibacterial activity against Stenotrophomonas maltophilia MBS101 containing plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID70571Compound was tested for inhibition of the gram-negative organism Escherichia coli vogel1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID532980Antibacterial activity against Escherichia coli DH5alpha in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID71795Percentage of GABA-induced chloride currents with compound alone at 10 e-4 M1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID529159Antibacterial activity against Pseudomonas aeruginosa 100609 after 20 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID105366Concentration required to reduce the viability of mock-infected MT-4 cells by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID429006Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT37 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID530349Antimicrobial activity against Escherichia coli TOP10 harboring pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID205665In vitro minimum inhibitory concentration against gram-positive Sa (I), Staphylococcus aureus IID803.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID563215Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID53311Inhibitory effect on DNA gyrase supercoiling activity from Escherichia coli K-12 C6001990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID428987Antimicrobial activity against Salmonella enterica Serovar Typhi isolate nar 108 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563015Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID520875Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolates isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID205924Antimicrobial activity against the faecium ATCC 8043 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID1907628Antibacterial activity against Staphylococcus aureus ATCC6538 incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID429026Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG182 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID559365Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP1 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1174107Antimycobacterial activity against isoniazid, rifampin, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID665367Antitubercular activity against Mycobacterium tuberculosis H37Rv at 10 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID687499Drug excretion in rat urine2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID285683Antimicrobial activity against Pseudomonas aeruginosa PAO1 with rpoN mutation after 24 hrs2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID395778Antibacterial activity against ceftriaxone-resistant Bacillus subtilis isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID1557281Antibacterial activity against Klebsiella by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID391979Antibacterial activity against Enterococcus faecalis JH2-2-delta-pG1KT mutant by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID563051Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID293584Antibacterial activity against Escherichia coli isolate assessed after 24 hrs by by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1730992Antitubercular activity against multi drug resistance Mycobacterium tuberculosis V2475 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID395364Antibacterial activity against Mycobacterium smegmatis CCM 2067 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID498189Antibacterial activity against Stenotrophomonas maltophilia MBS109 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID428984Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 102 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID207175Antibacterial activity against Staphylococcus aureus (H228)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID559557Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1743441Antibacterial activity against Mycobacterium aurum measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1412157Bactericidal activity against Pseudomonas aeruginosa ATCC 9027 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID287377Antibacterial activity against Mycobacterium smegmatis after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID164706In vitro minimum inhibitory concentration against gram-negative Pa(I), Pseudomonas aeruginosa IFO 3445.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID529456Antimicrobial activity against Klebsiella pneumoniae containing PFGE clone A expressing beta-lactamase Oxa-48, TEM-1, SHV-12 and Oxa-9 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Spread of OXA-48-positive carbapenem-resistant Klebsiella pneumoniae isolates in Istanbul, Turkey.
AID391981Antibacterial activity against Enterococcus faecalis JH2-2-omega-pG1KT/pORI23::qnr-cat mutant with qnr gene complementation by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID65384Minimum inhibition concentration against Enterococcus faecalis LS-101 strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID392220Antibacterial activity against Lactococcus lactis IL-1419 containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID560590Antimicrobial activity against Pseudomonas aeruginosa isolate IMCJ798 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID535841Antimicrobial activity against wild-type Pseudomonas aeruginosa GP4 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID352805Antimicrobial activity against Bacillus cereus NCIM 2155 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID563212Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID637605Permeability of the compound by PAMPA2012European journal of medicinal chemistry, Feb, Volume: 48A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.
AID563023Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene and deletion of codons 678 and 679 in gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID96075Antimicrobial activity against the klebsiella pneumoniae 8045 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID530417Antimicrobial activity against Pseudomonas aeruginosa harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559558Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID762022Antibacterial activity against Pseudomonas aeruginosa 9027 measured every 24 hrs for 5 days by conventional dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Antimicrobial activity of imidazo[1,5-a]quinoxaline derivatives with pyridinium moiety.
AID559581Antimicrobial activity against Chlamydophila pneumoniae infected in Vero cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID563339Induction of Cwp84 protease expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID535840Antimicrobial activity against Pseudomonas aeruginosa GP4KT111 harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID1230215Antibacterial activity against Enterococcus faecalis CIP 103214 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID534418Antibacterial activity against Mycobacterium bovis BCG-Russia2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID550047Antibacterial activity against Staphylococcus aureus assessed as inhibition of visible growth after 48 hrs by agar dilution method2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Conventional and microwave assisted synthesis of 2-oxo-4-substituted aryl-azetidine derivatives of benzotriazole: a new class of biological compounds.
AID563026Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1230247Antibacterial activity against Staphylococcus saprophyticus CIP 76125 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1694879Permeability of compound after 16 hrs by PAMPA-BBB assay2020RSC medicinal chemistry, Feb-01, Volume: 11, Issue:2
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.
AID562792Antimicrobial activity against Chlamydophila caviae GPIC/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID559555Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID96228Compound was tested for in vitro antibacterial activity (minimum inhibition concentration) against gram-negative Kp, Klebsiella pneumoniae B54.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID1557283Antibacterial activity against Haemophilus influenzae with horse blood by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID206854Minimum bactericidal concentration required in vitro against Staphylococcus aureus1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID529160Antibacterial activity against Pseudomonas aeruginosa 100609 after 20 hrs by broth microdilution assay in presence of 250 ug/ml polyethylenimine2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID396104Antibacterial activity against Escherichia coli AG100 by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID1152781Ratio of MIC for 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant to MIC for wild-type Mycobacterium tuber2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1230220Antibacterial activity against Enterococcus faecium CIP 103014 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1360043Bactericidal activity against Bacillus cereus after 24 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID1909448Permeability of the compound by PAMPA-BBB assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis, and in vitro and in vivo characterization of new memantine analogs for Alzheimer's disease.
AID1516027Antibacterial activity against Acinetobacter baumannii AB1902 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1230226Antibacterial activity against Enterococcus gallinarum CIP 105985 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1743444Antibacterial activity against Pseudomonas aeruginosa measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID295109Antibacterial activity against Proteus vulgaris ATCC 8427 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID395363Antibacterial activity against Bacillus cereus ATCC 7064 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID1743456Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ala-90-Val mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1377752Effective permeability of the compound at 25 ug/ml by PAMPA assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents.
AID1516086Resistance index, ratio of MIC for antibacterial activity against ciprofloxacin-resistant Escherichia coli to MIC for Escherichia coli ATCC 25922 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID53321Inhibition of DNA gyrase supercoiling in Escherichia coli.1998Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
DNA gyrase inhibitory activity of ellagic acid derivatives.
AID67545Activity against Enterobacter aerogenes2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Search compounds with antimicrobial activity by applying molecular topology to selected quinolones.
AID530372Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID352092Antimicrobial activity against multidrug-resistant Escherichia coli after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID1463958Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 131 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID529670Antimicrobial activity against Escherichia coli J53 transconjugate by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
ISEcp1-mediated transposition of qnrB-like gene in Escherichia coli.
AID1274477Antibacterial activity against Methicillin-resistant Staphylococcus aureus N 315 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID429003Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT9 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID133954In vivo antibacterial activity against Escherichia coli (Vogel) in mice administered subcutaneously1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID510168Antimicrobial activity against extended spectrum beta lactamase expressing Klebsiella pneumoniae by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID1295090Tuberculostatic activity against Mycobacterium terrae assessed as induction of penetration size stunting incubated for 10 days by vertical diffusion method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
AID1230213Antibacterial activity against Enterococcus casseliflavus CIP 103018 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID532037Antimicrobial activity against azide-resistant Escherichia coli J53 by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID203276Antimicrobial activity against the Staphylococcus aureus 45 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID563039Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1577331Antimycobacterial activity against XDR Mycobacterium tuberculosis Praha 131 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID540231Dose normalised AUC in dog after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID557099Binding affinity to human serum albumin assessed as fraction of binding sites occupied by compound at >145 ug/ml by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID429012Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT54 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1173785Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID428979Antimicrobial activity against Salmonella enterica Serovar Typhi isolate E86 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID532034Antimicrobial activity against Citrobacter freundii S008 expressing PMQR determinant qnrB23 gene by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID450461Antibacterial activity against Escherichia coli after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID1662847Bactericidal activity against Staphylococcus aureus ATCC 209p2020Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13
Design and synthesis of amphiphilic 2-hydroxybenzylphosphonium salts with antimicrobial and antitumor dual action.
AID542142Antimicrobial activity against Salmonella enterica HN-GSS-2007-057 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID1224527Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1412158Bactericidal activity against Pseudomonas aeruginosa isolate 1 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID1516019Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1230221Antibacterial activity against Enterococcus faecium CIP 107387 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID562932Antimicrobial activity against Clostridium difficile 6425 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID429016Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG6 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID530385Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I and A83S mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID95885Antibacterial activity against Klebsiella pneumonia (MGH-2)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID163554Tested in vitro against Proteus vulgaris OX-19 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID559360Antimicrobial activity against compound-susceptible Coxiella burnetii Nine-Mile obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID395717Antibacterial activity against Escherichia coli DH10B containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID162777In vitro minimum inhibitory concentration against Pseudomonas aeruginosa IFO 34451993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID206284In vitro antibacterial activity against Staphylococcus aureus 507741990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1309358Acute toxicity in po dosed mouse2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID562240Antimycobacterial activity against Mycobacterium smegmatis grown in Luria-Bertani broth medium assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID198342Tested in vivo against Staphylococcus aureus IID803 in mice after peroral dose of drug with 0.5% sodium carboxy methyl cellulose1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1230241Antibacterial activity against Staphylococcus aureus CIP 7625 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID293587Antibacterial activity against Klebsiella pneumoniae RSHM 574 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID162740Compound was tested for antibacterial activity against gram negative Proteus mirabilis JY-101998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID429028Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG259 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID96098Compound was tested for antibacterial activity against gram negative Klebsiella pneumoniae KC-11998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID574796Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID733009Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed as drug concentration causing =<1% reduction in bacterial growth incubated for 21 to 30 days by proportion method2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID1335284Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling activity using relaxed pBR322 as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1557285Antibacterial activity against Streptococcus pneumoniae by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1480942Permeability of the compound at pH 7.4 at 1 mg/ml after 4 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID530392Antimicrobial activity against Escherichia coli harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID324745Inhibition of Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as inhibition of pBR322 DNA supercoiling2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID521967Antibacterial activity against Campylobacter coli assessed as resistant isolates by disk diffusion method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID1349196Antichlamydial activity against Chlamydia trachomatis serovar A 454/Bu infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Natural product inspired library synthesis - Identification of 2,3-diarylbenzofuran and 2,3-dihydrobenzofuran based inhibitors of Chlamydia trachomatis.
AID540225Volume of distribution at steady state in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID206812Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus pyogenes C2031990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID69626Antibacterial activity against Escherichia coli Vogel1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID205652Compound was tested for antibacterial activity against gram positive Staphylococcus aureus KP-90-31998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID1463962Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 8666/2010 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID530623Ratio of CC25 for Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I and A83S mutant to CC25 for Escherichia coli DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID510167Antimicrobial activity against Klebsiella pneumoniae RSKK 574 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID1730994Antitubercular activity against isoniazid/rifampin/levofloxacin/ofloxacin/kanamycin extensively drug resistance Mycobacterium tuberculosis TF274 XDR by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID271563Residual activity of human CK2 at 30 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Evaluation of 3-carboxy-4(1H)-quinolones as inhibitors of human protein kinase CK2.
AID694360Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis MS-115 under anaerobic condition by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID530347Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M carrying blaCTX-M-15 and pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID563341Induction of Cwp84 protease expression in Clostridium difficile 6269 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID207260Tested in vitro for antibacterial activity against Staphylococcus aureus (IID 803)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID395775Antibacterial activity against Pseudomonas aeruginosa ATCC 25853 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID563340Effect on Cwp84 protease expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID562785Antimicrobial activity against Chlamydia muridarum MoPn/oflR harboring ompA gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID534341Antimicrobial activity against Burkholderia pseudomallei Bp227 harboring deleted (bpeAB-oprA)::FRT gene after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID429027Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG258 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID198344Tested in vitro against Staphylococcus aureus IID803 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID131003Compound was tested for oral efficacy on systemic infections caused by Staphylococcus aureus IID803 in mice1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID1593376Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in extensively drug-resistant Mycobacterium tuberculosis TF274 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID540226Clearance in monkey after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID532036Antimicrobial activity against azide-resistant Escherichia coli J53 TrcS008 harboring PMQR determinant qnrB23 by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID144017Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium fortuitum (clinical isolate) by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID283088Antibacterial activity against Staphylococcus aureus SA1199B overexpressing NorA at 5 ug by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID352841Antimicrobial activity against Aspergillus parasiticus NCIM 904 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID572151Antimicrobial activity against AcrAB-deficient Escherichia coli AG100AX harboring pBADomegaydhE plasmid containing Escherichia coli multidrug efflux pump YdhE after 18 to 24 hrs by two fold dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
AID521966Antibacterial activity against Campylobacter jejuni assessed as resistant isolates by disk diffusion method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID534346Antimicrobial activity against Burkholderia pseudomallei Bp207 harboring deleted (bpeAB-oprA)::FRT gene after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID450457Antibacterial activity against Staphylococcus aureus after 24 hrs by twofold serial dilution method2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
Interaction of drug based binuclear mixed-ligand complexes with DNA.
AID1177575Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by microdilution method2014Journal of natural products, Aug-22, Volume: 77, Issue:8
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
AID562943Upregulation of slpA gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID200334Minimum bactericidal concentration required in vitro against Salmonella1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID1143269Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis 17003 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1295088Tuberculostatic activity against Mycobacterium tuberculosis H37Rv assessed as induction of penetration size stunting incubated for 10 days by vertical diffusion method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
AID1762620Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in bacterial growth after 6 to 8 days by green fluorescent protein microplate assay
AID163732Antibacterial activity against Providencia rettgeri M17711988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID1511119Permeability of the compound at 25 ug/ml by PAMPA-BBB assay2019European journal of medicinal chemistry, Oct-15, Volume: 180A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.
AID131400Oral efficacy against Pseudomonas aeruginosa 12 on Systemic Infections in Mice1990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID122920Antimicrobial activity against the micrococcus luteus 9341 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID1623120Effective permeability of the compound by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID574583Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID530618Antimicrobial activity against Mycobacterium fortuitum harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID65203Minimum inhibitory concentration against Escherichia coli KC14 strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID694359Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition assessed as growth inhibition at 2 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID1174106Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID540233Dose normalised AUC in human after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID67219Compound was tested for its minimal inhibitory constant against Gram-positive microorganism Enterococcus faecalis IID682 (Ef)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID733005Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB A91V mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID95891Inhibition of growth of Klebsiella pneumonia1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID1360037Antimicrobial activity against Staphylococcus aureus after 18 to 20 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID1230238Antibacterial activity against Staphylococcus aureus CIP 53154 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1773264Permeability of the compound at 100 ug/ml incubated for 18 hrs by PAMPA2021European journal of medicinal chemistry, Nov-05, Volume: 223Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1296388Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 131 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID405115Antimicrobial activity against Vibrio splendidus LGP32 expressing plasmid-mediated QnrS-like quinolone resistance determinants2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID563330Upregulation of cwp84 gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1653555Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.375 ug/ml in presence of 0.05 ug/ml rifabutin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID352096Antimicrobial activity against Staphylococcus aureus ATCC 25923 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID207390In vitro antibacterial activity against Staphylococcus aureus 209P JC-11992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1404015Permeability of the compound after 2.5 hrs by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID205805Compound was tested for its minimal inhibitory constant against Gram-positive microorganism Staphylococcus aureus IID 803 (Sa(I))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID572519Antimicrobial activity against qnrS-positive Salmonella enterica serovar Typhimurium isolate s2425 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID520870Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU47 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID70429Compound was tested for antibacterial activity against gram negative Escherichia coli NIHJ JC-21998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID681306TP_TRANSPORTER: increase in Vincristine intracellular accumulation (Vincristine: 0.03 uM, Ofloxacin: 21.7 mg/mL) in HL60R cells: flow cytometric analysis2000Antimicrobial agents and chemotherapy, Jun, Volume: 44, Issue:6
Interactions of ofloxacin and erythromycin with the multidrug resistance protein (MRP) in MRP-overexpressing human leukemia cells.
AID1595267Antibacterial activity against Escherichia coli assessed as inhibition zone incubated for 24 hrs by disk diffusion method relative to control2019European journal of medicinal chemistry, Jun-01, Volume: 171Insights into the chemistry and therapeutic potential of furanones: A versatile pharmacophore.
AID563024Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID297186Antibacterial activity against multidrug resistant Staphylococcus aureus 495892007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationships of phenyl-furanyl-rhodanines as inhibitors of RNA polymerase with antibacterial activity on biofilms.
AID755684Inhibition of human ERG current by patch clamp assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1503776Antichlamydial activity against Chlamydia pneumoniae K7 infected in HL cells after 70 hrs by fluorescent microscopic analysis2017Journal of natural products, 10-27, Volume: 80, Issue:10
Identification of Privileged Antichlamydial Natural Products by a Ligand-Based Strategy.
AID562787Antimicrobial activity against Chlamydia suis R19/tetR harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID163738Compound was tested for inhibition of the gram-negative organism Providencia rettgeri H17711986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID433580Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID442658Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID69479Minimum inhibitory concentration against Escherichia coli ATCC 259222003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
Antibacterial activity of quinolone-macrocycle conjugates.
AID200869In vitro minimum inhibitory concentration against Salmonella Typhimurium IID 9711993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1174109Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID765104Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID205964Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus aureus H2281990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID530419Antimicrobial activity against Methylovorus sp. harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID133812Compound was evaluated for protective dose against the Escherichia coli vogel lethal infection following sc administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1301204Cytotoxicity against human FEH cells after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides.
AID534338Antimicrobial activity against Burkholderia pseudomallei Bp250 harboring mini-Tn7T-bpeA+B+ -oprB+ after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID209894Antibacterial activity against Streptococcus pneumoniae SV-11988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID1143266Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis 136570 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1174111Antimycobacterial activity against isoniazid, rifampin, ethambutol-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1435648Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID429010Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT48 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID542139Antimicrobial activity against Salmonella enterica HN-GSS2006-142 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID17991Bioavailability2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Search compounds with antimicrobial activity by applying molecular topology to selected quinolones.
AID1743448Antibacterial activity against Staphylococcus aureus measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID206632Compound was tested for the in vitro antibacterial activity (minimum inhibitory concentration) against 50% of clinical isolates of methicillin-resistant Staphylococcus aureus (MIC range)1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID574784Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2403 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID563041Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID530620Antimicrobial activity against Treponema pallidum harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID562940Effect on fbp69 gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1279139Permeability of the compound at 25 ug/ml at pH 7.4 after 16 hrs by PAMPA2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID530390Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA M74I and A83S mutant/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID656232Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID293585Antibacterial activity against Bacillus subtilis isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID530414Antimicrobial activity against Escherichia coli harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID352845Antimicrobial activity against Penicillium chrysogenum NCIM 707 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID498192Antibacterial activity against Stenotrophomonas maltophilia MBS100 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID1695809Antibacterial activity against Bacillus subtilis assessed as inhibition zone at 1 mg/ml measured after overnight incubation by disc diffusion method2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID763999Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 assessed as diameter of inhibition zone at 1 mg/ml after 24 hrs by cup diffusion method (Rvb = 16 mm)2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID559556Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP6 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1129167Permeability of the compound by PAMPA2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis.
AID287375Antibacterial activity against Micrococcus luteus after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID581505Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA D94Y mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID529161FIC index, ratio of MIC for Pseudomonas aeruginosa 100609 in presence of 250 ug/ml polyethylenimine to MIC for Pseudomonas aeruginosa 1006092008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID429004Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT15 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID206825Compound was tested for antibacterial activity against gram positive Staphylococcus pyogenes cook1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID285687Increase in GFP tagged vqsR protein expression in Pseudomonas aeruginosa PAO1 with rpoN mutation at 8 ug/ml by flow cytometry relative to wild type2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID202106Minimum inhibition concentration against Streptococcus pneumoniae Type I strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID1201746Permeability of the compound after 16 hrs by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
AID1113446Antibacterial activity against Salmonella enterica subsp. enterica serovar Typhi assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID429030Antimicrobial activity against Salmonella enterica Serovar Typhi isolate BL 21801 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID530423Antimicrobial activity against Bacteroides fragilis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID279818Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774A.1 macrophages2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID557091Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 4% human serum albumin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID433581Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A G89C mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1230210Antibacterial activity against Corynebacterium striatum N840 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID78707MIC at which cleaved DNA (linear) is observed at an intensity relative to oxolinic acid at 10 ug/mL by using Gyrase Induced DNA-Cleavage assay1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID428901Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation assessed as complete cell killing at 4 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1264455Permeability of the compound by high throughput PAMPA method2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID530346Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M plasmid carrying blaCTX-M-15 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID563209Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563029Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID572150Antimicrobial activity against AcrAB-deficient Escherichia coli AG100AX harboring pBAD plasmid after 18 to 24 hrs by two fold dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
AID405118Antimicrobial activity against Escherichia coli TOP10 harbouring pS1 plasmid expressing quinolone resistant QnrS1 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID395772Antibacterial activity against Klebsiella pneumoniae isolate containing extended spectrum beta lactamase after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID1730993Antitubercular activity against isoniazid/rifampin resistance Mycobacterium tuberculosis KZN494 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID563334Upregulation of slpA gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID691688Antibacterial activity against Bartonella henselae infected in african green monkey Vero cells by immunofluorescence staining2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Studies on the antimicrobial properties of N-acylated ciprofloxacins.
