Page last updated: 2024-11-10

tilmicosin

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Description

tilmicosin: semi-synthetic antibiotic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tilmicosin : A macrolide antibiotic with formula C46H80N2O13. It is used for the treatment of respiratory disease in cattle at high risk of developing bovine respiratory disease associated with Mannheimia haemolytica. [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 CID45357310
MeSH IDM0148552
PubMed CID5282521
CHEMBL ID1908333
CHEBI ID195409
SCHEMBL ID149192
MeSH IDM0148552

Synonyms (78)

Synonym
108050-54-0
tilmicosin
AKOS015951255
AC-8389
D02492
micotil (tn)
tilmicosin (usp/inn)
tylosin, 4a-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-
micotil
4(sup a)-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(cis-3,5-dimethylpiperidino)tylosin
tylosin, 4(sup a)-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-, 20(cis)-
tilmicosina [inn-spanish]
hsdb 7446
tilmicosinum [inn-latin]
tilmicosine [inn-french]
pulmotil
tilmicosinum
ly 177370
tilmicosina
el 870
20-deoxy-20-(3,5-dimethylpiperidin-1-yl)-desmycosin
ly177370
el870
tilmicosine
ly-177370
el-870
CHEBI:195409
[(2r,3r,4e,6e,9r,11r,12s,13s,14r)-12-{[3,6-dideoxy-3-(dimethylamino)-beta-d-glucopyranosyl]oxy}-11-{2-[(3r,5s)-3,5-dimethylpiperidin-1-yl]ethyl}-2-ethyl-14-hydroxy-5,9,13-trimethyl-8,16-dioxo-1-oxacyclohexadeca-4,6-dien-3-yl]methyl 6-deoxy-2,3-di-o-methyl
antibiotic el 870
tox21_111546
dtxcid3026011
cas-108050-54-0
dtxsid5046011 ,
S4122
unii-xl4103x2e3
tylosin, 4a-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-((3r,5s)-3,5-dimethyl-1-piperidinyl)-
nsc 759584
tilmicosin [usan:usp:inn:ban]
xl4103x2e3 ,
nsc-759584
CHEMBL1908333
tilmicosin [who-dd]
tilmicosin [mart.]
tilmicosin [usp monograph]
tilmicosin [usp-rs]
tilmicosin [hsdb]
tilmicosin [mi]
tilmicosin [green book]
4 sup(a)-o-de(2,6-dideoxy-3-c-methyl-.alpha.-l-ribo-hexopyranosyl)-20-deoxo-20-(cis-3,5-dimethylpiperidino)tylosin
tilmicosin [usan]
tilmicosin [inn]
tylosin, 4 sup(a)-o-de(2,6-dideoxy-3-c-methyl-.alpha.-l-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-, (20(cis))-
SCHEMBL149192
JTSDBFGMPLKDCD-XVFHVFLVSA-N
tilmicosine, antibiotic for culture media use only
Q-100992
HY-B0905
AB01566912_01
AKOS030526067
NCGC00348375-02
20-deoxo-20-(3,5-dimethylpiperidin-1-yl)desmycosin
DB11471
tilmicosin 100 microg/ml in acetonitrile
Q722387
CCG-270545
NCGC00348375-01
Z2583154269
tilmovet 90
tilmicosine (inn-french)
4(superscript a)-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)tylosin
tilmicosin (mart.)
4 sup(a)-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(cis-3,5-dimethylpiperidino)tylosin
tilmicosin (usan:usp:inn:ban)
tylosin, 4 sup(a)-o-de(2,6-dideoxy-3-c-methyl-alpha-l-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)-, (20(cis))-
tilmicosinum (inn-latin)
tilmicosin (usp-rs)
tilmicosin (usp monograph)
tilmicosina (inn-spanish)

Research Excerpts

Toxicity

The present study evaluated the toxic effects of Tilmicosin (TIL) on adult rats. Administration of L-carnitine could ameliorate these adverse toxic effects in mice.