AID524826Antibacterial activity against erythromycin resistant Campylobacter sp. assessed as resistance breakpoint by CLSI method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID1331869Antibacterial activity against Bacillus subtilis 1682017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID203190In vitro antibacterial activity against Shigella flexneri 2a EW-101992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID449435Antimycobacterial activity against Mycobacterium tuberculosis XDR infected in MDBK by BACTEC analysis2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Pentacyclo-undecane derived cyclic tetra-amines: synthesis and evaluation as potent anti-tuberculosis agents.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID352825Antimicrobial activity against Aspergillus niger NCIM 902 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID74727Antibacterial activity against five Gram-negative bacteria1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID1743449Antibacterial activity against Klebsiella pneumoniae measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID530391Inhibition of Escherichia coli DNA gyrase GyrA/GyrB assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID574802Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID765112Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1152776Antimycobacterial activity against 2-oxo-1-(2-(4-((3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino)piperidin-1-yl)ethyl)-1,2-dihydroquinoline-7-carbonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA A74V mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID763997Antibacterial activity against Shigella flexneri ATCC 15391 assessed as diameter of inhibition zone at 1 mg/ml after 24 hrs by cup diffusion method (Rvb = 17 mm)2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.
AID524827Antibacterial activity against erythromycin susceptible Campylobacter sp. assessed as resistance breakpoint by CLSI method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID562828Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID535842Antimicrobial activity against Pseudomonas aeruginosa PAO1 SO20 harboring mexAB-oprM gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID133807Compound was evaluated for protective dose against Streptococcus pneumoniae SV-1 lethal infection following sc administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID530369Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID581503Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA D94G mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID67217In vitro minimum inhibitory concentration against gram-positive Ef Enterococcus faecalis IID 682.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID1230219Antibacterial activity against Enterococcus faecalis N520 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID429024Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG169 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID498187Antibacterial activity against Stenotrophomonas maltophilia D457 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID510169Antimicrobial activity against methicillin-resistant Staphylococcus aureus by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID563218Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1557282Antibacterial activity against Bacteroides fragilis by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1390097Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 50 ug/ml after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis.
AID1315652Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured daily for 8 days by GFP-based fluorescence assay2016Journal of natural products, 06-24, Volume: 79, Issue:6
Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.
AID535834Antimicrobial activity against wild-type Pseudomonas aeruginosa GP62 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID428982Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT29 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID295853Antimicrobial activity against Streptococcus pyogenes KUKEM676 by disk diffusion method at 10 ug/disc2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID395780Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID206370In vitro minimum inhibitory concentration against Streptococcus faecalis (ATCC 29212)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID694367Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis MS-115 under anaerobic condition assessed as growth inhibition at 2 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID96099Compound was tested for antibacterial activity against gram negative Klebsiella pneumoniae No.421998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID687496Half life in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID428978Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate B111 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID562794Antimicrobial activity against Chlamydia trachomatis J/6276/oflR-rifR1 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1502706Antimycobacterial activity against Mycobacterium avium 104 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID687493Oral bioavailability in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID96230Compound was tested for its minimal inhibitory constant against Gram-negative microorganism Klebsiella pneumoniae B54 (Kp)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID530427Antimicrobial activity against Enterococcus faecalis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID534421Antibacterial activity against Mycobacterium bovis BCG-Denmark2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID70427Compound was tested for antibacterial activity against gram negative Escherichia coli CSH2/RK11998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID207201In vitro minimum inhibitory concentration against Staphylococcus aureus (ATCC 29213)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID163786Tested in vitro for antibacterial activity against Pseudomonas aeruginosa (IFO 3445)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1231418Antibacterial activity against Bacillus cereus ATCC 14579 assessed as growth inhibition at 5 ug after 24 hrs by disc agar diffusion method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of caracasine acid derivatives.
AID295115Antibacterial activity against Mycobacterium smegmatis CCM 2067 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID396099Antibacterial activity against Staphylococcus aureus K1902 by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID1593377Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in extensively drug-resistant Mycobacterium tuberculosis R506 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID447215Antibacterial activity against Micrococcus luteus La 2971 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID572520Antimicrobial activity against qnrS-positive Salmonella enterica serovar Virginia isolate s2219 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1231420Antibacterial activity against Escherichia coli ATCC 35218 assessed as growth inhibition at 5 ug after 24 hrs by disc agar diffusion method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of caracasine acid derivatives.
AID206877Antibacterial activity against Staphylococcus aureus H-2281988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID433402Inhibition of Mycobacterium leprae DNA gyrase subunit A A91V mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID530407Antimicrobial activity against Streptococcus pneumoniae harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID396103Antibacterial activity against Escherichia coli AG102 overexpressing acrAB by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1577327Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 1 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID70781In vitro antibacterial activity against Escherichia coli NIH JC-21992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1672290Antibacterial activity against Pseudomonas aeruginosa assessed as bacterial growth inhibition after 24 hrs by CLSI protocol based broth microdilution assay
AID1412153Bactericidal activity against Staphylococcus aureus ATCC 6538 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID322318Antibacterial activity against CTX-M group 9 enzyme producing Escherichia coli isolates assessed as percent nonsusceptible isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID352821Antimicrobial activity against Proteus vulgaris NCIM 2027 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID535845Antimicrobial activity against Pseudomonas aeruginosa PAO1 KTL1 harboring oprD, mexAB-oprM gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID352801Antimicrobial activity against Bacillus subtilis NCIM 2063 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID1319973Permeability of the compound by PAMPA assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID429005Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT18 harboring DNA gyrase A S83F and D87G mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID207207In vitro minimum inhibitory concentration against Staphylococcus aureus IID 8031993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID563010Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID560259Antimicrobial activity against Salmonella enterica serovar Typhimurium STYM61/9 expressing qnrB19 gene variant carried by IncL/M-like plasmid by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID540229Volume of distribution at steady state in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID681771TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, OFLX: 2000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.
AID1230224Antibacterial activity against Enterococcus faecium N733 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1562256Antimycobacterial activity against Mycobacterium smegmatis atR40 assessed as decrease in drug resistance development at 2 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID560592Antimicrobial activity against multidrug resistant Pseudomonas aeruginosa isolate IMCJ2S1 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID563331Upregulation of slpA gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1413649Ratio of MIC for methicillin-resistant Staphylococcus aureus JCSC 4788 re-passaged at 24 hrs intervals for 20 times to MIC for methicillin-resistant Staphylococcus aureus JCSC 47882018MedChemComm, Oct-01, Volume: 9, Issue:10
Structural optimization and antibacterial evaluation of rhodomyrtosone B analogues against MRSA strains.
AID67549Antimicrobial activity against the enterobacter aerogenes ATCC 13048 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID510161Antimicrobial activity against Proteus mirabilis ATCC 7002 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID532990Antibacterial activity against Klebsiella pneumoniae NCIM 2883 assessed as growth inhibition in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID279841Drug level in Mycobacterium tuberculosis infected BALB/c mouse model at 225 to 115000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID64252Activity against Escherichia coli (K-12 C600)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID1478796Permeability of the compound by PAMPA-BBB assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Design, synthesis and biological activity of novel donepezil derivatives bearing N-benzyl pyridinium moiety as potent and dual binding site acetylcholinesterase inhibitors.
AID164873Evaluated for minimum inhibitory concentration against gram-negative bacteria Pseudomonas aeruginosa UI-181990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID1324014Permeability of the compound at 25 ug/ml after 18 hrs by PAMPA-BBB method2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Neuroprotective effects of benzyloxy substituted small molecule monoamine oxidase B inhibitors in Parkinson's disease.
AID535846Antimicrobial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID279817Antimicrobial activity against Mycobacterium tuberculosis H37Rv in 7H9 broth2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID207206In vitro minimum inhibitory concentration against Staphylococcus aureus FDA 209P JC-11993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID65221Minimum inhibition concentration against Escherichia coli NIHJ JC-2 strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID1390094Antimycobacterial activity against active form of Mycobacterium tuberculosis H37Rv measured after 7 days by alamar blue assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis.
AID687494Cmax in rat at 10 mg/kg, iv2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID428986Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 107 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1516024Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID68976Minimum concentration of the drug needed to produce linear DNA at an intensity relative to oxolinic acid(at 10 ug/mL)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID530387Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID534339Antimicrobial activity against Burkholderia pseudomallei 1026b after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID1056992Permeability of the compound by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
AID1273398Anti-tubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294T after 7 days by mircodilution method2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID285686Increase in vqsR gene expression in Pseudomonas aeruginosa PAO1 with rpoN mutation at 8 ug/ml relative to wild type2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID133817Compound was evaluated for protective dose against the Streptococcus pneumoniae SV-1 lethal infection following po administration1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1335283Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in BL21(DE3)pLysS cells assessed as inhibition of DNA supercoiling activity in presence of ATP measured after 30 mins by malachite green dye based assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID70570Compound was tested for inhibition of the gram-negative organism Escherichia coli H5601986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID405117Antimicrobial activity against Escherichia coli TOP10 harbouring pVS2 expressing quinolone resistant Vibrio splendidus LGP32 QnrVS2 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID71070Concentration required to produce linear DNA from closed circular DNA by the denaturation of the drug-gyrase-DNA complex1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID68013Antibacterial activity against Enterobacter cloacae MA26461988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID572522Antimicrobial activity against qnrA-positive Salmonella enterica serovar Mbandaka isolate s2093 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID94137Activity against Klebsiella pneumoniae (PCI-602)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID563208Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID531332Antibacterial activity against Pseudomonas aeruginosa PAO4290 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID391985Inhibition of Escherichia coli DNA gyrase-mediated Escherichia coli pBR322 DNA supercoiling at 1 ug/mL by agarose gel electrophoresis2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID203278Antimicrobial activity against the Staphylococcus epidermis 3519 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID581513Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA A90V and D94G mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID530244Antimicrobial activity against Escherichia coli K-12 BW-25113 assessed as survival rate at 5 ug/ml after 6 hrs by time kill analysis2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Role of global regulators and nucleotide metabolism in antibiotic tolerance in Escherichia coli.
AID69951Antimicrobial activity against the Escherichia coli H560 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID534343Antimicrobial activity against Burkholderia pseudomallei Bp173 harboring mini-Tn7T after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID563045Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID206197Tested in vitro for antibacterial activity against Staphylococcus epidermidis (IAM 1296)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID535844Antimicrobial activity against Pseudomonas aeruginosa PAO1 KTS harboring mexAB-oprM gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID68849In vitro minimum inhibitory concentration against Escherichia coli (ATCC 1-25922)1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID530377Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA A83S mutant/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1557288Antibacterial activity against Clostridium perfringens by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID279839Ratio of fraction AUC in Mycobacterium tuberculosis infected BALB/c mouse to MIC in Mycobacterium tuberculosis infected BALB/c mouse model at 225 to 115000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID530412Antimicrobial activity against Treponema pallidum harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID531334Antibacterial activity against Pseudomonas aeruginosa TNP030 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID1412155Bactericidal activity against Staphylococcus epidermidis ATCC 35984 incubated for 24 hrs followed by replating on Mueller hinton agar plates and measured after 24 hrs2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID563030Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID447080Antibacterial activity against Escherichia coli ATCC 11230 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID1163979Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID563216Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID447219Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID1113451Antibacterial activity against Staphylococcus aureus assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID1421885Effective permeability of the compound at 1 mg/ml after 4 hrs by BBB-PAMPA method2018European journal of medicinal chemistry, Oct-05, Volume: 158Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
AID114660Compound was evaluated for oral Pseudomonas aeruginosa E-21992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID371463Antimicrobial activity against Escherichia coli isolate after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID532039Antimicrobial activity against azide-resistant Escherichia coli DH5alpha TrfS008 harboring PMQR determinant qnrB23 by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID1516029Antibacterial activity against Staphylococcus aureus 11011 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID520872Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU67 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID572517Antimicrobial activity against qnrS-positive Salmonella enterica serovar Braenderup isolate s2856 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID559363Antimicrobial activity against compound-susceptible Coxiella burnetii Q212 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID208946Inhibition of growth of Streptococcus pyogenes1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID563009Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID7869250% inhibitory concentration against DNA-gyrase1988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID1516023Antibacterial activity against Escherichia coli ATCC 25922 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID562944Upregulation of fbp68 gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID429007Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT40 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1230216Antibacterial activity against Enterococcus faecalis CIP 104676 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID64889Tested in vitro for antibacterial activity agains Escherichia coli (NIHJ JC-2)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1412150Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 57 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID395715Antibacterial activity against Lactococcus lactis IL-1419 containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID563016Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID208740Antimicrobial activity against the streptococcus agalactiae CMX 508 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID428991Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 46 harboring DNA gyrase A D87G mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563333Upregulation of cwp84 gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID424862Antimicrobial activity against carbapenem-susceptible Pseudomonas aeruginosa clinical isolate assessed as resistant isolates2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Molecular epidemiology and mechanisms of carbapenem resistance in Pseudomonas aeruginosa isolates from Spanish hospitals.
AID1295089Tuberculostatic activity against Mycobacterium avium assessed as induction of penetration size stunting incubated for 10 days by vertical diffusion method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID151057Activity against Pseudomonas aeruginosa (E-2)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID563336Induction of Cwp84 protease expression in Clostridium difficile 6425 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID427198Membrane permeability dissolved in PBS/EtOH (80:20) mixture by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID352094Antimicrobial activity against Bacillus subtilis ATCC 6633 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID198023Activity against Streptococcus faecalis (IID 682)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1480849Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment.
AID70770Inhibition of growth of Escherichia coli H5601988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID429036Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT18 harboring DNA gyrase A S83F and D87G mutation assessed as decrease in viable count at 4 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID201406Minimum inhibitory concentration against Staphylococcus aureus Smith1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID68172Compound was tested for antibacterial activity against gram negative Enterobacter cloacae Nek391998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID429001Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT2 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1577329Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 4 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID562926Antimicrobial activity against Clostridium difficile CD196 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1301202Antimycobacterial activity against Mycobacterium terrae after 10 days by micro broth dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides.
AID371461Antimicrobial activity against Bacillus subtilis isolate after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID1463961Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 7357/1998 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID563056Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID429002Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT3 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1171223Ratio of MIC for wild-type Escherichia coli to MIC for tolC-deficient Escherichia coli2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID559563Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID542144Antimicrobial activity against Escherichia coli DH10B harboring pBR322 by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID540230Dose normalised AUC in rat after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID563042Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID498872Antimicrobial activity against Acinetobacter baumannii B9 containing carbapenemase blaOXA-23 gene assessed as growth inhibition by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
First isolation of the blaOXA-23 carbapenemase gene from an environmental Acinetobacter baumannii isolate.
AID1224523Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID656230Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID557092Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID562933Upregulation of slpA gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID532986Antibacterial activity against Pseudomonas aeruginosa NCIM 50292010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID391984Inhibition of Escherichia coli DNA gyrase-mediated Escherichia coli pBR322 DNA supercoiling at 1 ug/mL in presence of 0.9 uM histidine6-tagged Enterococcus faecalis qnr protein preincubated before compound administration by agarose gel electrophoresis2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID395774Antibacterial activity against gentamicin-resistant Pseudomonas aeruginosa isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID433401Inhibition of Mycobacterium leprae DNA gyrase subunit A G89C mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID535835Antimicrobial activity against Pseudomonas aeruginosa GP37KT31 harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID279830Half life in BALB/c mouse at 37.5 to 2400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID352097Antimicrobial activity against multidrug-resistant Staphylococcus aureus after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID562937Upregulation of cwp84 gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID68848In vitro minimum inhibitory concentration against Escherichia coli NIHJ JC-21993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID96249In vitro antibacterial activity against Klebsiella pneumoniae 131990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID510159Antimicrobial activity against extended spectrum beta lactamase expressing Proteus mirabilis by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID530376Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB N464S mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1562258Antimycobacterial activity against Mycobacterium smegmatis atR19 assessed as decrease in drug resistance development at 2 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID433578Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A G89A mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID95916Antibacterial activity against Klebsiella pneumoniae MGH-21988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID285685Increase in pvdS gene expression in Pseudomonas aeruginosa PAO1 with rpoN mutation at 8 ug/ml after 3 hrs relative to wild type2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
rpoN gene of Pseudomonas aeruginosa alters its susceptibility to quinolones and carbapenems.
AID540224Clearance in dog after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID562942Upregulation of cwp84 gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1143264Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID560261Antimicrobial activity against Escherichia coli CSH26RifR receiving qnrB19 gene variant carried by IncL/M-like plasmid from Salmonella enterica serovar Typhimurium STYM61/9 by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID1743447Antibacterial activity against Enterobacter cloacae measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID279819Fraction unbound ligand in mouse plasma at 0.01 to 50 mg/litre2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID424863Antimicrobial activity against carbapenem-resistant Pseudomonas aeruginosa clinical isolate assessed as resistant isolates2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Molecular epidemiology and mechanisms of carbapenem resistance in Pseudomonas aeruginosa isolates from Spanish hospitals.
AID209302Compound was tested for inhibition of the gram-negative organism Streptococcus pyogenes C203.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1230246Antibacterial activity against Staphylococcus lugdunensis ATCC 43809 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID395359Antibacterial activity against Staphylococcus aureus ATCC 6538 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID510163Antimicrobial activity against Pseudomonas aeruginosa ATCC 10145 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID540223Volume of distribution at steady state in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID529457Antimicrobial activity against Klebsiella pneumoniae containing PFGE clone B expressing beta-lactamase Oxa-48, TEM-1, CTX-M-15 and Oxa-1 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Spread of OXA-48-positive carbapenem-resistant Klebsiella pneumoniae isolates in Istanbul, Turkey.
AID114659Compound was evaluated for oral efficacy on systemic infections in mice by Escherichia coli KC-141992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1230236Antibacterial activity against Staphylococcus aureus ATCC 9144 oxford after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID562793Antimicrobial activity against Chlamydia trachomatis L2/oflR-rifR2 harboring ampA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID534345Antimicrobial activity against Burkholderia pseudomallei Bp175 harboring mini-Tn7T-P1-bpeR+ after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID28851The compound was evaluated for the solubility in water at 25 degrees Centigrade1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID352817Antimicrobial activity against Staphylococcus albus NCIM 2178 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID560591Antimicrobial activity against Pseudomonas aeruginosa isolate IMCJ799 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID395776Antibacterial activity against Escherichia coli isolate containing extended spectrum beta lactamase after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID659472Effective permeability across porcine polar brain lipid after 4 hrs by PAMPA2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
5-imino-1,2,4-thiadiazoles: first small molecules as substrate competitive inhibitors of glycogen synthase kinase 3.
AID206794Tested for in vitro for antibacterial activity against 16 clinical isolated of methicillin-resistant Staphylococcus aureus1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID293591Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID405119Antimicrobial activity against Escherichia coli TOP10 harbouring pS2 plasmid expressing quinolone resistant QnrS2 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID200345Minimum inhibitory concentration required in vitro against Salmonella1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID279823Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 142007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID559368Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID540222Clearance in rat after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID562786Antimicrobial activity against Chlamydia trachomatis L2/oflR-rifR1 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1230235Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID534342Antimicrobial activity against Burkholderia pseudomallei Bp58 harboring deleted bpeR::FRT gene after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID164268Evaluated for minimum inhibitory concentration against gram-negative bacteria Pseudomonas rettgeri H17711990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID352090Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID96229Compound was tested for inhibition of the gram-negative organism Klebsiella pneumoniae MGH-21986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID530398Antimicrobial activity against Neisseria gonorrhoeae harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID110152Percentage of mice with convulsion (400 mg/kg fenbufen)1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID687498Volume of distribution in rat2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID208735Minimum bactericidal concentration required in vitro against Streptococcus D1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID562929Antimicrobial activity against Clostridium difficile CD196 M1 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1743469Inhibition of DNA gyrase in Mycobacterium smegmatis assessed as elongation of bacterial cells at 2 ug/ml measured after 6 hrs by DAPI/FM 4-64 staining based confocal fluorescence microscopic analysis2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1331873Antibacterial activity against Acinetobacter baumannii ATCC 196062017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID1435654Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1274478Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID198018Activity against Staphylococcus epidermidis (IAM 1296)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID635079Permeability of the compound after 2.5 hrs by PAMPA-BBB assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Neuroprotective efficacy of quinazoline type phosphodiesterase 7 inhibitors in cellular cultures and experimental stroke model.
AID532983Antibacterial activity against Escherichia coli W31102010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID562934Upregulation of slpA gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID207384Inhibition of growth of Staphylococcus aureus (resistant)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID205389Compound was tested for antibacterial activity against gram negative Serratia marcescens No.16-21998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID694227Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID530371Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A, I85V, F96W and P101M mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID563036Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID64884Tested in vitro for antibacterial activity against Escherichia coli (KC-14)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID164701Compound was tested for antibacterial activity against gram negative Pseudomonas aeruginosa K-131998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID385168Antimicrobial activity against Staphylococcus aureus by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID1485936Effective permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Synthesis and pharmacological evaluation of novel chromone derivatives as balanced multifunctional agents against Alzheimer's disease.
AID279837Reduction of Mycobacterium tuberculosis H37Rv in orally dosed BALB/c mouse lung2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID385164Antimicrobial activity against Candida albicans by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID1743460Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ala-90-Val/gyrB Glu-540-Val mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID563038Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID581499Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying mutation2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1230245Antibacterial activity against Staphylococcus intermedius N987 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1435652Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID425073Antimicrobial activity against Escherichia coli DH10B expressing pCR2.1 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID1113450Antibacterial activity against Klebsiella pneumoniae assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID1693561Effective permeability of compound in PBS/EtOH buffer (7:3) at 25 ug/ml incubated for 18 hrs by PAMPA-BBB assay2021Bioorganic & medicinal chemistry, 01-15, Volume: 30Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.
AID1143270Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis 12119 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID687495AUC (0 to infinity) in rat at 10 mg/kg, iv2012Bioorganic & medicinal chemistry, Oct-15, Volume: 20, Issue:20
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties.