ExcerptReferenceRelevance
" However, administration of L-carnitine could ameliorate these adverse toxic effects of tilmicosin in mice."( The possible protective effect of L-carnitine on tilmicosin-induced cardiotoxicity in mice.
Citil, M; Karapehlivan, M; Kart, A; Yapar, K, 2007
)
0.34
" The high nanoparticle dose induced transient clinical symptoms of treatment effect such as transient reversible action retardation, anorexy and gloomy spirit, increased spleen and liver coefficients and decreased heart coefficients, microscopic pathological changes of liver, spleen and heart, and minor changes in hematologic and biochemical parameters, but no adverse effects were observed in the nanoparticle low dose group."( Acute toxicity study of tilmicosin-loaded hydrogenated castor oil-solid lipid nanoparticles.
Dong, Z; Li, X; Wang, F; Wang, X; Wang, Y; Xie, S; Zhou, W; Zhu, L, 2011
)
0.37
"The results revealed that the LD50 of Til-HCO-SLN and blank HCO-SLN exceeded 5 g/kg."( Acute toxicity study of tilmicosin-loaded hydrogenated castor oil-solid lipid nanoparticles.
Dong, Z; Li, X; Wang, F; Wang, X; Wang, Y; Xie, S; Zhou, W; Zhu, L, 2011
)
0.37
" We conclude that myrrh and (or) vitamin C administration minimizes the toxic effects of TIL through their free-radical-scavenging and potent antioxidant activities."( Synergistic protective role of mirazid (Commiphora molmol) and ascorbic acid against tilmicosin-induced cardiotoxicity in mice.
Abdel-Daim, MM; Fayez, M; Ghazy, EW, 2015
)
0.42
"The present study evaluated the toxic effects of Tilmicosin (TIL) on adult rats."( Astragalus polysaccharides alleviate tilmicosin-induced toxicity in rats by inhibiting oxidative damage and modulating the expressions of HSP70, NF-kB and Nrf2/HO-1 pathway.
Ahmed, SYA; Alagawany, M; Elhady, WM; Farag, MR; Taha, HSA, 2019
)
0.51

Pharmacokinetics

The intravenous pharmacokinetic profile of tilmicosin is yet to be achieved because of the cardiovascular effects.

ExcerptReferenceRelevance
" The elimination half-life (t1/2 beta) values for 3 cows were 46."( Tilmicosin antibacterial activity and pharmacokinetics in cows.
Glickman, A; Saran, A; Shem-Tov, M; Winkler, M; Ziv, G, 1995
)
0.29
" Various pharmacokinetic parameters including area under plasma concentration-time curve (AUC(0-72)), maximum plasma concentration (C(max)), time to peak concentration (t(max)), elimination half-life (t(1/2beta)), elimination rate (k(el)), clearance (Cl(B)), mean residence time (MRT) and volume of distribution (V(d,area)) were determined for both formulations."( Pharmacokinetics of tilmicosin (Provitil powder and Pulmotil liquid AC) oral formulations in chickens.
Abu-Basha, EA; Al-Shunnaq, AF; Idkaidek, NM, 2007
)
0.34
" A pharmacokinetic study evaluated the disposition of tilmicosin in the horse after oral (4 mg/kg) or subcutaneous (s."( Pharmacokinetics of tilmicosin in equine tissues and plasma.
Boison, JO; Clark, C; Dowling, PM; Ross, S; Woodbury, M, 2008
)
0.35
"The intravenous pharmacokinetic profile of tilmicosin is yet to be achieved because of the cardiovascular effects of tilmicosin."( Pharmacokinetics of tilmicosin in beef cattle following intravenous and subcutaneous administration.
Hassfurther, R; Hunter, RP; Lombardi, KR; Portillo, T, 2011
)
0.37
"23 µg/mL, the time required to reach the peak concentration (t max) was found to be 2nd and 4th h, and elimination half-lives (t 1/2β ) were found to be 20."( Milk and blood pharmacokinetics of tylosin and tilmicosin following parenteral administrations to cows.
Avci, T; Elmas, M, 2014
)
0.4
" Finally, a pharmacokinetic study was performed."( Preparation, characterization, and pharmacokinetics of tilmicosin taste-masked formulation via hot-melt extrusion technology.
Deng, R; Deng, X; Feng, X; He, J; Ji, M; Liang, Q; Lv, L; Peng, J; Wen, X; Wu, L; Yan, G, 2020
)
0.56