AID1703921Permeability of the compound by PAMPA-BBB assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID1437020Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID1230217Antibacterial activity against Enterococcus faecalis N491 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID95735Compound was tested for antibacterial activity against gram negative Klebsiella oxytoca GN 106501998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID510164Antimicrobial activity against extended spectrum beta lactamase expressing Escherichia coli by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1230229Antibacterial activity against Enterococcus hirae CIP 5855 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID563058Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559371Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID205806Compound was tested for its minimal inhibitory constant against Gram-positive microorganism Staphylococcus aureus FDA 209P JC-1 (Sa(F))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID574806Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 horboring rpoB S531L/G566R/I569L, katG S315T/R463L, gyrA A90V/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID143107Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium tuberculosis ATCC 27294 by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID532984Antibacterial activity against Escherichia coli MG1655 in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID530370Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A and I85V mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID395366Antibacterial activity against Micrococcus luteus La 2971 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID131701Effective dose against Staphylococcus aureus smith strain in mouse1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID1577339Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1623078Effective permeability of the compound at 100 ug/ml after 10 hrs by BBB-PAMPA method2019European journal of medicinal chemistry, Feb-01, Volume: 163Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.
AID1653557Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.375 ug/ml in presence of 0.0125 ug/ml KRM-1648 measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID352853Antimicrobial activity against Trichoderma viride NCIM 1195 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID1230228Antibacterial activity against Enterococcus gallinarum N492 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID762020Antibacterial activity against Bacillus cereus 8035 measured every 24 hrs for 5 days by conventional dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Antimicrobial activity of imidazo[1,5-a]quinoxaline derivatives with pyridinium moiety.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID540232Dose normalised AUC in monkey after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID1171218Antibacterial activity against MeXABCDXY-deficient Pseudomonas aeruginosa2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID762019Antibacterial activity against Escherichia coli F-50 measured every 24 hrs for 5 days by conventional dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Antimicrobial activity of imidazo[1,5-a]quinoxaline derivatives with pyridinium moiety.
AID1143267Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis 912253 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1230250Antibacterial activity against Streptococcus agalactiae CIP 103227 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID562935Upregulation of slpA gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID510158Antimicrobial activity against Acinetobacter baumannii RSKK 02026 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID469403Permeability across PAMPA membrane 2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
AID520869Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU33 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID532040Antimicrobial activity against azide-resistant Escherichia coli DH5alpha by Etest2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
AID205881In vitro minimum inhibitory concentration against Staphylococcus epidermidis IAM 12961993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID352809Antimicrobial activity against Vibrio fischeri NCIM 2154 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID1143265Antimycobacterial activity against Mycobacterium tuberculosis D-211 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID563049Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID395718Antibacterial activity against Escherichia coli DH10B containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID163961In vitro antibacterial activity against Pseudomonas aeruginosa E-21992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID563217Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1412148Antibacterial activity against methicillin-resistant Staphylococcus aureus 15 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID143859Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium avium complex (MAC) ATCC 49601 by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID1171224Ratio of MIC for wild-type Pseudomonas aeruginosa to MIC for MeXABCDXY-deficient Pseudomonas aeruginosa2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Trends and exceptions of physical properties on antibacterial activity for Gram-positive and Gram-negative pathogens.
AID542143Antimicrobial activity against Escherichia coli DH10B by broth microdilution assay2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
qnrD, a novel gene conferring transferable quinolone resistance in Salmonella enterica serovar Kentucky and Bovismorbificans strains of human origin.
AID1335286Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 100 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID581511Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrB A90V and T539P mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID562243Antimycobacterial activity against Mycobacterium smegmatis grown in Luria-Bertani broth medium assessed as growth inhibition in mid-logarithmic phase by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID572512Antimicrobial activity against Salmonella enterica serovar Montevideo isolate s2317 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID210196Compound was tested for inhibition of the gram-negative organism Streptococcus pneumoniae SV-11986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID395781Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID581493Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrA D94A mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID96264In vitro antibacterial activity against clinical isolates of Klebsiella pneumoniae-4 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID406847Antibacterial activity against Enterobacter cloacae S1 isolate expressing quinolone resistance determinant QnrB4 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID396100Antibacterial activity against Pseudomonas aeruginosa K1536 overexpressing mexCD by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID523001Cytotoxicity against human 5637 cells assessed as mild induction of cell death by trypan blue exclusion assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID1230249Antibacterial activity against Staphylococcus sciuri N993 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID68201In vitro antibacterial activity against clinical isolates of Enterobacter cloacae 041 (gram negative) by agar dilution assay.1987Journal of medicinal chemistry, Mar, Volume: 30, Issue:3
Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids.
AID70575Compound was tested for its minimal inhibitory constant against Gram-negative microorganism Escherichia coli KC-14 (Ec(K))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID1593375Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis KZN494 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID559580Antimicrobial activity against Chlamydia trachomatis infected in Vero cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID557098Binding affinity to human serum albumin assessed as fraction of binding sites occupied by compound at 18 to 36 ug/ml by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID1126743Antibacterial activity against 0.5 ug/ml Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID386887Antimicrobial activity against Candida albicans ATCC 2091 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID563052Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID574810Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 horboring rpoB D516V, katG S315T/R463L, gyrA D94G/S95T/R128S/Y129C, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1593373Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in drug-susceptible Mycobacterium tuberculosis V4207 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID71981Inhibition of [3H]muscimol binding to GABA A receptor with compound alone at 10 e-4 M1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID352813Antimicrobial activity against Corynebacterium rubrum NCIM 2252 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID429035Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT144 harboring DNA gyrase A D87G mutation assessed as decrease in viable count at 4 times MIC after 4 hrs by time-kill analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID51918Mammalian cell cytotoxicity test in chinese hamster V79 cells (clonogenic cytotoxicity)1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID530386Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA S69V, A71G, E72D, T73V, M74I, N76K, A83S, S84A, I85V, F96W and P101M mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID572510Antimicrobial activity against Salmonella enterica serovar Braenderup isolate s2906 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID133810Compound was evaluated for protective dose against the Escherichia coli vogel lethal infection following peroral administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1055943Antibacterial activity against Enterococcus faecalis ATCC 29212 after 16 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID70576Compound was tested for its minimal inhibitory constant against Gram-negative microorganism Escherichia coli NIHJ JC-2 (Ec(N))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID1301201Antimycobacterial activity against Mycobacterium avium after 10 days by micro broth dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides.
AID562824Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID498780Antimicrobial activity against strong ciprofloxacin-resistant Streptococcus pyogenes by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID530380Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559550Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID559554Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1230208Antibacterial activity against Bacillus cereus N349 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID563059Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1347981Permeability of the compound at pH 7.4 at 25 ug/ml after 18 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID144567Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium smegmatis ATCC 19420 by 90%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID206034Tested in vitro against Staphylococcus epidermidis IAM12896 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID572514Antimicrobial activity against Salmonella enterica serovar Corvallis isolate s2064 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1230218Antibacterial activity against Enterococcus faecalis N518 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1890598Antibacterial activity against Streptococcus pneumoniae assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID203277Antimicrobial activity against the Staphylococcus aureus ATCC 6538 P by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID560601Antimicrobial activity against multidrug resistant Pseudomonas aeruginosa by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID144019Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium fortuitum (clinical isolate) by 90%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID385165Antimicrobial activity against Pseudomonas aeruginosa by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID581507Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrB D500N mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID324749Antibacterial activity in Mycobacterium leprae infected mouse foot-pad model assessed as parasite killing at 150 mg/kg/day after 9 months2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID563222Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1866897Permeability for across blood brain barrier by PAMPA2022European journal of medicinal chemistry, Apr-15, Volume: 234Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors.
AID1331874Antibacterial activity against Enterobacter cloacae ATCC 130472017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID1360039Antimicrobial activity against Pseudomonas aeruginosa after 18 to 20 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID563500Antimicrobial activity against Serratia marcescens ATCC 13880 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID563033Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID405114Antimicrobial activity against Vibrio splendidus 12B01 expressing plasmid-mediated QnrS-like quinolone resistance determinants2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID279840Ratio of fraction Cmax in Mycobacterium tuberculosis infected BALB/c mouse to MIC in Mycobacterium tuberculosis infected BALB/c mouse model at 225 to 115000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID574807Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 horboring rpoB S531L/Q510P, katG S315T/R463L, gyrA D94N/S95T, rrs G1484T by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID429011Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT49 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID763993Antibacterial activity against Shigella flexneri ATCC 15391 after 24 hrs by two-fold serial dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.
AID530396Antimicrobial activity against Klebsiella oxytoca harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID563221Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563035Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID209126Antibacterial activity against Streptococcus pyogenes C2031988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID1502709Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID295103Antibacterial activity against Klebsiella pneumoniae UC57 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID530622Ratio of CC25 for Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S mutant to CC25 for Escherichia coli DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1672292Antifungal activity against Candida albicans assessed as fungal growth inhibition after 24 hrs by CLSI protocol based broth microdilution assay
AID287376Antibacterial activity against Proteus vulgaris after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID352829Antimicrobial activity against Aspergillus flavus NCIM 902 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID428988Antimicrobial activity against Salmonella enterica Serovar Typhi isolate ipt 2 harboring DNA gyrase A D87G mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID205663Compound was tested for in vitro antibacterial activity (minimum inhibition concentration) against gram-positive Sa (F) Staphylococcus aureus FDA 209P JC-11994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID208910Antimicrobial activity against the streptococcus bovis A 5169 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID429025Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG176 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID429021Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG17 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1173783Inhibition of purified Mycobacterium smegmatis GyrB at 50 to 100 uM after 100 mins by ATPase assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID563211Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene assessed as microbial susceptibility and deletion of codons 678 and 679 in gyrB mutant gene assessed as microbial susceptibility by agar proportion m2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1413530Toxicity in Staphylococcus aureus after 18 to 24 hrs by two-fold serial dilution method2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis, and biological evaluation of
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID396098Antibacterial activity against Staphylococcus aureus K2361 overexpressing norA by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID295850Antimicrobial activity against Proteus vulgaris A161 by disk diffusion method at 10 ug/disc2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
AID68183Evaluated for minimum inhibitory concentration against gram-negative bacteria Enterobacter cloacae HA 26461990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID395358Antibacterial activity against Escherichia coli ATCC 11230 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID433583Selectivity index, ratio of CC25 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to CC25 for Mycobacterium leprae wild type DNA gyrase A2B2 by DNA cleavage assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID510171Antimicrobial activity against cephalosporin-resistant Enterococcus faecalis by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID428999Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT145 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID680399TP_TRANSPORTER: inhibition of TEA uptake (TEA: 60 uM, OFLX: 1000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, May, Volume: 289, Issue:2
Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations.
AID559559Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1331870Antibacterial activity against Listeria monocytogenes ATCC 191152017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID151194Activity against Pseudomonas cepacia (IID-1341)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID560593Antimicrobial activity against rifampin-resistant Pseudomonas aeruginosa ATCC 27853 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID563025Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1412152Antibacterial activity against Pseudomonas aeruginosa isolate 1 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID563007Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1753998Permeability of the compound in PBS/EtOH buffer (7:3) incubated for 16 hrs by UV plate reader based PAMPA-BBB assay2021European journal of medicinal chemistry, Jul-05, Volume: 219Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
AID1177574Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by microdilution method2014Journal of natural products, Aug-22, Volume: 77, Issue:8
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
AID133815Compound was evaluated for protective dose against the Streptococcus aureus UC-76 lethal infection following sc administration in mouse1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1230211Antibacterial activity against Enterococcus avium CIP 104053 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID197875Minimum inhibition concentration against Staphylococcus aureus FDA209P strain1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID530418Antimicrobial activity against Klebsiella oxytoca harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1295093Toxicity in healthy mouse administered as single peroral dose measured after 14 days2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
A convenient and efficient approach to polyfluorosalicylic acids and their tuberculostatic activity.
AID1326673Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID540228Clearance in human after iv administration2006Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 34, Issue:7
Extrapolation of preclinical pharmacokinetics and molecular feature analysis of "discovery-like" molecules to predict human pharmacokinetics.
AID78695Gyrase inhibitory activity against Escherichia coli1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID396102Antibacterial activity against Pseudomonas aeruginosa PAO1 by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID429018Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG8 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID530345Antimicrobial activity against Escherichia coli BicA expressing blaTEM-1, blaCTX-M-15 and qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID529669Antimicrobial activity against Escherichia coli R4525 expressing gyrA S83L and D87Y and parC S80I and E84G mutant gene by CLSI method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
ISEcp1-mediated transposition of qnrB-like gene in Escherichia coli.
AID530389Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA A83S mutant/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID520868Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU28 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID1296386Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 1 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID530399Antimicrobial activity against Helicobacter pylori 1 harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID279842Toxicity in Mycobacterium tuberculosis infected BALB/c mouse model at 225 to 115000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID352849Antimicrobial activity against Lipomyces lipofer NCIM 3252 at 5 ug/disk after 72 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID530401Antimicrobial activity against Ehrlichia chaffeensis harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1113449Antibacterial activity against Bacillus subtilis assessed as growth inhibition at 50 ug/ml by cup-plate method (Rvb = 8 to 10 mm)2013Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 22, Issue:4
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-
AID78709Inhibition of DNA gyrase of Escherichia coli H560 cells1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID165048In vitro antibacterial activity against Pseudomonas aeruginosa IFO 34451990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID352093Antimicrobial activity against Pseudomonas aeruginosa ATCC 25853 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID563028Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1230237Antibacterial activity against Staphylococcus aureus CIP 483 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1161578Permeability of the compound by PAMPA-BBB assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties.
AID1163978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID534340Antimicrobial activity against Burkholderia pseudomallei Bp50 harboring deleted (amrRAB-oprA)::FRT gene after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
The BpeAB-OprB efflux pump of Burkholderia pseudomallei 1026b does not play a role in quorum sensing, virulence factor production, or extrusion of aminoglycosides but is a broad-spectrum drug efflux system.
AID316444Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID563223Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563037Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID69952Antimicrobial activity against the Escherichia coli JUHL by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID386886Antibacterial activity against sEscherichia coli ATCC 25922 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID563047Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID535843Antimicrobial activity against Pseudomonas aeruginosa PAO1 IPM46 harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID581492Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrA A90V mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID428996Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT118 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1319976Permeability of the compound at 25 ug/ml at 7.4 pH after 18 hrs by PAMPA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis and biological evaluation of N-cyanoalkyl-, N-aminoalkyl-, and N-guanidinoalkyl-substituted 4-aminoquinoline derivatives as potent, selective, brain permeable antitrypanosomal agents.
AID1230242Antibacterial activity against Staphylococcus aureus CRBIP 2121 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID143121Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium tuberculosis ATCC 27294 by 90%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID1557297Half life in human at 0.4 g, po bid2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1636268Permeability of the compound at pH 7.4 after 18 hrs by PAMPA-BBB assay2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Design, synthesis and biological evaluation of N-methyl-N-[(1,2,3-triazol-4-yl)alkyl]propargylamines as novel monoamine oxidase B inhibitors.
AID563226Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID64253Activity against Escherichia coli (KC-14)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID428992Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 50 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1309356Antimycobacterial activity against rifampin and isoniazid resistant-Mycobacterium tuberculosis Beijing harboring Ser 531 to Leu 315 and Ser to Thr in rpoB and katG genes mutation after 24 hrs by microbroth dilution method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.
AID447082Antibacterial activity against Klebsiella pneumoniae UC57 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID1173449Effective permeability of the compound by PAMPA assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
AID395097Antitrypanosomal activity against wild type Trypanosoma brucei brucei s427 after 48 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
Targeted delivery of compounds to Trypanosoma brucei using the melamine motif.
AID30399Compound was tested for antibacterial activity against gram negative Acinetobacter calcoaceticus No.41998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID510166Antimicrobial activity against Escherichia coli ATCC 35218 by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID1230206Antibacterial activity against Bacillus cereus N190 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID574811Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis H37Rv by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID197994Activity against Staphylococcus aureus (FDA207PJC-1)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID287378Antibacterial activity against Listeria monocytogenes after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID1274480Antibacterial activity against Proteus vulgaris ATCC 8427 after 24 hrs by two-fold serial dilution method2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and biological evaluation of novel phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents.
AID322317Antibacterial activity against CTX-M group 9 enzyme producing Escherichia coli isolates assessed as percent resistant isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID563220Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID531335Antibacterial activity against Pseudomonas aeruginosa TNP030 selected after 1.0 ug/ml of azithromycin by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID530397Antimicrobial activity against Methylovorus sp. harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID467863Antibacterial activity against Micrococcus luteus ATCC 9341 after 18 hrs2009Journal of natural products, Dec, Volume: 72, Issue:12
Structurally diverse limonoids from the fruits of Swietenia mahagoni.
AID405116Antimicrobial activity against Escherichia coli TOP10 harbouring pVS1 expressing quinolone resistant Vibrio splendidus 12B01 QnrVS1 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID1435651Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID295118Antibacterial activity against Listeria monocytogenes ATCC 15313 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID122925Compound was tested for its minimal inhibitory constant against Gram-positive microorganism Micrococcus luteus ATCC 9341 (MI)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID1143263Antimycobacterial activity against Mycobacterium tuberculosis Beijing (E-47/94) assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID581508Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrB D540D mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1743439Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID206216Compound was tested for its minimal inhibitory constant against Gram-positive microorganism Staphylococcus epidermidis IAM 1296 (Se)1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID391989Antibacterial activity against Lactococcus lactis IL-1419 by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID559562Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP8 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID429031Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate BL 21095 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1463960Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 234/2005 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID279824Cmax in BALB/c mouse at 37.5 to 2400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID1143268Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis 19000 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID656228Antimycobacterial activity against isoniazid-, rifampin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID395779Antibacterial activity against Bacillus subtilis ATCC 6633 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID530395Antimicrobial activity against Pseudomonas aeruginosa harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID30416Antimicrobial activity against the acinetobacter sp. CMX 669 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID371459Antimicrobial activity against Staphylococcus aureus isolate after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID429009Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT47 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1224519Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID581512Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA A90V and D94A mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1378879Effective permeability of the compound at 100 mg/ml after 16 hrs by UV based PAMPA-BBB assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Design, synthesis and biological evaluation of novel coumarin-N-benzyl pyridinium hybrids as multi-target agents for the treatment of Alzheimer's disease.
AID163227Compound was tested for antibacterial activity against gram negative Proteus vulgaris KS-1341998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID70566Compound was tested for in vitro antibacterial activity (minimum inhibition concentration) against gram-negative Ec(N), Escherichia coli NIHJ JC-2.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID1360038Antimicrobial activity against Bacillus cereus after 18 to 20 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID581498Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrB D540D mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID563214Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID206652Compound was tested for the in vitro antibacterial activity (minimum inhibitory concentration) against 90% of clinical isolates of methicillin-resistant Staphylococcus aureus (MIC range)1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID131001Compound was tested for oral efficacy on systemic infections caused by Escherichia coli KC-14 in mice1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterials.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1231419Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as growth inhibition at 5 ug after 24 hrs by disc agar diffusion method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of caracasine acid derivatives.
AID530373Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I and A83S mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID562791Antimicrobial activity against Chlamydia trachomatis F/70/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID1502711Antimycobacterial activity against Mycobacterium avium isolate MAV2 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1201747Permeability of the compound by PAMPA2015European journal of medicinal chemistry, May-05, Volume: 95Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
AID1296384Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 9449/2007 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID386885Antibacterial activity against Staphylococcus aureus ATCC 19433 by cup plate method2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
AID391982Antibacterial activity against Enterococcus faecalis JH2-2 containing ORI23::qnr-cat promoter mutant overexpressing qnr by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1743443Antibacterial activity against Mycobacterium bovis BCG measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1653553Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.75 ug/ml in presence of 0.2 ug/ml rifampin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1152780Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates after 2 to 4 weeks by BACTEC 460 radiometric assay2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1435649Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID385167Antimicrobial activity against Bacillus cereus by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID682301TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, OFLX: 500 uM) in OCTN2-expressing HEK293 cells1999The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance.
AID1230233Antibacterial activity against Listeria monocytogenes N836 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID557095Binding affinity to first site on human serum albumin by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID1743445Antibacterial activity against Acinetobacter baumannii measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID206684Evaluated for minimum inhibitory concentration against gram-negative bacteria Staphylococcus pneumoniae SV-11990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID530416Antimicrobial activity against Haemophilus influenzae harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID562796Antimicrobial activity against Chlamydia trachomatis J/6276/oflR-rifR2 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID530246Antimicrobial activity against surA deficient Escherichia coli K-12 BW-25113 assessed as survival rate at 5 ug/ml after 6 hrs by time kill analysis2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Role of global regulators and nucleotide metabolism in antibiotic tolerance in Escherichia coli.
AID1230222Antibacterial activity against Enterococcus faecium N490 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID562799Antimicrobial activity against Chlamydia muridarum MoPn/tetR1 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID428980Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate A102 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID557097Protein binding in serum2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID1352675Effective permeability at 25 ug/ml after 18 hrs by PAMPA2018European journal of medicinal chemistry, Feb-25, Volume: 146Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID713896Antimycobacterial activity against Mycobacterium tuberculosis isolate CIBIN/UMF 15:192012European journal of medicinal chemistry, Mar, Volume: 49Recent advances in antitubercular natural products.
AID69826Tested in vitro against Escherichia coli NIHJ JC-2 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1349195Antichlamydial activity against Chlamydia trachomatis serovar D 454/Bu infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Natural product inspired library synthesis - Identification of 2,3-diarylbenzofuran and 2,3-dihydrobenzofuran based inhibitors of Chlamydia trachomatis.
AID316446Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis by agar dilution method2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Novel ofloxacin derivatives: synthesis, antimycobacterial and toxicological evaluation.
AID428983Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate CT61 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID713895Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 272942012European journal of medicinal chemistry, Mar, Volume: 49Recent advances in antitubercular natural products.
AID520874Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU90 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID1557296AUC in human at 0.4 g, po bid2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID572518Antimicrobial activity against qnrS-positive Salmonella enterica serovar Typhimurium isolate s2705 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID559372Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1071344Permeability of the compound by BBB-PAMPA2014European journal of medicinal chemistry, Feb-12, Volume: 731,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies.
AID1915642Antimycobacterial activity against Mycobacterium tuberculosis My 331/88 (H37Rv) assessed as reduction in bacterial growth incubated for 14 days by microdilution method2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID1230230Antibacterial activity against Listeria innocua E044 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID530382Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A and I85V mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1577335Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 234/2005 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID143862Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium avium complex (MAC) ATCC 49601 by 90%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID563014Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1230240Antibacterial activity against Staphylococcus aureus CIP 5710 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID1516021Antibacterial activity against Salmonella enterica serovar typhimurium C77-31 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID530400Antimicrobial activity against Helicobacter pylori 2 harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1695810Antibacterial activity against Staphylococcus aureus assessed as inhibition zone at 1 mg/ml measured after overnight incubation by disc diffusion method2019European journal of medicinal chemistry, Apr-15, Volume: 168Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids.
AID68191In vitro antibacterial activity against Enterobacter cloacae 9631990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID498786Antimicrobial activity against strong ciprofloxacin-resistant Streptococcus pyogenes at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID1230239Antibacterial activity against Staphylococcus aureus CIP 53156 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID203317In vitro antibacterial activity against Serratia marcescens IFO 37361992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1193923Cytotoxicity against mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID395773Antibacterial activity against Klebsiella pneumoniae RSHM 574 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID530393Antimicrobial activity against Salmonella enterica Typhimurium harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID429014Antimicrobial activity against Salmonella enterica Serovar Typhi isolate AG3 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1412147Antibacterial activity against Staphylococcus aureus ATCC 6538 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID1230205Antibacterial activity against Bacillus cereus CIP 6624 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID425070Antimicrobial activity against multidrug-resistant Escherichia coli M7943-TC2 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID287372Antibacterial activity against Staphylococcus aureus after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID559551Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP4 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1393806Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition at 6.25 ug/ml by broth dilution assay relative to control2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID1907631Antibacterial activity against Pseudomonas aeruginosa incubated for 18 to 20 hrs by double dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Novel benzothiazole‒urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA.
AID429015Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG5 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID433579Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A A91V mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID78705Inhibition constant against DNA Gyrase isolated from Escherichia coli1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID163785Tested in vitro for antibacterial activity against Pseudomonas aeruginosa (E-2)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID133953In vivo antibacterial activity against Escherichia coli (Vogel) in mice administered perorally1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative.
AID131005Compound was tested for oral efficacy on systemic infections on mice by peroral administration1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID639368Permeability of the compound by PAMPA assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease.
AID1703887Permeability of the compound incubated for 165 mins by PAMPA-BBB assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID143108Minimum inhibitory concentration required in vitro to reduce the number of viable of Mycobacterium tuberculosis clinical isolate 1104 by 50%1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID510162Antimicrobial activity against trimethoprim-sulfamethoxazole and tazobactum-induced Pseudomonas aeruginosa by spectrophotometry2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A study of cytotoxicity of novel chlorokojic acid derivatives with their antimicrobial and antiviral activities.
AID395362Antibacterial activity against Proteus vulgaris ATCC 8427 at 5 ug after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis, Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of mixed aza-oxo-thia macrocyclic compounds.
AID391977Antibacterial activity against Enterococcus faecalis JH2-2 by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1188154Inhibition of Mycobacterium tuberculosis DNA gyrase supercoiling activity using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID530368Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID762021Antibacterial activity against Staphylococcus aureus 209p measured every 24 hrs for 5 days by conventional dilution method2013European journal of medicinal chemistry, Aug, Volume: 66Antimicrobial activity of imidazo[1,5-a]quinoxaline derivatives with pyridinium moiety.
AID530415Antimicrobial activity against Salmonella enterica Typhimurium harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1227981Antimycobacterial activity against GFP expressing Mycobacterium tuberculosis H37Ra assessed as microbial growth inhibition incubated at 37 degC for 7 days by fluorescence based assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Eremophilane Sesquiterpenes and Diphenyl Thioethers from the Soil Fungus Penicillium copticola PSU-RSPG138.
AID352625Antimicrobial activity against Klebsiella aerogenes NCIM 2239 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID1056993Permeability of the compound at 100 mg/mL after 10 hrs by PAMPA2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID442657Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID352633Antimicrobial activity against Escherichia coli NCIM 2065 at 5 ug/disk after 24 hrs by disk diffusion method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Microwave-induced synthesis and anti-microbial activities of 7,10,11,12-tetrahydrobenzo[c]acridin-8(9H)-one derivatives.
AID425071Antimicrobial activity against Escherichia coli J53-AzR in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID287374Antibacterial activity against Bacillus cereus after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID74853Antibacterial activity against five Gram-positive bacteria targeting topoisomerase II (DNA gyrase B GyrB)1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Fluoroquinolones: relationships between structural variations, mammalian cell cytotoxicity, and antimicrobial activity.
AID71793Percentage of GABA-induced chloride currents with 10 e-5 M 4-biphenylacetic acid1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID396096Antibacterial activity against Staphylococcus aureus K1758-A overexpressing mepA by broth microdilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps.
AID429019Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG15 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID69784Antibacterial activity against Escherichia coli (vogel)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1743459Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ser-91-Pro mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID205650Compound was tested for antibacterial activity against gram positive Staphylococcus aureus FDA 209P JC-11998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID581501Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA A90V mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID38471Activity against Bacillus subtilis (ATCC 6633)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID1412151Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 after 24 hrs by microbroth dilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Design, synthesis and antibacterial evaluation of a polycationic calix[4]arene derivative alone and in combination with antibiotics.
AID279827AUC(0-infinity) in BALB/c mouse at 37.5 to 2400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID1230234Antibacterial activity against Listeria monocytogenes N851 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID563210Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID447083Antibacterial activity against Bacillus cereus ATCC 7064 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID1360042Bactericidal activity against Staphylococcus aureus after 24 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID563057Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID162776In vitro minimum inhibitory concentration against Pseudomonas aeruginosa E-21993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID535848Antimicrobial activity against Pseudomonas aeruginosa GP61KT51 harboring oprD,mexAB-oprM gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID562790Antimicrobial activity against Chlamydia trachomatis J/6276/tetR harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1321386Antibacterial activity against Escherichia coli ATCC 25922 by broth microdilution method2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
The Rational Design, Synthesis, and Antimicrobial Properties of Thiophene Derivatives That Inhibit Bacterial Histidine Kinases.
AID279822Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 72007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID1502713Antimycobacterial activity against Mycobacterium avium isolate MAV4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID1437019Antimycobacterial activity against isoniazid/rifampicin/ethambutol-sensitive Mycobacterium tuberculosis H37Rv after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID1672291Antifungal activity against Candida tropicalis assessed as fungal growth inhibition after 24 hrs by CLSI protocol based broth microdilution assay
AID70426Compound was tested for antibacterial activity against gram negative Escherichia coli CSH2/RE451998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID433582Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID523004Antibacterial activity against uropathogenic Escherichia coli UTI89 assessed as degradation of preexisting biofilm after 24 hrs by microscopy2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
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AID498785Antimicrobial activity against mild ciprofloxacin-resistant Streptococcus pyogenes at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID70804Inhibition of growth of Escherichia coli vogel1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID65376Tested in vitro for antibacterial activity agains Enterococcus faecalis (IID 682)1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID1480943Permeability of the compound at pH 7.4 at 5 mg/ml after 18 hrs by PAMPA-BBB assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Enzymatic and solid-phase synthesis of new donepezil-based L- and d-glutamic acid derivatives and their pharmacological evaluation in models related to Alzheimer's disease and cerebral ischemia.
AID322315Antibacterial activity against CTX-M group 1 enzyme producing Escherichia coli isolates assessed as percent nonsusceptible isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Spread of extended-spectrum beta-lactamase CTX-M-producing escherichia coli clinical isolates in community and nosocomial environments in Portugal.
AID581514Antimycobacterial activity against mixture of fluoroquinolone-resistant and sensitive Mycobacterium tuberculosis Beijing genotype isolates carrying heteropeaks upon sequencing at mutation site and harboring gyrA D94G and D94A mutant genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID563020Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID209278Antimicrobial activity against the streptococcus pyogenes 2548 by 2-fold agar dilution method using brain-heart infusion agar.1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
AID96239Evaluated for minimum inhibitory concentration against gram-negative bacteria Klebsiella pneumoniae MGH-21990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID562795Antimicrobial activity against Chlamydia muridarum MoPn/oflR-rifR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1463959Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 9449/2007 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1163981Cytotoxicity against mouse RAW264.7 cells at 100 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID164565Compound was tested for antibacterial activity against gram negative Pseudomonas aeruginosa AK1091998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID1502707Antimycobacterial activity against Mycobacterium avium 104 mc'2 3 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID563213Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1224517Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID1331877Antibacterial activity against Pseudomonas aeruginosa ATCC 278532017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID1368749Antibacterial activity against Bacillus subtilis MTCC 441 at 1 ug/ml under overnight incubation condition by paper disc method2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Synthesis and biological evaluation of 1-amino isochromans from 2-bromoethyl benzaldehyde and amines in acid medium.
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Synthesis and biological activity of some new benzoxazoles.
AID563021Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID295851Antimicrobial activity against Proteus vulgaris KUKEM1329 by disk diffusion method at 10 ug/disc2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
AID1296387Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 4 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID162792Inhibition of growth of Pseudomonas aeruginosa1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID287373Antibacterial activity against Klebsiella pneumoniae after 72 hrs by disk diffusion method2007European journal of medicinal chemistry, Feb, Volume: 42, Issue:2
Synthesis, characterization and antimicrobial activity of Fe(II), Zn(II), Cd(II) and Hg(II) complexes with 2,6-bis(benzimidazol-2-yl) pyridine ligand.
AID1413648Antibacterial activity against methicillin-resistant Staphylococcus aureus JCSC 4788 at sub-MIC re-passaged at 24 hrs intervals for 5 times by micro dilution susceptibility test2018MedChemComm, Oct-01, Volume: 9, Issue:10
Structural optimization and antibacterial evaluation of rhodomyrtosone B analogues against MRSA strains.
AID164245Antibacterial activity against Pseudomonas aeruginosa UI-181988Journal of medicinal chemistry, Mar, Volume: 31, Issue:3
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
AID530350Antimicrobial activity against Escherichia coli TOP10 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID295852Antimicrobial activity against Streptococcus pyogenes ATCC 176 by disk diffusion method at 10 ug/disc2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
AID208893Compound was tested for inhibition of the gram-negative organism Streptococcus aureus H228.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID1331875Antibacterial activity against Escherichia coli MC10612017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.
AID1413531Toxicity in Escherichia coli after 18 to 24 hrs by two-fold serial dilution method2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis, and biological evaluation of
AID203326In vitro antibacterial activity against Serratia marcescens S-91990Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
AID562826Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID428997Antimicrobial activity against Salmonella enterica Serovar Typhi isolate CT142 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID563053Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID1516025Antibacterial activity against Escherichia coli 20411 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID52938Compound was tested for antibacterial activity against gram negative Citrobacter freundii No.71998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID1593374Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis V2475 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID371466Antimicrobial activity against Pseudomonas aeruginosa ATCC 25853 after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID535839Antimicrobial activity against Pseudomonas aeruginosa GP4KT111 harboring oprD,mexAB-oprM gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID563044Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562789Antimicrobial activity against Chlamydia trachomatis L2/tetR13 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID391978Antibacterial activity against Enterococcus faecalis JH2-2-omega-pG1KT mutant with inactivated qnr gene by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID559553Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP5 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID563019Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID197995Activity against Staphylococcus aureus (IID 803)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Synthesis and antibacterial activity of thiazolo-, oxazolo-, and imidazolo[3,2-a][1,8]naphthyridinecarboxylic acids.
AID562946Upregulation of slpA gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID563022Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563335Upregulation of fbp68 gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID572515Antimicrobial activity against Salmonella enterica serovar Stanley isolate s2043 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID532989Antibacterial activity against Klebsiella aerogenes NCIM 2281 in presence of 10 mM N-Acetylcysteine2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
AID563054Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID395716Antibacterial activity against Escherichia coli DH10B by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1360044Antimicrobial activity against methicillin-resistant Staphylococcus aureus after 18 to 20 hrs by micro broth dilution method2018European journal of medicinal chemistry, Jun-25, Volume: 154Free radical rearrangement synthesis and microbiological evaluation of novel 2-sulfoether-4-quinolone scaffolds as potential antibacterial agents.
AID1577337Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 7357/1998 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID562825Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID550049Antibacterial activity against Streptococcus pneumoniae assessed as inhibition of visible growth after 48 hrs by agar dilution method2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Conventional and microwave assisted synthesis of 2-oxo-4-substituted aryl-azetidine derivatives of benzotriazole: a new class of biological compounds.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID530404Antimicrobial activity against Clostridium perfringens harboring DNA gyrase GyrA QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID151535Tested in vitro against Pseudomonas aeruginosa E-2 by agar dilution method1993Journal of medicinal chemistry, Sep-17, Volume: 36, Issue:19
Synthesis of antimicrobial agents. 5. In vivo metabolism of 7-(4-hydroxypiperazin-1-yl)quinolones.
AID1516085Antibacterial activity against ciprofloxacin-resistant Escherichia coli ATCC 25922 incubated for 18 to 24 hrs2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID562936Upregulation of cwp84 gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID563008Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562938Upregulation of cwp84 gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID581496Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrA D94Y mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1326672Growth inhibition of mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID1765292Permeability of compound by PAMPA-BBB assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Design, synthesis and biological evaluation of harmine derivatives as potent GSK-3β/DYRK1A dual inhibitors for the treatment of Alzheimer's disease.
AID425074Antimicrobial activity against Escherichia coli DH10B in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID1309355Antimycobacterial activity against Mycobacterium terrae after 24 hrs by microbroth dilution method2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Synthesis and evaluation of antitubercular activity of fluorinated 5-aryl-4-(hetero)aryl substituted pyrimidines.
AID1557298Protein binding in human at 0.4 g, po bid2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1653554Antimicrobial activity against Mycobacterium leprae assessed as microbial growth at 0.375 ug/ml in presence of 0.025 ug/ml rifabutin measured at 4 weeks (Rvb = 147 +/- 19.1%)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1326670Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID324746Effect on Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as enhancement of supercoiled pBR322 DNA cleavage2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID530374Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA S69V, A71G, E72D, T73V, M74I, N76K, A83S, S84A, I85V, F96W and P101M mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID557090Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 0.1% alpha-1-acid glycoprotein2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID391980Antibacterial activity against Enterococcus faecalis JH2-2 containing ORI23 promoter by broth microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID572509Antimicrobial activity against Salmonella enterica serovar Typhimurium isolate SL1344 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID405477Antibacterial activity against methicillin-resistant Staphylococcus aureus 2884 isolate at 5 ug by disc diffusion method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Identification and phenotypic characterization of a beta-lactam-dependent, methicillin-resistant Staphylococcus aureus strain.
AID530381Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1172969Antibacterial activity against Escherichia coli TG12014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Identification and characterization of an anti-pseudomonal dichlorocarbazol derivative displaying anti-biofilm activity.
AID656229Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID429020Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate AG16 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1230231Antibacterial activity against Listeria monocytogenes CIP 103575 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID562941Effect on fbp69 gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID530375Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID391975Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID559369Antimicrobial activity against compound-susceptible Coxiella burnetii isolate CP2 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID572521Antimicrobial activity against qnrS-positive Salmonella enterica serovar Montevideo isolate s2209 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1516022Antibacterial activity against Escherichia coli UB1005 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID531333Antibacterial activity against Pseudomonas aeruginosa PAO4290 selected after 1.0 ug/ml of azithromycin by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
AID405478Antibacterial activity against methicillin-resistant Staphylococcus aureus 2884 isolate at 30 ug by disc diffusion method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Identification and phenotypic characterization of a beta-lactam-dependent, methicillin-resistant Staphylococcus aureus strain.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID427196Membrane permeability by PAMPA-BBB assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.
AID1890597Antibacterial activity against methicillin resistant Staphylococcus aureus assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1296383Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 234/2005 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID395777Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID208894Compound was tested for inhibition of the gram-negative organism Streptococcus aureus UC-76.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
AID293586Antibacterial activity against Staphylococcus aureus isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID391986Antibacterial activity against Staphylococcus aureus RN4220 by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID563101Upregulation of fbp68 gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID428977Antimicrobial activity against Salmonella enterica Serovar Typhi isolate D43 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID385163Antimicrobial activity against Escherichia coli by broth microdilution method2008Journal of natural products, Apr, Volume: 71, Issue:4
Antimicrobial triterpenoids from Vladimiria muliensis.
AID535832Antimicrobial activity against wild-type Pseudomonas aeruginosa GP61 after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID563227Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1743446Antibacterial activity against Enterobacter aerogenes measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID442659Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID563342Induction of Cwp84 protease expression in Clostridium difficile CD07-259 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID562827Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1231421Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as growth inhibition at 5 ug after 24 hrs by disc agar diffusion method2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and biological evaluation of caracasine acid derivatives.
AID1230232Antibacterial activity against Listeria monocytogenes N783 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID447081Antibacterial activity against Staphylococcus aureus ATCC 6538 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID205653Compound was tested for antibacterial activity against gram positive Staphylococcus aureus smith1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
AID206009Minimum inhibitory concentration required in vitro against Staphylococcus aureus1999Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12
Nitroquinolones with broad-spectrum antimycobacterial activity in vitro.
AID563501Antimicrobial activity against cetylpyridinium chloride-resistant Serratia marcescens 01 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Mutational upregulation of a resistance-nodulation-cell division-type multidrug efflux pump, SdeAB, upon exposure to a biocide, cetylpyridinium chloride, and antibiotic resistance in Serratia marcescens.
AID210022Antibacterial activity against Streptococcus pneumoniae (SV-1)1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay.
AID1502708Antimycobacterial activity against Mycobacterium avium 104 mc'2 4 assessed as reduction in bacterial viability incubated for 3 days by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Natural isoflavone biochanin A as a template for the design of new and potent 3-phenylquinolone efflux inhibitors against Mycobacterium avium.
AID563034Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1301200Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 10 days by micro broth dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis and antimycobacterial activity of N-(2-aminopurin-6-yl) and N-(purin-6-yl) amino acids and dipeptides.
AID530420Antimicrobial activity against Neisseria gonorrhoeae harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID209240Inhibition of growth of Streptococcus faecalis1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
AID559370Antimicrobial activity against compound-resistant Coxiella burnetii isolate CP3 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID1126742Antibacterial activity against 1 ug/ml Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID581495Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis Beijing genotype isolates without carrying multiple mutation and harboring gyrA D94N mutant gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Beijing genotype of Mycobacterium tuberculosis is significantly associated with high-level fluoroquinolone resistance in Vietnam.
AID1230248Antibacterial activity against Staphylococcus saprophyticus E260 after 18 hrs by agar dilution method2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Antibacterial Labdane Diterpenoids from Vitex vestita.
AID429008Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate DT42 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID429029Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate HTD 798 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID405470Antibacterial activity against oxacillin-dependent methicillin-resistant Staphylococcus aureus 2884D isolate at 5 ug by disc diffusion method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Identification and phenotypic characterization of a beta-lactam-dependent, methicillin-resistant Staphylococcus aureus strain.
AID572524Antimicrobial activity against qnrS-positive Salmonella enterica serovar Stanley isolate s2018 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID563011Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
AID1296385Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID428981Antimicrobial activity against Salmonella enterica Serovar Typhi isolate C152 harboring DNA gyrase A S83Y mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID1167605Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
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Antibacterial Labdane Diterpenoids from Vitex vestita.
AID535847Antimicrobial activity against Pseudomonas aeruginosa PAO1 KTL harboring oprD gene after 18 hrs by agar dilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
AID522870Antibacterial activity against uropathogenic Escherichia coli UTI89 infected in human 5637 cells assessed as decrease in intracellular bacterial level at 400 to 700 ug/ml after 12 hrs by serial dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID428989Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate nar 28 harboring DNA gyrase A S83F mutation by disk diffusion method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID96421In vitro minimum inhibitory concentration against Klebsiella pneumoniae B541993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID560260Antimicrobial activity against Salmonella enterica serovar Typhimurium transconjugant p61/9T expressing qnrB19 gene variant carried by IncL/M-like plasmid by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID534419Antibacterial activity against Mycobacterium bovis BCG-Connaught2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID447217Antibacterial activity against Mycobacterium smegmatis CCM 2067 at 5 ug after 24 hrs by agar disk diffusion assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis, Raman, FT-IR, NMR spectroscopic characterization, antimicrobial activity, cytotoxicity and DNA binding of new mixed aza-oxo-thia macrocyclic compounds.
AID67422In vitro minimum inhibitory concentration against E. Faecalis IID6821993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
AID164713Compound was tested for its minimal inhibitory constant against Gram-negative microorganism Pseudomonas aeruginosa IFO 3445 (Pa(I))1994Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17
Synthesis and antibacterial activity of thiazolopyrazine-incorporated tetracyclic quinolone antibacterial agents. 2.
AID563013Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID530425Antimicrobial activity against Clostridium perfringens harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1326671Inhibition of Mycobacterium tuberculosis DNA gyrase subunit A2B2 supercoiling activity using relaxed pBR322 as substrate after 30 mins in presence of ATP by agarose gel electrophoresis2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID733006Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose gel electro2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID1183278Permeability of the compound by PAMPA2014European journal of medicinal chemistry, Sep-12, Volume: 84Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies.
AID110153Percentage of mice with convulsion with compound alone at 400 mg/kg1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Quinolone antimicrobial agents substituted with morpholines at the 7-position. Syntheses and structure-activity relationships.
AID429032Antimicrobial activity against multidrug-resistant Salmonella enterica Serovar Typhi isolate BL 3769 harboring DNA gyrase A S83F mutation by disk diffusion method in presence of plasmid mediated quinolone-resistant gene qnrA and qnrS2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial drug resistance of Salmonella enterica serovar typhi in asia and molecular mechanism of reduced susceptibility to the fluoroquinolones.
AID70721Evaluated for minimum concentration needed to produce linear DNA at an intensity relative to oxolinic acid at 10 mg/mL. by gyrase mediated cleavage of DNA in Escherichia coli 560.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
AID559560Antimicrobial activity against compound-intermediate susceptible Coxiella burnetii isolate CP7 obtained from patient with acute Q fever infected in african green monkey Vero cells after 24 hrs by shell vial assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
AID371465Antimicrobial activity against Klebsiella pneumoniae after 24 hrs by disk diffusion method2008European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
Synthesis and biological activity of some new benzoxazoles.
AID530621Antimicrobial activity against Bacillus subtilis harboring DNA gyrase GyrB QRDR2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1177576Antibacterial activity against Micrococcus luteus ATCC 9341 after 18 hrs by microdilution method2014Journal of natural products, Aug-22, Volume: 77, Issue:8
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
AID559582Antimicrobial activity against Chlamydophila psittaci infected in Vero cells2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
AID391976Antibacterial activity against Escherichia coli ATCC 25922 by broth dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1900247Permeability of the compound at pH 7.4 PBS/EtOH buffer (70:30) by PAMPA-BBB assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy.
AID295106Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 at 5 ug after 24 hrs by disk diffusion method2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Raman, FT-IR, NMR spectroscopic data and antimicrobial activity of bis[micro2-(benzimidazol-2-yl)-2-ethanethiolato-N,S,S-chloro-palladium(II)] dimer, [(micro2-CH2CH2NHNCC6H4)PdCl]2.C2H5OH complex.
AID1152778Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis harboring DNA gyraseA G88N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1177577Antibacterial activity against Bacillus subtilis ATCC 6633 after 18 hrs by microdilution method2014Journal of natural products, Aug-22, Volume: 77, Issue:8
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,062)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990679 (11.20)18.7374
1990's1543 (25.45)18.2507
2000's2270 (37.45)29.6817
2010's1307 (21.56)24.3611
2020's263 (4.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 126.13