Compound-Compound Interactions

ExcerptReferenceRelevance
" Left ventricular function, systemic arterial blood pressure, and heart rate (HR) responses to TM alone and in combination with propranolol(P) or dobutamine HCl(DOB) were evaluated."( Cardiovascular effects of the macrolide antibiotic tilmicosin, administered alone and in combination with propranolol or dobutamine, in conscious unrestrained dogs.
Main, BW; Means, JR; Rinkema, LE; Sarazan, RD; Smith, WC, 1996
)
0.29
" Despite that, little is comprehended about influences of the drug-drug interactions (DDIs) caused by EF and TIM."( A new drug-drug interaction-tilmicosin reduces the metabolism of enrofloxacin through CYP3A4.
Badawy, S; Liu, Z; Tao, Y; Wang, L; Wang, X; Xie, C; Zhang, L, 2022
)
0.72

Bioavailability

TMS-sNLCs were the most efficient drug delivery carriers, with a relative oral bioavailability of 203. NLCs could enhance oral absorption of TMS compared to 10% tilmicosin phosphate solution in broilers.

ExcerptReferenceRelevance
" bioavailability was 22%."( Tilmicosin antibacterial activity and pharmacokinetics in cows.
Glickman, A; Saran, A; Shem-Tov, M; Winkler, M; Ziv, G, 1995
)
0.29
"A bioavailability and pharmacokinetics study of powder and liquid tilmicosin formulations was carried out in 18 healthy chickens according to a single-dose, two-period, two-sequence, crossover randomized design."( Pharmacokinetics of tilmicosin (Provitil powder and Pulmotil liquid AC) oral formulations in chickens.
Abu-Basha, EA; Al-Shunnaq, AF; Idkaidek, NM, 2007
)
0.34
" The data from the two different studies were used to calculate bioavailability values, which support the assumption that tilmicosin is 100% bioavailable in cattle."( Pharmacokinetics of tilmicosin in beef cattle following intravenous and subcutaneous administration.
Hassfurther, R; Hunter, RP; Lombardi, KR; Portillo, T, 2011
)
0.37
" Furthermore, TMS-NLCs showed higher oral bioavailability in piglets compared to the API suspension."( Nanostructured lipid carriers with exceptional gastrointestinal stability and inhibition of P-gp efflux for improved oral delivery of tilmicosin.
Gao, X; Guo, D; Ji, H; Jiang, S; Li, X; Peng, L; Sahito, B; Wang, L; Yang, H; Zhang, Q, 2020
)
0.56
" NLCs could enhance oral absorption of TMS compared to 10% tilmicosin phosphate solution in broilers, among which the TMS-sNLCs were the most efficient drug delivery carriers, with a relative oral bioavailability of 203."( Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation.
Gao, X; Guo, D; Jiang, S; Kashif, J; Peng, L; Sahito, B; Ul Aabdin, Z; Wang, L; Yang, H; Zhang, Q, 2020
)
0.56
"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

Dosage Studied

Tilmicosin is a veterinary antibiotic with significant human toxicity at doses commonly used in animals. The parenteral dose-response relationship has not been well characterized. Treatment with tilmicosIn was effective at all dosage levels, as determined by significant (P less than or equal to 0.1) Residue depletion of tilmicOSin in broiler chickens was examined after dosing over a 5-day period.