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index126.13 (24.57)
Research Supply Index8.92 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index239.98 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (126.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials976 (15.05%)5.53%
Reviews333 (5.14%)6.00%
Case Studies782 (12.06%)4.05%
Observational6 (0.09%)0.25%
Other4,387 (67.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (86)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Oral Antibiotic Prophylaxis of Early Infection in Multiple Myeloma [NCT00002850]Phase 3212 participants (Actual)Interventional1997-03-31Completed
Quinolone Prophylaxis for the Prevention of BK Virus Infection in Kidney Transplantation: A Pilot Study [NCT01353339]Phase 4154 participants (Actual)Interventional2011-11-30Completed
A Randomized, Controlled, Open Label Study of the Safety and Efficacy of a Topical Gentamicin Collagen Sponge Combined With An Antibiotic Compared to Antibiotic Therapy Alone in Diabetic Patients With Moderately Infected Foot Ulcers [NCT00659646]Phase 256 participants (Actual)Interventional2008-04-30Completed
Evaluation of Two Strategies of Antibiotic Treatment With Levofloxacin in Acute Exacerbation of Chronic Obstructive Pulmonary Disease: Short Treatment-versus Standard Treatment [NCT03698682]Phase 2310 participants (Actual)Interventional2018-01-01Completed
Efficacies of Antimicrobial Susceptibility-Guided Versus Empirical Therapy for Rescue Treatment of Helicobacter Pylori Infection-A Randomized Clinical Trial [NCT03658746]Phase 4420 participants (Actual)Interventional2019-01-01Completed
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
An International, Multicenter, Randomized, Blinded-assessor, Parallel-group Clinical Study Comparing Eye Drops of Combined LEvofloxAcin + DExamethasone foR 7 Days Followed by Dexamethasone Alone for an Additional 7 Days vs. Tobramycin + Dexamethasone for [NCT03739528]Phase 3808 participants (Actual)Interventional2018-09-03Completed
A Multi-center, Randomized, Double-blind, Double-dummy Clinical Study to Evaluate the Safety and Efficacy of Prulifloxacin Film-coated Tablet for the Treatment of Acute Uncomplicated Lower Urinary Tract Infection With Levofloxacin Hydrochloride Tablet as [NCT02439632]Phase 3216 participants (Anticipated)Interventional2014-02-28Completed
Conventional Antibiotic Prophylaxis Versus Add-On 5 Days Levofloxacin Before Percutaneous Nephrolithotomy (PCNL) [NCT03178292]300 participants (Anticipated)Interventional2017-06-15Not yet recruiting
Study of Nitazoxanide (NTZ) Based New Therapeutic Regimens for Helicobacter Pylori [NCT02422706]Phase 3120 participants (Anticipated)Interventional2015-01-31Recruiting
Sanjin Tablets for the Treatment of Acute Simple Lower Urinary Tract Infection and Its Influence on Recurrence Rate: a Randomized, Double Blind, Parallel Control of Positive Drugs, Multi-center Clinical Study [NCT03658291]Phase 4252 participants (Anticipated)Interventional2019-01-01Not yet recruiting
Efficacies of Tetracycline-levofloxacin Quadruple Therapy, Standard Bismuth Quadruple Therapy and Amoxicillin-levofloxacin Quadruple Therapy in the Second-line Treatment of H Pylori Infection [NCT05850117]240 participants (Anticipated)Interventional2020-02-10Recruiting
Evaluation of Two Strategies of Antibiotic Treatment With Levofloxacin in Acute Exacerbation of Chronic Obstructive Pulmonary Disease: Short Treatment-versus Treatment Guided by Markers of Inflammation [NCT02067780]Phase 3310 participants (Actual)Interventional2017-05-01Completed
Safety and Efficacy of a Topical Otic Formulation in the Treatment of Acute Otitis Media With Otorrhea Through Tympanostomy Tubes (AOMT) [NCT00578474]Phase 3911 participants (Actual)Interventional2005-12-31Completed
A Open-label, Single Sequence Clinical Trial to Investigate the Pharmacokinetic Characteristics of Second-Line Anti-Tuberculosis Agents After Multiple Oral/Intramuscular Administration in Healthy Male Volunteers [NCT02128308]Phase 116 participants (Actual)Interventional2013-11-30Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Asymptomatic Bacteriuria & Risk of Urinary Tract Infection in Renal Transplants [NCT01349738]200 participants (Anticipated)Observational2011-05-31Enrolling by invitation
Determination of a Trough Serum Concentration of Ofloxacin Associated to Increase in Side Effects Frequency in Elderly Treated for Bone and Joint Infection [NCT04496024]110 participants (Anticipated)Interventional2020-06-02Recruiting
Gel-Sinuplasty for Chronic Rhinosinusitis With and Without Nasal Polyposis [NCT03472144]Phase 360 participants (Anticipated)Interventional2017-07-07Recruiting
VisuMax Femtosecond Laser Small Incision Lenticule Extraction for the Correction of High Myopia [NCT02528123]187 participants (Anticipated)Interventional2016-04-30Active, not recruiting
High Eradication Rate of Helicobacter Pylori Infection With Moxifloxacin-Based Triple Therapy in Comparison With Levofloxacin-Based Sequential Therapy: Randomized Controlled Trials [NCT05863858]Phase 3162 participants (Actual)Interventional2020-06-01Completed
Double-Blind, Placebo-Controlled Study of Three-Month Treatment With the Combination of Ofloxacin and Roxithromycin in Recent-Onset Reactive Arthritis [NCT00621387]56 participants (Actual)Interventional1993-11-30Completed
Comparison of the Effectiveness of Preurodynamic Single Dose of Levofloxacin With Posturodynamic Levofloxacin for Three Days on the Incidence of Urinary Tract Infections [NCT05219877]Phase 1/Phase 2134 participants (Actual)Interventional2022-02-04Completed
[NCT02157571]Phase 3360 participants (Anticipated)Interventional2013-06-30Recruiting
Evaluation of Lactated Ringers for Protection From Cisplatin Ototoxicity. [NCT00584155]Phase 10 participants (Actual)Interventional2006-07-31Withdrawn(stopped due to PI left the university.)
A Phase II, Multi-Center, Randomized, Parallel Controlled Study to Evaluate the Clinical Efficacy and Safety of IVIEW 1201 Compared to Ofloxacin Eye Drops in the Treatment of Acute Bacterial Conjunctivitis [NCT05816070]Phase 2129 participants (Actual)Interventional2023-01-05Completed
Evaluation of the Congruity of Methods Used in the Diagnostics of Chronic Endometritis in the Course of Infertility and the Effectiveness of Antibiotic Therapy in the Context of Remission of Symptoms and Obstetric Results [NCT05946655]100 participants (Actual)Interventional2021-04-01Completed
A Multicenter, Double-Blind, Phase 3B Study to Compare the Safety and Clinical Efficacy of Levofloxacin in 750mg for 2 Weeks and Levofloxacin 750mg for 3 Weeks to That of Levofloxacin 500mg for 4 Weeks in the Treatment of Chronic Prostatitis [NCT00402688]Phase 3242 participants (Actual)Interventional2006-11-30Completed
Comparison of Early Changes in Ocular Surface and Inflammatory Mediators Between Lenticule Extraction and Small-Incision Lenticule Extraction [NCT02540785]41 participants (Actual)Interventional2014-04-30Completed
Prospective, Randomized, Double-blind, Multicenter, Multinational Study Comparing Efficacy and Safety of Moxifloxacin 400 mg po od for 14 Days With Ofloxacin 400 mg po Bid Plus Metronidazole 500 mg po Bid for 14 Days in Patients With Uncomplicated Pelvic [NCT00683865]Phase 3749 participants (Actual)Interventional2003-04-30Completed
Efficacy of Tympanostomy Tubes for Children With Recurrent Acute Otitis Media [NCT02567825]250 participants (Actual)Interventional2015-11-30Completed
Does the Use of Topical Otic Drops at the Time of Tympanostomy Tube Placement Improve Outcomes When no Middle Ear Effusion is Present at the Time of Surgery [NCT03655665]Phase 4125 participants (Anticipated)Interventional2019-05-16Recruiting
A Pilot, Multicenter, Open Label, Non Comparative Study of the Safety and Efficacy of Floxin Otic Solution in the Treatment of Acute Otitis Media Twice Daily for Seven Days in Children With Tympanostomy Tubes [NCT00781521]Phase 396 participants (Actual)Interventional2002-11-30Completed
A Randomized, Double-masked, Parallel Group Study of DE-108 Ophthalmic Solution in Patients Who Are Scheduled for Cataract Surgery (Levofloxacin 0.5% Ophthalmic Solution as a Comparator) - Phase III, Confirmatory Study of Perioperative Bacteria Eradicatio [NCT02573610]Phase 3576 participants (Actual)Interventional2015-09-21Completed
MSI-78 Topical Cream vs. Oral Ofloxacin in the Treatment of Infected Diabetic Ulcers [NCT00563394]Phase 3584 participants (Actual)Interventional1994-08-31Completed
Randomized Controled Multicentric Trial, of Non Inferiority, Comparing Two Durations of Antibiotherapy (5 Days Versus 10 Days) in COMMUNAUTARY Acute Uncomplicated Pyelonephritis. [NCT00873626]Phase 4310 participants (Actual)Interventional2009-06-30Completed
Phase 4 Study of Azitromicin in the Treatment of PID [NCT01241110]Phase 4100 participants (Actual)Interventional2010-01-31Completed
Safety and Efficacy Study of Levofloxacin Combined With Endovascular Thrombectomy for Acute Ischemic Stroke Due to Large Vessel Occlusion of Anterior Circulation [NCT05743101]80 participants (Anticipated)Interventional2023-02-13Not yet recruiting
Penetrance of Third Generation Fluoroquinolones in Eyes With Functioning Filtering Blebs [NCT00392275]Phase 448 participants Interventional2002-11-30Completed
An Open Label, Three Arm, Pilot Study of the Safety and Clinical Efficacy of Topical Dermacyn™ Wound Care vs. Oral Levofloxacin vs. Combined Therapy for Mild Diabetic Foot Infections [NCT00516958]Phase 265 participants (Anticipated)Interventional2007-05-31Completed
Comparison of Early Changes in Ocular Surface and Inflammatory Mediators Among Lenticule Extraction, Laser in Situ Keratomileusis and Femtosecond Laser-assisted Laser in Situ Keratomileusis [NCT02551796]75 participants (Actual)Interventional2015-09-30Completed
Phase II Study: Treatment of Relapsed Lymphoid Malignancies With an Anti-angiogenic Approach [NCT00250718]Phase 217 participants (Actual)Interventional2004-10-31Terminated(stopped due to Low rate of accrual)
Efficacy and Safety of 14-day Concomitant Therapy for Difficult-to-Treat Helicobacter Pylori: A Pilot Study [NCT05126121]60 participants (Anticipated)Interventional2021-11-20Not yet recruiting
Safety and Efficacy of Levofloxacin Combined With Intravenous Thrombolysis for Acute Ischemic Stroke [NCT05741905]100 participants (Anticipated)Interventional2023-06-01Recruiting
Does Prophylactic Antibiotic Decrease the Rate of Urinary Tract Infection After Robot Assisted Radical Cystectomy [NCT04502095]Phase 4100 participants (Anticipated)Interventional2020-09-02Recruiting
Helicobacter Pylori Eradication in Mexico With a Levofloxacin-containing Scheme Versus Clarithromycin-based Triple Therapy: a Randomized, Open-label, Non-inferiority, Phase 3b Trial. [NCT02726269]Phase 3230 participants (Actual)Interventional2012-06-30Completed
An Open-label, Randomized, 3-way Crossover Study to Evaluate the Bioequivalence of an Oral Suspension Formulation, an Oral Solution Formulation, and the Marketed Tablet Formulation of Levofloxacin in Healthy Subjects [NCT00602589]Phase 172 participants (Actual)Interventional2002-10-31Completed
MSI-78 Topical Cream vs. Oral Ofloxacin in the Treatment of Infected Diabetic Ulcers [NCT00563433]Phase 3342 participants (Actual)Interventional1994-08-31Completed
Susceptibility-Guided Sequential Therapy Versus Empirical Therapy for Helicobacter Pylori Infection: a Randomised Controlled Trial [NCT05549115]500 participants (Anticipated)Interventional2022-09-20Recruiting
Swiss PACK-CXL (Photoactivated Chromophore for Infectious Keratitis Cross-linking) Multicenter Trial for the Treatment of Infectious Keratitis [NCT02717871]Phase 335 participants (Actual)Interventional2016-03-31Completed
Efficacy of Two Antimicrobial Susceptibility Testing Guided Antibiotic Selection Strategies in Salvage Helicobacter Pylori Treatment [NCT02988089]Phase 4480 participants (Anticipated)Interventional2017-04-20Recruiting
Ofloxacin vs. Gentamicin as Prophylaxis Prior Transrectal Biopsy of Prostate [NCT00480376]Phase 4160 participants (Anticipated)Interventional2007-06-30Not yet recruiting
A Single- Centre, Randomised Study Of The Clinical And Microbiological Efficacy Of Decreasing The Dosage Of Levofloxacin 0,5% Eye Drops As Compared To Standard Eye Drop Dosage In Patients With Bacterial Conjunctivitis [NCT00565123]Phase 2/Phase 3119 participants (Actual)Interventional2004-09-30Completed
Effect of Nasal Ointment on Epistaxis of Nasotracheal Intubation in Children: A Randomized Controlled Trial [NCT04426409]108 participants (Actual)Interventional2020-07-08Completed
Comparison of the Efficacy of Levofloxacin-based Sequential Therapy and Triple Therapy as Second Line Therapy for Refractory Helicobacter Pylori Infection- A Multi-center Randomized Trial [NCT01537055]Phase 4600 participants (Anticipated)Interventional2012-02-29Recruiting
A Multi-center, Randomized, Double-blind, Double-dummy Parallel-controlled Phase II Clinical Study to Assess the Efficacy and Safety of Nemonoxacin Malate in Treating Adult Patients With Community-acquired Pneumonia (CAP) [NCT01537250]Phase 2192 participants (Actual)Interventional2009-08-31Completed
A Randomized, Multicenter, Open Label Trial Comparing Intravenous Zithromax® (Azithromycin) Plus Intravenous Rocephin® (Ceftriaxone) Followed By Oral Zithromax® (Azithromycin) With Intravenous Levaquin® (Levofloxacin) Followed By Oral Levaquin® (Levofloxa [NCT00035347]Phase 4219 participants (Actual)Interventional2001-01-31Completed
Comparison of Two Rescue Therapies for Helicobacter Pylori Infection - A Multicenter Randomized Controlled Trial [NCT02547012]51 participants (Actual)Interventional2013-11-30Completed
An Evaluation of the Safety and Efficacy of Moxifloxacin Ophthalmic Solution 0.5% Versus Ofloxacin Ophthalmic Solution 0.3% in the Treatment of Bacterial Conjunctivitis in Chinese Patients [NCT01573910]Phase 3985 participants (Actual)Interventional2012-05-31Completed
Treatment of Methicillin-sensitive Staphylococcus Aureus Orthopaedic Infections With Clindamycin in Combination With Rifampin or Levofloxacin: a Randomized Pharmacological and Clinical Study (the CLINDOS Trial) [NCT01500837]23 participants (Actual)Interventional2010-10-31Completed
The Study on the Selection of Time for Retreatment of Helicobacter Pylori After Eradication Failure [NCT04810793]820 participants (Actual)Observational [Patient Registry]2020-07-01Completed
A Prospective Randomized Control Trial of Pilocarpine Use After Combined Cataract/Kahook Dual Blade Surgery [NCT03933631]Phase 3142 participants (Anticipated)Interventional2019-05-01Recruiting
"A Prospective, Randomized, Comparative Clinical Trial of the Efficacy and Safety of Levofloxacin Versus Isoniazid in the Treatment of Latent Tuberculosis Infection in Liver Transplant Patients." [NCT01761201]Phase 368 participants (Actual)Interventional2012-01-31Terminated(stopped due to Recruitment rythm not sufficent to reach the simple size needed.)
An Open Label, Randomized Controlled Trial to Establish the Efficacy and Safety of a Study Strategy Consisting of 6 Months of Bedaquiline (BDQ), Delamanid (DLM), and Linezolid (LNZ), With Levofloxacin (LVX) and Clofazimine (CFZ) Compared to the Current So [NCT04062201]Phase 3402 participants (Actual)Interventional2019-08-22Active, not recruiting
A Prospective Randomized Trial of Levofloxacin-amoxicillin Triple Therapy vs. Levofloxacin-tetracycline Quadruple Therapy in Second-line Helicobacter Pylori Treatment [NCT02978157]102 participants (Actual)Interventional2015-02-28Completed
Descemet Endothelial Thickness Comparison Trial [NCT02373137]Phase 438 participants (Actual)Interventional2015-01-22Active, not recruiting
Safety and Efficacy of Levofloxacin for Acute Ischemic Stroke: A Randomized Controlled Clinical Trial [NCT05799326]100 participants (Anticipated)Interventional2023-06-30Recruiting
An International, Multicenter, Randomized, Double-blind, Double-dummy, Two-way, Parallel Group, Controlled Study to Compare the Efficacy and Safety of Intravenous and Oral Nemonoxacin Versus Tavanic® in Adult Patients With Community-acquired Pneumonia [NCT03551210]Phase 3342 participants (Actual)Interventional2016-05-04Completed
Efficacies of Two Bismuth Quadruple Therapies in the Second-line Treatment of H Pylori Infection - a Multi-center Randomized Controlled Trial [NCT03779087]112 participants (Actual)Interventional2018-07-11Completed
Visiting Staff, Division of Gastroenterology and Department of Internal Medicine, Mackay Memorial Hospital, Taipei, Taiwan [NCT03832465]Phase 420 participants (Actual)Interventional2019-06-14Completed
[NCT01799356]Phase 41,303 participants (Actual)Interventional2010-06-30Completed
The Usefulness of Melatonin Supplementation in Postmenopausal Women With Helicobacter Pylori-associated Dyspepsia [NCT04352062]152 participants (Actual)Interventional2011-01-09Completed
A Prospective Randomized Control Trial of Pilocarpine Use After Combined Cataract/Trabectome Surgery [NCT04005079]Phase 30 participants (Actual)Interventional2019-06-05Withdrawn(stopped due to not performing Trabectomes)
Personalized Treatment for Refractory H Pylori Infection [NCT02547025]126 participants (Actual)Interventional2012-08-01Completed
Antibiotic Treatment for 7 Days Versus 14 Days in Patients With Acute Male Urinary Tract Infection Due to Fluoroquinolones Susceptible Bacteria: a Multicentre, Non-inferiority, Double Blind, Randomized Placebo-controlled Trial [NCT02424461]Phase 3400 participants (Anticipated)Interventional2015-02-28Recruiting
Aqueous Humour Concentrations After Topical apPlication of combinEd Levofloxacin-dexamethasone Eye dRops and of Its Single Components: a randoMized, assEssor-blinded, Parallel-group Study in Patients Undergoing Cataract Surgery - iPERME [NCT03740659]Phase 2125 participants (Actual)Interventional2018-09-04Completed
An Open Label Non Placebo Study to Evaluate Efficacy and Safety of Levofloxacin as an Empirical Therapy in Patients With Complicated Urinary Tract Infections [NCT03160807]Phase 4214 participants (Anticipated)Interventional2017-04-15Recruiting
Development of an Adjustment Assistance Tool Dosage of Fluoroquinolones in a Population Pharmacokinetic Model [NCT02357407]Phase 431 participants (Actual)Interventional2015-06-30Completed
Efficacy of Seven-day Combined Rabeprazole Plus Levofloxacin Plus Augmentin for Eradication of Helicobacter Pylori. [NCT01575899]Phase 4208 participants (Actual)Interventional2007-12-31Terminated(stopped due to Early termination due to efficacy)
Comparison of Ofloxacin and Metronidazole/Amoxicillin on the Treatment of Periodontitis. [NCT04353362]Phase 474 participants (Actual)Interventional2017-04-01Completed
Bioequivalence Study of Levomerc (Levofloxacin) 500 mg Tablet With Tavanic (Levofloxacin) 500 mg Tablets [NCT05339295]Phase 124 participants (Actual)Interventional2012-07-11Completed
Prospective Cohort Study on Patients With Tedizolid Prolonged Therapy for Orthopedic Device Infections [NCT03378427]35 participants (Actual)Interventional2018-08-28Completed
Phase 3, Open-label, Randomized Trial to Evaluate the Safety and Efficacy of MP-376 Inhalation Solution (Aeroquin) vs. Tobramycin Inhalation Solution (TIS) in Stable CF Patients [NCT01270347]Phase 3267 participants (Actual)Interventional2011-01-31Completed
Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis [NCT05398679]Phase 4360 participants (Anticipated)Interventional2022-06-01Not yet recruiting
Oral Versus Topical Antibiotic Therapy for Treatment of Chronic Rhinosinusitis Exacerbations [NCT01988779]Phase 333 participants (Actual)Interventional2013-10-31Completed
Absorption of Antibiotics With High Oral Bioavailability in Short-bowel Syndrome : a Monocentric Pilot Study [NCT05302531]Phase 110 participants (Anticipated)Interventional2022-12-09Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00002850 (1) [back to overview]Proportion of Patients Experiencing a Serious Bacterial Infection
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00402688 (6) [back to overview]Total NIH-CPSI Score
NCT00402688 (6) [back to overview]Clinical Success
NCT00402688 (6) [back to overview]Clinical Success (Non-Relapse) or Failure (Relapse)
NCT00402688 (6) [back to overview]Clinical Success (Non-Relapse) or Failure (Relapse)
NCT00402688 (6) [back to overview]Clinical Success (Non-Relapse) or Failure (Relapse)
NCT00402688 (6) [back to overview]Symptom Relief (Resolved)
NCT00659646 (8) [back to overview]Number of Participants With a Clinical Cure at Visit 3 (Day 7)
NCT00659646 (8) [back to overview]Time to Clinical Cure
NCT00659646 (8) [back to overview]Change From Baseline in Total Wound Surface Area Measured in cm^2
NCT00659646 (8) [back to overview]Lipsky Wound Score
NCT00659646 (8) [back to overview]Number of Participants With a Clinical Cure at Each Visit Except Visit 3 (Day 7)
NCT00659646 (8) [back to overview]Number of Participants With a Positive Clinical Response at Each Time Point
NCT00659646 (8) [back to overview]Number of Participants With Pathogen Eradication by Visit
NCT00659646 (8) [back to overview]Visual Analog Scale (VAS) for Pain Assessment
NCT01573910 (2) [back to overview]Microbiological Success Rate
NCT01573910 (2) [back to overview]Clinical Cure Rate
NCT01575899 (3) [back to overview]Eradication Rate (Participants Naive to Anti-H. Pylori Treatment)
NCT01575899 (3) [back to overview]Eradication Rate of Participants Living in Rural Area.
NCT01575899 (3) [back to overview]Re-eradication Rate
NCT01988779 (5) [back to overview]Mean Change in the Total Bacterial Community
NCT01988779 (5) [back to overview]Number of Participants With Post-treatment Culture Negativity
NCT01988779 (5) [back to overview]Change in Bilateral Endoscopy Findings Using POSE Score
NCT01988779 (5) [back to overview]Change in Rhinosinusitis Disability Index (RSDI) Score
NCT01988779 (5) [back to overview]Change in Sino-nasal Outcome Test (SNOT-22) Score
NCT02373137 (13) [back to overview]Graft Failure/Graft Rejection
NCT02373137 (13) [back to overview]Corneal Higher-Order Aberrations
NCT02373137 (13) [back to overview]Corneal Higher-Order Aberrations
NCT02373137 (13) [back to overview]Best Spectacle-Corrected Visual Acuity
NCT02373137 (13) [back to overview]Adverse Events/Complication Rates
NCT02373137 (13) [back to overview]Endothelial Cell Count
NCT02373137 (13) [back to overview]Endothelial Cell Count
NCT02373137 (13) [back to overview]Interface Haze
NCT02373137 (13) [back to overview]National Eye Institute - Visual Functioning Questionnaire (NEI-VFQ)
NCT02373137 (13) [back to overview]Graft Thickness
NCT02373137 (13) [back to overview]Best Spectacle-Corrected Visual Acuity
NCT02373137 (13) [back to overview]Best Spectacle-Corrected Visual Acuity
NCT02373137 (13) [back to overview]Interface Haze
NCT02547012 (1) [back to overview]Number of Participants in Which H. Pylori Was Eradicated
NCT02567825 (12) [back to overview]The Mean Scores on the 6 Item Caregiver Impact Questionnaire (CIQ)
NCT02567825 (12) [back to overview]The Mean Scores on the 6 Item Quality of Life Survey Questionnaire (OM-6)
NCT02567825 (12) [back to overview]The Rate of Occurrence of Acute Otitis Media (AOM) Episodes Per Child-Year According to the Estimated Risk of Acute Otitis Media (AOM) Recurrences at Enrollment
NCT02567825 (12) [back to overview]The Total Cost of Management of Recurrent Acute Otitis Media Per Quality Adjusted Life Days (QALDs) as a Measure of Cost-Effectiveness According to the Estimated Risk of Acute Otitis Media Recurrences at Enrollment
NCT02567825 (12) [back to overview]The Distribution of Children With a Penicillin-Nonsusceptible Nasopharyngeal or Throat Isolate At Any Follow-up Visit According to the Colonization Status at Enrollment
NCT02567825 (12) [back to overview]The Mean Days Per Year Children Receive Systemic Antimicrobials for AOM
NCT02567825 (12) [back to overview]The Mean Days Per Year Children Experience Tube Otorrhea
NCT02567825 (12) [back to overview]The Mean Days Per Year Children Experience AOM Symptoms With an Intact Tympanic Membrane (TM)
NCT02567825 (12) [back to overview]The Mean Score Representing Parental Satisfaction With Clinical Management
NCT02567825 (12) [back to overview]The Rate of Occurrence of Acute Otitis Media (AOM) Episodes Per Child-Year
NCT02567825 (12) [back to overview]The Time to the First Episode of AOM
NCT02567825 (12) [back to overview]The Total Cost of Management of Recurrent Acute Otitis Media Per Quality Adjusted Life Days (QALDs) as a Measure of Cost-Effectiveness
NCT02978157 (1) [back to overview]Number of Participants in Which H. Pylori Was Eradicated
NCT03551210 (10) [back to overview]Nemnoxacin Concentration Changes
NCT03551210 (10) [back to overview]Number of Patients With Microbiological Success
NCT03551210 (10) [back to overview]Number of Patients With Clinical Success as Judged by the Investigator
NCT03551210 (10) [back to overview]Number of Patients Required for Other Antibiotic Treatment
NCT03551210 (10) [back to overview]Number of Patients With Infection Relapse
NCT03551210 (10) [back to overview]Terminal Elimination Half-life (T1/2) of Nemonoxacin
NCT03551210 (10) [back to overview]Time to Switch Therapy From Intravenous to Oral Therapy
NCT03551210 (10) [back to overview]Volume of Distribution at Steady State (Vss) of Nemonoxacin
NCT03551210 (10) [back to overview]Сlearance (CL) of Nemonoxacin
NCT03551210 (10) [back to overview]Area Under the Concentration-time Curve (AUC) of Nemonoxacin
NCT03739528 (10) [back to overview]Intraocular Pressure (IOP)
NCT03739528 (10) [back to overview]Ocular Pain/Discomfort: 4-point Scale
NCT03739528 (10) [back to overview]Adverse Events
NCT03739528 (10) [back to overview]Number of Participants Without Signs of Anterior Ocular Chamber Inflammation
NCT03739528 (10) [back to overview]Conjunctival Hyperemia
NCT03739528 (10) [back to overview]Visual Acuity
NCT03739528 (10) [back to overview]Total Ocular Symptoms Score (TOSS)
NCT03739528 (10) [back to overview]Number of Participants With Endophthalmitis
NCT03739528 (10) [back to overview]Global Evaluation of Local Tolerability
NCT03739528 (10) [back to overview]Burning, Stinging, Blurred Vision
NCT03740659 (3) [back to overview]Aqueous Humour Concentration of Dexamethasone
NCT03740659 (3) [back to overview]Aqueous Humour Concentration of Dexamethasone 21-phosphate
NCT03740659 (3) [back to overview]Aqueous Humour Concentration of Levofloxacin
NCT05219877 (1) [back to overview]Number of Participant With Urinary Tract Infection

Proportion of Patients Experiencing a Serious Bacterial Infection

This study evaluated the impact of prophylactic antibiotics on the incidence of serious bacterial infections (SBIs) during the first 2 months of treatment in patients with newly diagnosed multiple myeloma. Patients with multiple myeloma receiving initial chemotherapy were randomized on a 1:1:1 basis to daily ciprofloxacin, trimethoprim-sulfamethoxazole, or observation and evaluated for SBI for the first 2 months of treatment. (NCT00002850)
Timeframe: First three months of chemotherapy

Interventionpercentage of participants (Number)
Ciprofloxacin or Ofloxacin12.5
TMP-SMX6.8
No Prophylaxis15.9

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (Median)
DTG 50mg q.d.32.8
EVG/COBI 150/150mg q.d.7.6
DRV/COBI 800/150 mg q.d.NA
EFV 600 mg q.d. (Outside THA)65.6

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.0.15
DTG 50mg q.d.1.25
EVG/COBI 150/150mg q.d.0.91
DRV/COBI 800/150 mg q.d.0.07
ATV/COBI 300/150 mg q.d.0.07
TFV 300mg q.d.0.88

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
EFV 600 mg q.d. (Outside THA)0.67
EFV 600mg q.d.0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.0.2
RAL 400mg b.i.d.1.5
ETR 200mg b.i.d.0.52
MVC 150 or 300mg b.i.d.0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.12
RPV 25mg q.d.0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.0.18

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Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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Total NIH-CPSI Score

National Institute of Health-Chronic Prostatitis Symptom Index numerically rates a total score (0-43) where 0 indicates no symptoms across any of the domains (pain or discomfort, urination, quality of life). (NCT00402688)
Timeframe: Screening/Admission, On-Therapy, Week 3, Week 4, Posttherapy (Study Day 33-36)

,,
InterventionScore on a scale (Mean)
Screening/Admission (n=73, 74, 75)On-Therapy (n=70, 70, 73)Week 3 (Visit 2) (n=62, 65, 68)Week 4 (Visit 3) (n=53, 57, 61)Posttherapy (Visit 4) (n=70, 71, 71)
Levofloxacin 500mg for 4 Weeks12.96.95.64.54.6
Levofloxacin 750mg for 2 Weeks11.87.26.55.15.4
Levofloxacin 750mg for 3 Weeks12.06.66.54.95.0

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Clinical Success

Defined as cured or improved. Response is based on the resolution of signs and symptoms at post-therapy. (NCT00402688)
Timeframe: Posttherapy Visit (Study Day 33-36)

InterventionParticipants (Number)
Levofloxacin 750mg for 2 Weeks46
Levofloxacin 750mg for 3 Weeks48
Levofloxacin 500mg for 4 Weeks52

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Clinical Success (Non-Relapse) or Failure (Relapse)

Number of Clinical Successes or Failures at 3 Month Poststudy Telephone Contact for Participants Cured/Improved at the Posttherapy Visit (NCT00402688)
Timeframe: Poststudy Telephone contact at 3 Months

,,
InterventionParticipants (Number)
Clinical SuccessFailureUnable to EvaluateMissing
Levofloxacin 500mg for 4 Weeks38419
Levofloxacin 750mg for 2 Weeks30808
Levofloxacin 750mg for 3 Weeks246117

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Clinical Success (Non-Relapse) or Failure (Relapse)

Number of Clinical Successes or Failures at the 6-month Poststudy Telephone Contact For Participants Cured/Improved at the Posttherapy Visit (NCT00402688)
Timeframe: Poststudy Telephone Contact at 6 Months

,,
InterventionParticipants (Number)
Clinical SuccessFailureUnable to EvaluateMissing
Levofloxacin 500mg for 4 Weeks316114
Levofloxacin 750mg for 2 Weeks1910116
Levofloxacin 750mg for 3 Weeks194124

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Clinical Success (Non-Relapse) or Failure (Relapse)

Number of Clinical Successes or Failures at the 6-Week Poststudy Telephone Contact for Participants Cured/Improved at the Posttherapy Visit (NCT00402688)
Timeframe: Poststudy Telephone contact at 6 weeks

,,
Interventionparticipants (Number)
Clinical SuccessFailureUnable to EvaluateMissing
Levofloxacin 500mg for 4 Weeks44512
Levofloxacin 750mg for 2 Weeks38305
Levofloxacin 750mg for 3 Weeks321213

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Symptom Relief (Resolved)

Participants With Resolution of Prostatitis Signs and Symptoms; Resolution is defined as symptoms present (mild, moderate or severe) at Screening/Admission and absent (none) at the Posttherapy evaluation. (NCT00402688)
Timeframe: Posttherapy Visit (Study Day 33-36)

,,
InterventionParticipants (Number)
Dysuria (n=35, 43, 42)Suprapubic discomfort (n=41, 36, 45)Painful ejaculation (n=32, 39, 34)Low back pain (n=43, 44, 44)Perineal discomfort (n=40, 42, 50)Frequency (n=58, 63, 62)Urgency (n=48, 52, 58)Hesitancy (n=37, 39, 54)Decreased urinary stream (n=50, 47, 52)Urinary retention (n=24, 26, 27)Pain on digital rectal examination (n=60, 59, 61)Perineal tenderness or pain (n=44, 38, 43)Chills (n=4, 5, 7)Other (n=5, 8, 8)Fever (n=3, 2, 1)
Levofloxacin 500mg for 4 Weeks273020262930353830174228751
Levofloxacin 750mg for 2 Weeks232417202029201924133028312
Levofloxacin 750mg for 3 Weeks291923221924281621133024352