ExcerptRelevanceReference
"To determine the effective dosage of tilmicosin phosphate when fed to pigs for the control of pneumonia attributable to Actinobacillus pleuropneumoniae."( Efficacy dose determination study of tilmicosin phosphate in feed for control of pneumonia caused by Actinobacillus pleuropneumoniae in swine.
Lechtenberg, KF; Moore, GM; Mowrey, DH; Schneider, JH; Tonkinson, LV, 1996
)
0.29
" The method was tested on milk from a cow dosed with tilmicosin."( Determination of tilmicosin in bovine milk by liquid chromatography with ultraviolet detection.
Ngoh, MA,
)
0.13
"0 mg/kg) were administered to complete a dose-response curve."( Cardiovascular effects of the macrolide antibiotic tilmicosin, administered alone and in combination with propranolol or dobutamine, in conscious unrestrained dogs.
Main, BW; Means, JR; Rinkema, LE; Sarazan, RD; Smith, WC, 1996
)
0.29
"When intermittent dosing is used during treatment, the concentrations of antibiotics fluctuate and subinhibitory concentrations may occur between doses."( Postantibiotic effects and postantibiotic sub-MIC effects of erythromycin, roxithromycin, tilmicosin, and tylosin on Pasteurella multocida.
Lim, J; Yun, H, 2001
)
0.31
"Three studies were conducted to determine and confirm the effective dosage rate of ceftiofur crystalline-free acid sterile suspension (CCFA-SS, 200 mg ceftiofur equivalents [CE]/ml), a long-acting ceftiofur formulation, for control and treatment of bovine respiratory disease (BRD)."( Dose determination and confirmation for ceftiofur crystalline-free acid administered in the posterior aspect of the ear for control and treatment of bovine respiratory disease.
Bryson, WL; Chester, ST; Dame, KJ; Hibbard, B; Moseley, WW; Robb, EJ, 2002
)
0.31
" Residue depletion of tilmicosin in broiler chickens was examined after dosing over a 5-day period by incorporation of the drug into drinking water at 37."( Residue depletion of tilmicosin in chicken tissues.
Fu, C; Guo, J; Jiang, H; Jin, X; Shen, J; Shen, Z; Zhang, Y, 2004
)
0.32
"Administration of erythromycin, tilmicosin, and tylosin at the label dosage increased abomasal emptying rate in calves."( Effect of parenteral administration of erythromycin, tilmicosin, and tylosin on abomasal emptying rate in suckling calves.
Constable, PD; Nouri, M, 2007
)
0.34
"Tilmicosin is a veterinary antibiotic with significant human toxicity at doses commonly used in animals, but the parenteral dose-response relationship has not been well characterized."( American association of poison control centers database characterization of human tilmicosin exposures, 2001-2005.
Oakes, J; Seifert, S, 2008
)
0.35
" A dose-response relationship could be demonstrated."( American association of poison control centers database characterization of human tilmicosin exposures, 2001-2005.
Oakes, J; Seifert, S, 2008
)
0.35
"5 times of the clinic dosage and below the median lethal dose (LD(50)) was subcutaneously administered twice on the first and 7th day."( Acute toxicity study of tilmicosin-loaded hydrogenated castor oil-solid lipid nanoparticles.
Dong, Z; Li, X; Wang, F; Wang, X; Wang, Y; Xie, S; Zhou, W; Zhu, L, 2011
)
0.37
" Normal clinic dosage of Til-HCO-SLN is safe as evaluated by acute toxicity."( Acute toxicity study of tilmicosin-loaded hydrogenated castor oil-solid lipid nanoparticles.
Dong, Z; Li, X; Wang, F; Wang, X; Wang, Y; Xie, S; Zhou, W; Zhu, L, 2011
)
0.37
" Dosing to achieve MPC concentrations (where possible) may serve to reduce the selection of bacterial subpopulations with reduced antimicrobial susceptibility."( Comparative minimum inhibitory and mutant prevention drug concentrations of enrofloxacin, ceftiofur, florfenicol, tilmicosin and tulathromycin against bovine clinical isolates of Mannheimia haemolytica.
Blondeau, BJ; Blondeau, JM; Blondeau, LD; Borsos, S; Hesje, CE, 2012
)
0.38
" None of the three suspensions were cytotoxic at clinical dosage levels."( Preparation and evaluation of tilmicosin-loaded hydrogenated castor oil nanoparticle suspensions of different particle sizes.
Chen, X; Lu, M; Wang, T; Wang, Y; Zhou, W; Zhu, L, 2014
)
0.4
" MPC concentrations provide a dosing target which may serve to reduce amplification of bacterial subpopulations with reduced antimicrobial susceptibility."( Mutant prevention and minimum inhibitory concentration drug values for enrofloxacin, ceftiofur, florfenicol, tilmicosin and tulathromycin tested against swine pathogens Actinobacillus pleuropneumoniae, Pasteurella multocida and Streptococcus suis.
Blondeau, JM; Fitch, SD, 2019
)
0.51
" The blood samples were taken before dosing and at 4th, 8th, 24th and 72nd hour post-dosing for measurement of cardiac markers such as H-FABP, cTn-I, CK-MB."( The effect of tilmicosin and diclofenac sodium combination on cardiac biomarkers in sheep.
Atik, O; Corum, O; Durna Corum, D; Ider, M; Ok, M; Uney, K; Yildiz, R, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
cardiotoxic agentA role played by a chemical compound exihibiting itself through the ability to induce damage to the heart and cardiomyocytes.
antibacterial drugA drug used to treat or prevent bacterial infections.
calcium channel blockerOne of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools.
[role 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]