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Number of Participants With a Clinical Cure at Visit 3 (Day 7)

Number of participants with a clinical cure in each treatment group at Visit 3 (Day 7). Clinical Cure is defined as positive clinical response and with pathogen eradication. (NCT00659646)
Timeframe: Day 7 of treatment

InterventionParticipants (Count of Participants)
Gentamicin Sponge0
Levofloxacin3

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Time to Clinical Cure

clinical cure is defined as having a positive clinical response and with pathogen eradication (NCT00659646)
Timeframe: Days 1 through 49

InterventionDays (Mean)
Gentamicin Sponge21
No Sponge14

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Change From Baseline in Total Wound Surface Area Measured in cm^2

Wound Surface Area was measured in cm² Actual Values Total wound surface area was compared across treatments using 2-sample t-tests. Wound tracings were obtained at study visits by trained study personnel who were blinded to the patient data and regimen. A centralized imaging facility provided both wound perimeter and area measurements. (NCT00659646)
Timeframe: Day 3, 7, 10, 14, 21, 28 & 42

,
Interventioncm^2 (Mean)
Visit 1 Day 1Visit 2 Day 3Visit 3 Day 7Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28Final Study Visit Day 42
Gentamicin Sponge5.114.504.474.314.142.932.673.73
No Sponge1.24.92.761.140.951.93.64

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Lipsky Wound Score

"The Lipsky wound scoring scale consists of scoring categories for purulent drainage, non-purulent drainage, erythema, induration, tenderness, pain, local warmth and wound measurements. This wound scoring system allows us to take the size and depth of the wound into consideration as well as all signs and symptoms of inflammation and infection. A quantitative score that assess wounds both at baseline and during therapy to compare wound scores over time. The higher the score the worse the inflammation and/or infection is. The Lowest score possible is 3 and the highest score possible is 64." (NCT00659646)
Timeframe: Days 3, 7, 10, 14, 21, 28, 42

,
Interventionscore on a scale (Mean)
Visit 1 Day 1Visit 2 Day 3Visit 3 Day 7Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28Final Study Visit Day 42
Gentamicin Sponge17.6713.5810.799.178.367.295.106.18
No Sponge13.10117.608.295.334.333.674.80

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Number of Participants With a Clinical Cure at Each Visit Except Visit 3 (Day 7)

clinical cure is defined as having a positive clinical response and with pathogen eradication (NCT00659646)
Timeframe: Day 3, 10, 14, 21, 28 & 42

,
InterventionParticipants (Count of Participants)
Visit 2 Day 3Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28Final Visit Day 42
Gentamicin Sponge01104922
No Sponge003017

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Number of Participants With a Positive Clinical Response at Each Time Point

"Number of patients with positive clinical response, defined as those with a clinical outcome of clinical cure or clinical improvement in each treatment group at/by each time point" (NCT00659646)
Timeframe: Day 3, 7, 10,14, 21, 28 and 42

,
InterventionParticipants (Count of Participants)
Visit 2 Day 3Visit 3 Day 7Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28Final Study Visit Day 42
Gentamicin Sponge24262524141022
Levofloxacin910763310

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Number of Participants With Pathogen Eradication by Visit

(NCT00659646)
Timeframe: Day 3, 7, 10, 14, 21 & 28

,
InterventionParticipants (Count of Participants)
Visit 2 Day 3Visit 3 Day 7Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28
Gentamicin Sponge20242318125
No Sponge122200

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Visual Analog Scale (VAS) for Pain Assessment

"Measured on a Visual Analog Pain Scale (VAS) with the lowest possible value of 0 and highest 100 (0 - 100) at each time point. A lower score is better which means the patient experience lower pain. The score is calculated using the number of hours * the VAS score. This represents the AUC (Area Under the Curve) of the pain intensities when calculated with the trapezoidal rule. For each measure outcome - the minimum score is 0 and the maximum score is 100* the number of hours in that period." (NCT00659646)
Timeframe: Day 3, 7, 10, 14, 21, 28 & 42

,
Interventionscore on a scale*days (Mean)
Visit 1 Day 1Visit 2 Day 3Visit 3 Day 7Visit 4 Day 10Visit 5 Day 14Visit 6 Day 21Visit 7 Day 28Final Study Visit Day42
Gentamicin Sponge39.227.617.517.213.322.914.317.3
No Sponge26.318.712.613.613.214.39.32.3

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Microbiological Success Rate

Microbiological specimen(s) from the affected eye(s) were collected according to a protocol-defined process. Microbiological success rate is presented as the percentage of participants for which the pre-therapy pathogens at Visit 1 (Day 1) were eradicated at Day 9 TOC/Exit Visit. (NCT01573910)
Timeframe: Day 9

Interventionpercentage of participants (Number)
Moxifloxacin95.3
Ofloxacin94.8

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Clinical Cure Rate

Ocular signs of bacterial conjunctivitis (bulbar conjunctival injection and conjunctival discharge/exudates) were rated by the investigator on a 4-point scale, with 0=normal/absent; 1=mild; 2=moderate, and 3=severe. Clinical cure rate is presented as the percentage of participants for which the sum of the numerical scores for the 2 cardinal ocular signs of bacterial conjunctivitis was 0 at Day 9 TOC/Exit Visit. (NCT01573910)
Timeframe: Day 9

Interventionpercentage of participants (Number)
Moxifloxacin85.4
Ofloxacin81.4

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Eradication Rate (Participants Naive to Anti-H. Pylori Treatment)

A negative post-treatment 13C-urea breath test or CLO test result at more than 4 weeks after complete use of drug for treatment. (NCT01575899)
Timeframe: 4 weeks after complete use of drug for treatment

Interventionpercentage of eradicated participants (Number)
Levofloxacin-Amox/Clav.78.1
Clarithromycin-Amoxicillin57.5

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Eradication Rate of Participants Living in Rural Area.

Subgroup analysis on eradication rate (percentage of participants with a negative result of C13 or CLO test at least four weeks after treatment) according to resident area of participants, especially who are living in rural area. (NCT01575899)
Timeframe: 4 weeks after complete use of drug for treatment

Interventionpercentage of eradicated participants (Number)
Levofloxacin-Amox/Clav.81.4
Clarithromycin-Amoxicillin51.3

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Re-eradication Rate

Re-eradication successful rate (percentage of participants with a negative result of C13 or CLO test at least four weeks after the 2nd treatment) with 7-day levofloxacin, amoxicillin/clavulanate and rabeprazole for patients still with Hp infection previously treated with regimen without levofloxacin and Augmentin. (NCT01575899)
Timeframe: 4 weeks after complete use of drug for treatment

Interventionpercentage of successful re-eradication (Number)
Levofloxacin-Amox/Clav. (Re-eradication)72.6

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Mean Change in the Total Bacterial Community

The bacterial community was determined using a 16S rRNA quantitative PCR processed using Quantitative Insights into Microbial Ecology (QIIME) software, version 1.8 to yield the number of operational taxonomic units in each subject sample. The count has a minimum of zero with an increasing score indicating a larger number of distinct bacterial species. (NCT01988779)
Timeframe: Baseline and 14 days after treatment

Interventionoperational taxonomic units (Mean)
Oral Placebo With Nebulized Intranasal Levofloxacin17.40
Oral Antibiotics With Nebulized Intranasal Placebo6.700

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Number of Participants With Post-treatment Culture Negativity

Post-treatment culture negativity, defined as less than 1+ growth of organisms. A subject is counted '1' if both nares are free of bacterial growth, and '0' if growth is 1+ of more (NCT01988779)
Timeframe: 14 days after treatment

InterventionParticipants (Count of Participants)
Oral Placebo With Nebulized Intranasal Levofloxacin5
Oral Antibiotics With Nebulized Intranasal Placebo2

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Change in Bilateral Endoscopy Findings Using POSE Score

"The Perioperative Sinus Endoscopy (POSE) instrument is a specific tool to endoscopically assess the sinus cavities of patients who have undergone endoscopic sinus surgery.~Each POSE score has a minimum of 0 and a maximum of 16, with a higher score indicating a worse outcome.~Here, the Left and Right POSE scores are summed and the difference between baseline and the 14 day after treatment is reported.~The change in bilateral POSE score can in principle be -32 to +32, with increased scores indicating worse outcome and negative scores indicating improvement over the treatment period." (NCT01988779)
Timeframe: Baseline and 14 days after treatment

Interventionunits on a scale (Mean)
Oral Placebo With Nebulized Intranasal Levofloxacin-2.889
Oral Antibiotics With Nebulized Intranasal Placebo-4.545

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Change in Rhinosinusitis Disability Index (RSDI) Score

"The Rhinosinusitis Disability Index is a 30-item questionnaire completed by the patient or subject. Each item has a value of zero to four, a higher score indicates a self-perception of worse symptoms. The minimum score is zero and the maximum score is 120.~The difference score here is the post-treatment score minus the pre-treatment score, with lower meaning more improvement" (NCT01988779)
Timeframe: Baseline and 14 days after treatment

Interventionunits on a scale (Mean)
Oral Placebo With Nebulized Intranasal Levofloxacin-8.000
Oral Antibiotics With Nebulized Intranasal Placebo-14.82

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Change in Sino-nasal Outcome Test (SNOT-22) Score

"The Sino-nasal outcome test is a 22-item questionnaire completed by the patient or subject. Each item has a value of zero to five, a higher score indicates a self-perception of worse symptoms. The minimum score is zero and the maximum score is 110.~The difference score here is the post-treatment score minus the pre-treatment score, with lower meaning more improvement" (NCT01988779)
Timeframe: Baseline and 14 days after treatment

Interventionunits on a scale (Mean)
Oral Placebo With Nebulized Intranasal Levofloxacin-2.333
Oral Antibiotics With Nebulized Intranasal Placebo-18.73

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Graft Failure/Graft Rejection

(NCT02373137)
Timeframe: Baseline 12 months

,
Interventioneyes (Count of Units)
Graft RejectionGraft Failure
DMEK01
UT-DSAEK01

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Corneal Higher-Order Aberrations

Corneal anterior and posterior surface higher-order aberrations (HOA) were measured with Scheimpflug imaging (Pentacam) before surgery and at 3, 6, and 12 months post-operatively. Zernike orders 3-8 were calculated at 4.0- and 6.0-mm-diameter optical zones. The results reported here represent total HOA (Sum of Zernike orders 3-8). Note a single observation was not available for one eye in the DMEK group at 6 months, this was analyzed with last observation carried forward. (NCT02373137)
Timeframe: 3, 6, 12 months

,
Interventionroot mean square in micrometers (Mean)
3 Months Anterior Cornea 4.0-mm3 Months Posterior Cornea 4.0-mm3 Months Anterior Cornea 6.0-mm3 Months Posterior Cornea 6.0-mm6 Months Anterior Cornea 4.0-mm6 Months Posterior Cornea 4.0-mm6 Months Anterior Cornea 6.0-mm6 Months Posterior Cornea 6.0-mm12 Months Anterior Cornea 4.0-mm12 Months Posterior Cornea 4.0-mm12 Months Anterior Cornea 6.0-mm12 Months Posterior Cornea 6.0-mm
DMEK0.2880.1160.8290.3460.2430.0950.7240.2880.2410.0980.7230.284
UT-DSAEK0.2740.2170.8970.6210.2300.1790.7390.5050.2280.1590.7250.459

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Corneal Higher-Order Aberrations

As measured by Pentacam (NCT02373137)
Timeframe: 24 months

,
Interventionroot mean square in micrometers (Mean)
24 Months Anterior Cornea 4.0-mm24 Months Posterior Cornea 4.0-mm24 Months Anterior Cornea 6.0-mm24 Months Posterior Cornea 6.0-mm
DMEK0.2110.0860.6790.260
DSAEK0.2150.1550.7070.450

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Best Spectacle-Corrected Visual Acuity

The BSCVA was recorded at 4 meters by a masked refractionist certified for the study using a protocol adapted from the Age-Related Eye Disease Study using Early Treatment Diabetic Retinopathy Study charts: chart R(2110), chart 1(2111), and chart 2(2112) (Precision Vision, Woodstock, IL). (NCT02373137)
Timeframe: 3 and 12 months

,
InterventionlogMAR (Mean)
3 Months12 Months
DMEK0.110.04
UT-DSAEK0.240.16

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Adverse Events/Complication Rates

composite measure (NCT02373137)
Timeframe: 3, 6, 12, 24 months

,
Interventionnew adverse events reported (Number)
Adverse Events at 3 monthsAdverse Events at 6 monthsAdverse Events at 12 monthsAdverse Events at 24 months
DMEK6540
UT-DSAEK4410

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Endothelial Cell Count

(NCT02373137)
Timeframe: 24 months

Interventioncells/mm^2 (Mean)
UT-DSAEK1626
DMEK1400

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Endothelial Cell Count

(NCT02373137)
Timeframe: 3, 6, 12 months

,
Interventioncells/mm^2 (Mean)
3 Months6 Months12 Months
DMEK203719631855
UT-DSAEK211421132070

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Interface Haze

As measured by Pentacam densitometry (NCT02373137)
Timeframe: 3, 6, 12 months

,
Interventioneyes (Number)
Mild Interface Haze at 3 monthsModerate Interface Haze at 3 monthsSevere Interface Haze at 3 monthsMild Interface Haze at 6 monthsoderate Interface Haze at 6 monthsSevere Interface Haze at 6 monthsMild Interface Haze at 12 monthsoderate Interface Haze at 12 monthsSevere Interface Haze at 12 months
DMEK100100000
UT-DSAEK200210000

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National Eye Institute - Visual Functioning Questionnaire (NEI-VFQ)

"The National Eye Institute has developed the validated Visual Functioning Questionnaire (NEI-VFQ) to assess the effect of ocular conditions and vision on patient quality of life. The answers to the questionnaire are transformed into sub-scales, including: general health, general vision, ocular pain, near activities, distance activities, social functioning, mental health, role difficulties, dependency, driving, color vision, peripheral vision. Participants are assigned a numerical value for each sub-scale based on their answers between 0-100, where higher numbers indicate better visual function. These sub-scales are then combined according to National Eye Institute guidelines into an overall composite score for each participant. This overall composite score is also on a scale of 0-100, where higher numbers indicate better visual function.~Composite score based on National Eye Institute guidelines." (NCT02373137)
Timeframe: Baseline, 12 months

,
InterventionComposite scores on a scale (Mean)
Baseline12 Months
DMEK72.387.3
UT-DSAEK72.585.9

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Graft Thickness

As measured by Optical coherence tomography (OCT) and Pachymetry (NCT02373137)
Timeframe: 3, 6, 12, 24 months

,
Interventionroot mean square in micrometers (Mean)
3 months6 months12 months24 months
DMEK516.5519.67521.36526.88
UT-DSAEK589.36592.24585.96593.67

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Best Spectacle-Corrected Visual Acuity

The BSCVA was recorded at 4 meters by a masked refractionist certified for the study using a protocol adapted from the Age-Related Eye Disease Study using Early Treatment Diabetic Retinopathy Study charts: chart R(2110), chart 1(2111), and chart 2(2112) (Precision Vision, Woodstock, IL). (NCT02373137)
Timeframe: 24 Months

InterventionLogMar (Mean)
UT-DSAEK0.15
DMEK0.09

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Best Spectacle-Corrected Visual Acuity

The BSCVA was recorded at 4 meters by a masked refractionist certified for the study using a protocol adapted from the Age-Related Eye Disease Study using Early Treatment Diabetic Retinopathy Study charts: chart R(2110), chart 1(2111), and chart 2(2112) (Precision Vision, Woodstock, IL). (NCT02373137)
Timeframe: 6 months

InterventionlogMAR (Mean)
UT-DSAEK0.22
DMEK0.05

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Interface Haze

As measured by Pentacam densitometry (NCT02373137)
Timeframe: 24 months

,
Interventioneyes (Number)
Mild Interface Haze at 24 monthsModerate Interface Haze at 24 monthsSevere Interface Haze at 24 months
DMEK000
UT-DSAEK010

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Number of Participants in Which H. Pylori Was Eradicated

Evaluate eradication outcome by endoscopy urease test and histology or urea breath test (NCT02547012)
Timeframe: six weeks after the end of anti-H pylori therapy.

Interventionparticipants (Number)
Esomeprazole+Amox+Levo+Tetra13
Esomeprazole+Amox+Levo21

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The Mean Scores on the 6 Item Caregiver Impact Questionnaire (CIQ)

The Caregiver Impact Questionnaire (CIQ) is a 6 item assessment addressing lack of sleep, absence from work or education, canceling of family activities, changing daily activities, feeling nervous and feeling helpless. Each of these responses is expanded to a continuous scale from 0 (no impact on caregiver) to 100 (greatest impact). The average response, i.e., score, for these 6 items is calculated. The overall caregiver's quality of life (QOL) score, also captured on the CIQ, is expressed on a ordinal response scale that ranges from 0 (worst quality of life) to 10 (best quality). The CIQ is administered to the parent every 16 weeks after randomization and occasionally at sick visits. (NCT02567825)
Timeframe: Day 1 until Day 786.

,
InterventionScore on a scale (Mean)
Caregiver impact questionnaire scoreCaregiver impact questionnaire--Caregiver's overall QOL score
Non-Surgical Management10.938.50
Surgical Management10.828.55

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The Mean Scores on the 6 Item Quality of Life Survey Questionnaire (OM-6)

The OM-6 is a 6 item quality of life assessment addressing physical suffering, hearing loss, speech impairment, emotional distress, activity limitations and caregiver concerns. Responses are regarded on an ordinal scale ranging from 1 (no problem) to 7 (greatest problem). The average response, i.e., score, for these 6 items is calculated. The overall child's quality of life (QOL) score, also captured on the OM-6, is expressed on an ordinal response scale that ranges from 0 (worst quality of life) to 10 (best quality). A OM-6 is administered to the parent every 16 weeks after randomization and occasionally at sick visits. (NCT02567825)
Timeframe: Day 1 until Day 786.

,
InterventionScore on a scale (Mean)
OM-6 survey scoreOM-6 survey--Children's overall QOL score
Non-Surgical Management1.558.37
Surgical Management1.58.45

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The Rate of Occurrence of Acute Otitis Media (AOM) Episodes Per Child-Year According to the Estimated Risk of Acute Otitis Media (AOM) Recurrences at Enrollment

An episode of AOM is considered a discrete occurrence if symptoms and signs persisted for, or recurred, >=17 days after the start of antimicrobial treatment. The rate is calculated by dividing the total # of occurrences by the total # of years of follow-up. Risk of recurrences was based on early age of onset of AOM; numerous and/or frequent previous AOM episodes; receipt of multiple courses of antibiotic; eligibility for enrollment first evident during warm-weather months; parental characterization of previous AOM episodes as severe; eligibility for enrollment despite nonexposure to other young children; moderate or marked tympanic membrane (TM) bulging with previous AOM episodes; most previous AOM episodes in both ears; and a high score on the Acute Otitis Media Severity of Symptom scale (with scores ranging from 0 to 10 and higher scores indicating greater severity of symptoms) during screening and/or at enrollment. Multiple imputation was used when follow-up was incomplete. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of actual follow-up was 662 days / 1.8 years. For each child with incomplete 2-year follow-up, multiple imputation was used and values for the remaining days/years were imputed.

,
InterventionOccurrences per child-year (Mean)
Children considered at low risk of AOM recurrenceChildren considered at high risk of AOM recurrence
Non-Surgical Management1.561.56
Surgical Management1.281.67

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The Total Cost of Management of Recurrent Acute Otitis Media Per Quality Adjusted Life Days (QALDs) as a Measure of Cost-Effectiveness According to the Estimated Risk of Acute Otitis Media Recurrences at Enrollment

Total costs in US dollars were calculated by summing costs of lost wages, office visits, medical procedures, hospitalizations, and medications. Total QALDs were calculated by summing daily utility values. A utility value of 1.0 was assumed for days without AOM, otorrhea, or hospitalization. For days where these states were reported, published utility values associated with each state were used. To arrive at the final measure, total costs were divided by total utility values. The estimated risk of AOM at enrollment is described under both Baseline Characteristics and Outcome Measure #2. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of actual follow-up was 662 days / 1.8 years.

,
InterventionUS dollars per quality adjusted life day (Number)
Children considered at low risk of AOM recurrenceChildren considered at high risk of AOM recurrence
Non-Surgical Management5.705.91
Surgical Management6.258.00

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The Distribution of Children With a Penicillin-Nonsusceptible Nasopharyngeal or Throat Isolate At Any Follow-up Visit According to the Colonization Status at Enrollment

Throat specimens were obtained mainly from children older than 24 months of age. The penicillin-nonsusceptible pathogens considered are penicillin-intermediate and penicillin-resistant Streptococcus pneumoniae and ß-lactamase-positive Haemophilus influenzae. Susceptibility to penicillin was defined as follows: susceptible as a minimum inhibitory concentration (MIC) of <0.1 μg/mL; intermediate as an MIC of 0.1 to 1μg/mL; and resistant as an MIC of >1 μg/mL. (NCT02567825)
Timeframe: Day 1 until Day 786.