Drug Classes (3)

ClassDescription
macrolide antibioticA macrocyclic lactone with a ring of twelve or more members which exhibits antibiotic activity.
monosaccharide derivativeA carbohydrate derivative that is formally obtained from a monosaccharide.
enoneAn alpha,beta-unsaturated ketone of general formula R(1)R(2)C=CR(3)-C(=O)R(4) (R(4) =/= H) in which the C=O function is conjugated to a C=C double bond at the alpha,beta position.
[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 (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency29.84930.000221.22318,912.5098AID743040
cytochrome P450 2D6Homo sapiens (human)Potency23.91850.00108.379861.1304AID1645840
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency6.30960.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID117681Protective dose at which 50% of infected, treated mice survive1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID1231422Antibacterial activity against Bacillus cereus ATCC 14579 assessed as growth inhibition at 15 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.
AID261794Antibacterial activity against Staphylococcus epidermidis ATCC 122282006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261781Antibacterial activity against Streptococcus pneumoniae ATCC 63012006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID26832Dissociation constant (pKa)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID261793Antibacterial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID19403Calculated partition coefficient (logD)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID19662Calculated partition coefficient (clogP)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID261795Antibacterial activity against Enterococcus faecalis ATCC 515752006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID1231425Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as growth inhibition at 15 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.
AID261786Antibacterial activity against macrolide resistant Streptococcus pneumoniae ATCC 7009062006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261787Antibacterial activity against Streptococcus pneumoniae ATCC 496192006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261784Antibacterial activity against macrolide resistant Streptococcus pneumoniae ATCC 7006772006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID23096The negative logarithm of the fraction of neutral molecules1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID261785Antibacterial activity against macrolide resistant Streptococcus pneumoniae ATCC 7009052006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261783Antibacterial activity against macrolide resistant Streptococcus pneumoniae ATCC 7006762006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261788Antibacterial activity against Staphylococcus aureus ATCC 6538p2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID117677Protected dose at which the test compound protects 50% of challenged mice from death owing to the Pasteurella multocida infection1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Repromicin derivatives with potent antibacterial activity against Pasteurella multocida.
AID1231424Antibacterial activity against Escherichia coli ATCC 35218 assessed as growth inhibition at 15 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.
AID1231423Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as growth inhibition at 15 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.
AID24865The negative logarithm of the fraction of singly charged molecules.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID23733Calculated partition coefficient (clogP)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID26629Dissociation constant (pKa)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID21658Calculated partition coefficient (clogP)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID155915Minimum inhibitory concentration against Pasteurella multocida.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID155774Minimum inhibitory concentration required to inhibit Pasteurella multocida 59A006 in vitro1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Repromicin derivatives with potent antibacterial activity against Pasteurella multocida.
AID261791Antibacterial activity against macrolide resistant Staphylococcus aureus ATCC BAA-392006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261782Antibacterial activity against Streptococcus pneumoniae ATCC 7006712006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261792Antibacterial activity against macrolide resistant Staphylococcus aureus ATCC BAA-442006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID19425HPLC capacity factor (k)1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Quantitative structure-activity relationships among macrolide antibacterial agents: in vitro and in vivo potency against Pasteurella multocida.
AID261789Antibacterial activity against macrolide resistant Staphylococcus aureus ATCC 335912006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
AID261790Antibacterial activity against macrolide resistant Staphylococcus aureus ATCC 1415412006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and in vitro antibiotic activity of 16-membered 9-O-arylalkyloxime macrolides.
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.
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.
AID1347159Primary screen GU Rhodamine 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.
AID1347160Primary 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (247)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (1.62)18.7374
1990's54 (21.86)18.2507
2000's95 (38.46)29.6817
2010's66 (26.72)24.3611
2020's28 (11.34)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 54.03

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 Index54.03 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index86.91 (26.88)
Search Engine Supply Index2.16 (0.95)

This Compound (54.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials51 (19.62%)5.53%
Trials0 (0.00%)5.53%
Reviews3 (1.15%)6.00%
Reviews0 (0.00%)6.00%
Case Studies4 (1.54%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other202 (77.69%)84.16%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]