InterventionParticipants (Count of Participants)
No pathogens at enrollment72440667No pathogens at enrollment72440668Positive only for at least 1 penicillin-susceptible pathogen at enrollment72440667Positive only for at least 1 penicillin-susceptible pathogen at enrollment72440668Positive for at least 1 penicillin-nonsusceptible pathogen at enrollment72440667Positive for at least 1 penicillin-nonsusceptible pathogen at enrollment72440668
Penicillin-nonsusceptible isolate at a follow-up vNo penicillin-nonsusceptible isolate at a follow-u
Surgical Management25
Non-Surgical Management24
Surgical Management12
Non-Surgical Management11
Surgical Management22
Non-Surgical Management20
Surgical Management11
Non-Surgical Management15
Surgical Management38
Non-Surgical Management34
Surgical Management5
Non-Surgical Management9

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The Mean Days Per Year Children Receive Systemic Antimicrobials for AOM

Systemic antibiotics include Amoxicillin-Clavulanate, Ceftriaxone, Cefdinir, Amoxicillin, Azithromycin, Clindamycin, Levofloxacin, Bactrim, Cefprozil, Omnicef and Trimethoprim-Sulfamethoxazole. The days per year, for each child, is calculated by dividing the total number of days the child receives systemic antimicrobials for AOM (based on the recorded start and stop dates) by the total number of years of follow-up. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of follow-up was 662 days / 1.8 years.

InterventionDays per year (Mean)
Surgical Management8.76
Non-Surgical Management12.92

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The Mean Days Per Year Children Experience Tube Otorrhea

Adverse events, including tube-associated otorrhea, were collected from enrollment through the end of study. Each study visit included a review of adverse events. Any such event that occurred since the previous visit was recorded, including the date of onset and the date of resolution. For each child, the days per year of tube otorrhea is calculated by dividing the total number of days of tube otorrhea (based on dates of onset and resolution) by the total number of years of follow-up. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of follow-up was 662 days / 1.8 years.

InterventionDays per year (Mean)
Surgical Management7.96
Non-Surgical Management2.83

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The Mean Days Per Year Children Experience AOM Symptoms With an Intact Tympanic Membrane (TM)

For a given child, if a day of follow-up coincides with a study visit, the status of the right and left TMs are recorded at the ear exam. If a day of follow-up does not coincide with a study visit the status of each TM is assumed to be the same as the status on the prior day. Scores are used from the 5-item Acute Otitis Media Severity of Symptoms (AOM-SOS) scale (version 4.0) in which parents are asked to rate symptoms, as compared with the child's usual state, as none, a little, or a lot, with corresponding scores of 0, 1, and 2. Total scores range from 0 to 10, with higher scores indicating greater severity of symptoms. Scores are recorded at study visits and on diaries. The total number of days with an intact TM and a AOM-SOS score greater than or equal to 1 is divided by the total number of years of follow-up to arrive at the days per year with AOM symptoms and an intact TM. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of follow-up was 662 days / 1.8 years.

InterventionDays per year (Mean)
Surgical Management2.00
Non-Surgical Management8.33

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The Mean Score Representing Parental Satisfaction With Clinical Management

At the end-of-study visit, parents were asked to rate their level of satisfaction with their child's assigned management using a 5-point scale with higher numbers indicating greater satisfaction, specifically 1 = very dissatisfied, 2 = somewhat dissatisfied, 3 = neither satisfied nor dissatisfied, 4 = somewhat satisfied, and 5 = very satisfied. (NCT02567825)
Timeframe: The end-of-study visit. The mean day for this visit was 726.

InterventionScore on a scale (Mean)
Surgical Management4.64
Non-Surgical Management4.43

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The Rate of Occurrence of Acute Otitis Media (AOM) Episodes Per Child-Year

An episode of AOM is considered a discrete occurrence if symptoms and signs persisted for, or recurred, 17 or more days after the start of antimicrobial treatment. The rate is calculated by dividing the total number of occurrences by the total number of years of follow-up. Multiple imputation was used when follow-up was incomplete. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of actual follow-up was 662 days / 1.8 years. For each child with incomplete 2-year follow-up, multiple imputation was used and values for the remaining days/years were imputed.

InterventionOccurrences per child-year (Mean)
Surgical Management1.48
Non-Surgical Management1.56

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The Time to the First Episode of AOM

The time to the first episode of AOM is defined as the time, expressed in months, from randomization until the first episode of AOM. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of follow-up was 662 days / 21.8 months.

InterventionMonths (Median)
Surgical Management4.34
Non-Surgical Management2.33

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The Total Cost of Management of Recurrent Acute Otitis Media Per Quality Adjusted Life Days (QALDs) as a Measure of Cost-Effectiveness

Total costs in US dollars were calculated by summing costs of lost wages, office visits, medical procedures, hospitalizations, and medications. Total QALDs were calculated by summing daily utility values. A utility value of 1.0 was assumed for days without AOM, otorrhea, or hospitalization. For days where these states were reported, published utility values associated with each state were used. To arrive at the final measure, total costs were divided by total utility values. (NCT02567825)
Timeframe: Day 1 until Day 786. The mean length of actual follow-up was 662 days / 1.8 years.

InterventionUS dollars per quality adjusted life day (Number)
Surgical Management7.19
Non-Surgical Management5.79

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Number of Participants in Which H. Pylori Was Eradicated

Number of participants with negative H pylori status in follow-up tests as a measure of successful eradication (NCT02978157)
Timeframe: six weeks after the end of anti-H pylori therapy.

Interventionparticipants (Number)
Esomeprazole+Amox+Levo36
Esomeprazole+Bismuth+Tetra+Levo49

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Nemnoxacin Concentration Changes

"Cmax - The peak Nemonoxacin concentration at Day 1-2 of treatment~C-22.5hours - 22.5-h drug concentration of Nemonoxacin" (NCT03551210)
Timeframe: Day 1 pre-dose and 0, 0.5, 2.5, 4, 6, 12, 16 and 22.5 (= Day 2 pre-dose) hrs after the end of first infusion on Day 1 of treatment

Interventionng/ml (Mean)
CmaxC-22.5hours
Nemonoxacin8163.84359.63

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Number of Patients With Microbiological Success

Microbiological response is evaluated as microbiological success if culture study demonstrates eradication of pathogen or no material available for culture because of clinical success (NCT03551210)
Timeframe: Visit 2 (day 4/8 ot treatment), 3 (within 1-2 days after last dose), 4 (within 7-9 days after last dose)

,
InterventionParticipants (Count of Participants)
Visit 2Visit 3Visit 4
Nemonoxacin171919
Tavanic®161616

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Number of Patients With Clinical Success as Judged by the Investigator

Clinical response is evaluated as clinical success if: all signs and symptoms of pneumonia are resolved or improved with no worsening or appearance of new signs and symptoms of pneumonia; there is no requirement for additional antibiotic therapy (NCT03551210)
Timeframe: Visit 2(day 4/8 ot treatment), Visit 3 (within 1-2 days after last dose)

InterventionParticipants (Count of Participants)
Visit 272195661Visit 272195662Visit 372195662Visit 372195661
Clinical successClinical non-efficacyIndefinite response
Nemonoxacin164
Tavanic®154
Nemonoxacin4
Tavanic®5
Nemonoxacin1
Nemonoxacin160
Tavanic®151
Nemonoxacin6
Tavanic®7
Nemonoxacin3
Tavanic®8

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Number of Patients Required for Other Antibiotic Treatment

(NCT03551210)
Timeframe: Up to 21-23 days after last dose

InterventionParticipants (Count of Participants)
Nemonoxacin2
Tavanic®5

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Number of Patients With Infection Relapse

(NCT03551210)
Timeframe: Visit 5 (within 21-23 days after last dose)

InterventionParticipants (Count of Participants)
Nemonoxacin0
Tavanic®2

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Terminal Elimination Half-life (T1/2) of Nemonoxacin

Terminal elimination half-life of Nemonoxacin (NCT03551210)
Timeframe: Day 1 pre-dose and 0, 0.5, 2.5, 4, 6, 12, 16 and 22.5 (= Day 2 pre-dose) hrs after the end of first infusion on Day 1 of treatment

Interventionhours (Mean)
Nemonoxacin7.04

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Time to Switch Therapy From Intravenous to Oral Therapy

(NCT03551210)
Timeframe: Up to Visit 2 (day 4/8 ot treatment)

Interventiondays (Median)
Nemonoxacin4
Tavanic®4

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Volume of Distribution at Steady State (Vss) of Nemonoxacin

Volume of distribution at steady state of Nemonoxacin (NCT03551210)
Timeframe: Day 1 pre-dose and 0, 0.5, 2.5, 4, 6, 12, 16 and 22.5 (= Day 2 pre-dose) hrs after the end of first infusion on Day 1 of treatment

Interventionliters (Mean)
Nemonoxacin123.76

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Сlearance (CL) of Nemonoxacin

Total systemic clearance of Nemonoxacin (NCT03551210)
Timeframe: Day 1 pre-dose and 0, 0.5, 2.5, 4, 6, 12, 16 and 22.5 (= Day 2 pre-dose) hrs after the end of first infusion on Day 1 of treatment

Interventionml/min (Mean)
Nemonoxacin247.32

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Area Under the Concentration-time Curve (AUC) of Nemonoxacin

"AUC (0-22.5) - Area under the concentration-time curve from 0 to 22.5 hours of Nemonoxacin~AUC(0-∞) - Areas under the concentration-time curve from 0 h to infinity of Nemonoxacin" (NCT03551210)
Timeframe: Day 1 pre-dose and 0, 0.5, 2.5, 4, 6, 12, 16 and 22.5 (= Day 2 pre-dose) hrs after the end of first infusion on Day 1 of treatment

Interventionhours*ng/ml (Mean)
AUC (0-22.5)AUC(0-∞)
Nemonoxacin34372.6938560.90

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Intraocular Pressure (IOP)

IOP is measured using a tonometer. IOP is measured as mmHg; normal intraocular pressures average between 12-22 mm Hg. (NCT03739528)
Timeframe: At day 0 (screening) and at day 4, 8, 15

,
InterventionmmHg (Mean)
Visit 1 - ScreeningVisit 3 - Day 4Visit 4 - Day 8Visit 5 - Day 15
Levofloxacin + Dexamethasone Followed by Dexamethasone15.1614.2614.2914.45
Tobramycin + Dexamethasone15.1214.4914.4514.37

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Ocular Pain/Discomfort: 4-point Scale

Overall ocular pain and discomfort was evaluated by the subject on a 4-point scale (0 = absent, 1 = mild, 2 = moderate, 3 = severe). (NCT03739528)
Timeframe: Day 4, 8, 15

InterventionParticipants (Count of Participants)
Visit 3 - Day 4: Presence/absence of ocular pain72467252Visit 3 - Day 4: Presence/absence of ocular pain72467251Visit 4 - Day 8: Presence/absence of ocular pain72467251Visit 4 - Day 8: Presence/absence of ocular pain72467252Visit 5 - Day 15: Presence/absence of ocular pain72467252Visit 5 - Day 15: Presence/absence of ocular pain72467251
Score=0Score>0
Levofloxacin + Dexamethasone Followed by Dexamethasone360
Tobramycin + Dexamethasone361
Levofloxacin + Dexamethasone Followed by Dexamethasone35
Tobramycin + Dexamethasone32
Levofloxacin + Dexamethasone Followed by Dexamethasone366
Tobramycin + Dexamethasone366
Levofloxacin + Dexamethasone Followed by Dexamethasone29
Tobramycin + Dexamethasone27
Levofloxacin + Dexamethasone Followed by Dexamethasone377
Tobramycin + Dexamethasone373
Levofloxacin + Dexamethasone Followed by Dexamethasone18
Tobramycin + Dexamethasone20

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Adverse Events

Adverse events were described according to System Organ Classes (SOC) and Preferred Terms (PT) using the Medical Dictionary for Regulatory Activities (MedDRA) and were presented by treatment group. (NCT03739528)
Timeframe: During all the treatment until day 15

,
InterventionParticipants (Count of Participants)
Patients with TEAEsPatients with serious TEAEsPatients with TEAEs suspected to be study relatedPatients with TEAEs leading to discontinuationPatients with fatal TEAEsPatients with severe TEAEs
Levofloxacin + Dexamethasone Followed by Dexamethasone56426413
Tobramycin + Dexamethasone51226300

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Number of Participants Without Signs of Anterior Ocular Chamber Inflammation

Number of participants without signs of anterior chamber inflammation (sum of cells and flare score = 0). (NCT03739528)
Timeframe: Day 0 (screening), 4, 8

InterventionParticipants (Count of Participants)
Visit 1 - Screening72467251Visit 1 - Screening72467252Visit 3 - Day 472467252Visit 3 - Day 472467251Visit 4 - Day 872467252Visit 4 - Day 872467251
Number of participants without signsNumber of participants with signs
Levofloxacin + Dexamethasone Followed by Dexamethasone395
Tobramycin + Dexamethasone393
Levofloxacin + Dexamethasone Followed by Dexamethasone0
Tobramycin + Dexamethasone0
Levofloxacin + Dexamethasone Followed by Dexamethasone289
Tobramycin + Dexamethasone302
Levofloxacin + Dexamethasone Followed by Dexamethasone106
Tobramycin + Dexamethasone91
Levofloxacin + Dexamethasone Followed by Dexamethasone338
Tobramycin + Dexamethasone341
Levofloxacin + Dexamethasone Followed by Dexamethasone57
Tobramycin + Dexamethasone52

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Conjunctival Hyperemia

Conjunctival hyperemia was evaluated with slit lamp and results provided as a score as follows: 0 = absence of inflammation, 1 = mild inflammation (some vessels injected), 2 = moderate inflammation (diffuse injection of vessels, but individual vessels are still discernable) 3 = severe inflammation (intense injection of vessels, individual vessels not easily discernable). (NCT03739528)
Timeframe: Day 4, 8, 15

InterventionParticipants (Count of Participants)
Visit 3 - Day 472467252Visit 3 - Day 472467251Visit 4 - Day 872467251Visit 4 - Day 872467252Visit 5 - Day 1572467252Visit 5 - Day 1572467251
Score>0Score=0
Levofloxacin + Dexamethasone Followed by Dexamethasone337
Tobramycin + Dexamethasone323
Levofloxacin + Dexamethasone Followed by Dexamethasone58
Tobramycin + Dexamethasone70
Levofloxacin + Dexamethasone Followed by Dexamethasone348
Tobramycin + Dexamethasone358
Levofloxacin + Dexamethasone Followed by Dexamethasone47
Tobramycin + Dexamethasone35
Levofloxacin + Dexamethasone Followed by Dexamethasone371
Tobramycin + Dexamethasone375
Levofloxacin + Dexamethasone Followed by Dexamethasone24
Tobramycin + Dexamethasone18

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Visual Acuity

"Visual acuity was assessed as per local clinical practice, i.e. with the Snellen (feet) or the ETDRS (meter) chart. Visual acuity was then analysed using decimal unit. Decimal score is the decimal expression of the Snellen (feet) or the ETDRS (meter) charts in which the numerator indicates the distance from the chart and the denominator indicates the size of the smallest line that can be read. Decimal values were provided directly from the investigator or computed as a result of the Snellen or ETDRS fraction.~Generally decimal values from 0.01 to 0.10 indicate severe vision loss; decimal values from 0.125 to 0.25 indicate moderate vision loss; decimal values from 0.32 to 0.63 indicate mild vision loss; decimal values from 0.8 to 1.6 indicate normal vision.~Lower decimal values correspond to a reduced visual acuity and worst outcomes, while higher decimal values indicate an improved visual acuity and better outcomes." (NCT03739528)
Timeframe: At day 0 (screening) and at day 15

,
Interventiondecimal score (Mean)
Visit 1 - ScreeningVisit 5 - Day 15
Levofloxacin + Dexamethasone Followed by Dexamethasone0.410.88
Tobramycin + Dexamethasone0.410.89

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Total Ocular Symptoms Score (TOSS)

The TOSS is a patient-reported evaluation in the TOSS Questionnaire of 3 ocular symptoms: itching/burning, hyperemia of conjunctiva and tearing. A score was given in the presence of symptoms: 0 = none, 1 = mild, 2 = moderate, 3 = severe. (NCT03739528)
Timeframe: Day 4, 8, 15

,
Interventionscore on a scale (Mean)
Visit 3 - Day 4Visit 4 - Day 8Visit 5 - Day 15
Levofloxacin + Dexamethasone Followed by Dexamethasone0.290.280.17
Tobramycin + Dexamethasone0.370.260.17

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Number of Participants With Endophthalmitis

The number of participants with endophthalmitis after administration of study treatment in the study was assessed and reported. Diagnosis of endophthalmitis is based on clinical evaluation of signs and symptoms (such as swollen eyelids, ocular pain, conjunctival hyperemia, decreased visual acuity, opaque vitreous) through slit lamp examination, and microbiological tests on conjunctival or corneal swabs. (NCT03739528)
Timeframe: Day 4, 8, 15

,
InterventionParticipants (Count of Participants)
Visit 3 - Day 4: no diagnosis of endophthalmitisVisit 4 - Day 8: no diagnosis of endophthalmitisVisit 5 - Day 15: no diagnosis of endophthalmitis
Levofloxacin + Dexamethasone Followed by Dexamethasone393391389
Tobramycin + Dexamethasone393393391

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Global Evaluation of Local Tolerability

Global evaluation was evaluated on a 4-point scale: 0 = no intolerability, 1 = mild intolerability, 2 = moderate intolerability, 3 = maximum intolerability. (NCT03739528)
Timeframe: Day 4, 8, 15

,
Interventionscore on a scale (Mean)
Visit 3 - Day 4Visit 4 - Day 8Visit 5 - Day 15
Levofloxacin + Dexamethasone Followed by Dexamethasone0.030.010.02
Tobramycin + Dexamethasone0.010.030.02

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Burning, Stinging, Blurred Vision

Burning, stinging, blurred vision were evaluated on a 4-point scale: 0 = none, 1 = mild, 2 = moderate, 3 = severe. (NCT03739528)
Timeframe: Day 4, 8, 15

,
Interventionscore on a scale (Mean)
Burning: visit 3 - day 4Burning: visit 4 - day 8Burning: visit 5 - day 15Stinging: visit 3 - day 4Stinging: visit 4 - day 8Stinging: visit 5 - day 15Blurred vision: visit 3 - day 4Blurred vision: visit 4 - day 8Blurred vision: visit 5 - day 15
Levofloxacin + Dexamethasone Followed by Dexamethasone0.080.060.070.050.070.060.060.060.03
Tobramycin + Dexamethasone0.090.110.070.040.070.040.050.040.01

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Aqueous Humour Concentration of Dexamethasone

Defined as the concentration of dexamethasone into the aqueous humour in all the three arms: Levofloxacin + Dexamethasone, Dexamethasone and Levofloxacin.The concentration of dexamethasone has been measured by LC tandem mass spectrometry. (NCT03740659)
Timeframe: 90±15 min after the first administration of the study treatments

Interventionnmol/mL (Mean)
Levofloxacin + Dexamethasone0.030
Levofloxacin0
Dexamethasone0.042

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Aqueous Humour Concentration of Dexamethasone 21-phosphate

Defined as the concentration of dexamethasone 21-phosphate into the aqueous humour in all the three arms: Levofloxacin + Dexamethasone, Dexamethasone and Levofloxacin. The concentration of dexamethasone 21-phosphate has been measured by LC tandem mass spectrometry. (NCT03740659)
Timeframe: 90±15 min after the first administration of the study treatments

Interventionnmol/mL (Mean)
Levofloxacin + Dexamethasone0
Levofloxacin0
Dexamethasone0

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Aqueous Humour Concentration of Levofloxacin

Defined as the concentration of levofloxacin into the aqueous humour in all the three arms: Levofloxacin + Dexamethasone, Dexamethasone and Levofloxacin.The concentration of levofloxacin has been measured by LC tandem mass spectrometry. (NCT03740659)
Timeframe: 90±15 min after the first administration of the study treatments

Interventionnmol/mL (Mean)
Levofloxacin + Dexamethasone1.970
Levofloxacin2.151
Dexamethasone0

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Number of Participant With Urinary Tract Infection

Urinary tract infection is defined based on the result of urinalysis in which one of the following condition present : leukocyes > 5 / high power field, bacteria positive, nitrite positive, and/or positive leukocyte esterase (NCT05219877)
Timeframe: 4 days after urodynamic

InterventionParticipants (Count of Participants)
Pre-urodynamic Levofloxacin12
Post-urodynamic Levofloxacin13

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