Page last updated: 2024-11-05

melarsoprol

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Description

Melarsoprol is an arsenic-containing drug used to treat the late-stage, neurological form of African trypanosomiasis (sleeping sickness) caused by Trypanosoma brucei gambiense. It is synthesized through a complex multi-step process involving the reaction of 4-amino-phenylarsonic acid with 3-hydroxypropanal in the presence of hydrochloric acid and sodium chloride. Melarsoprol exhibits trypanocidal activity by inhibiting the enzyme trypanothione reductase, which is essential for the survival of Trypanosoma brucei. The drug has been effective in treating late-stage sleeping sickness, but it can cause severe side effects, including encephalopathy, coma, and death. Due to its toxicity, melarsoprol is typically reserved for cases where other treatments have failed. The high toxicity of melarsoprol has led to research efforts aimed at developing safer and more effective trypanocidal drugs. Research on melarsoprol focuses on understanding its mechanism of action, developing safer analogs, and exploring potential alternative treatments for African trypanosomiasis.'

Melarsoprol: Arsenical used in trypanosomiases. It may cause fatal encephalopathy and other undesirable side effects. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10311
CHEMBL ID166
CHEBI ID6729
SCHEMBL ID61707
MeSH IDM0013318

Synonyms (34)

Synonym
chebi:6729 ,
CHEMBL166
melarsoprolum
unii-zf3786q2e8
zf3786q2e8 ,
1,3,2-dithiarsolane-4-methanol, 2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-
2-(p-(4,6-diamino-s-triazin-2-ylamino)phenyl)-1,3,2-dithiarsolane-4-methanol
melarsoprol [inn:ban:dcf]
einecs 207-793-4
melarsoprolum [inn-latin]
rp 3854
2-[4-{(4,6-diamino-1,3,5-triazin-2-yl)amino}phenyl]-1,3,2-dithiarsolan-e-4-methanol
[2-[4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl]-1,3,2-dithiarsolan-4-yl]methanol
494-79-1
melarsoprol
C08001
D00832
melarsoprol (inn)
mel b (tn)
arsobal
specia
rp-3854
mel b
SCHEMBL61707
DB12864
(2-{4-[(4,6-diamino-1,3,5-triazin-2-yl)amino]phenyl}-1,3,2-dithiarsolan-4-yl)methanol
DTXSID90862033
Q419753
(2-(4-((4,6-diamino-1,3,5-triazin-2-yl)amino)phenyl)-1,3,2-dithiarsolan-4-yl)methanol
melarsoprol [mart.]
melarsoprol [mi]
melarsoprol [who-dd]
melarsoprol [inn]
AKOS040752991

Research Excerpts

Overview

Melarsoprol is an arsenic-containing drug, and has been applied in the treatment of human African trypanosomiasis at the late stage.

ExcerptReferenceRelevance
"Melarsoprol (MEL) is an arsenic-containing drug, and has been applied in the treatment of human African trypanosomiasis at the late stage."( Delivery of melarsoprol using folate-targeted PEGylated cyclodextrin-based nanoparticles for hepatocellular carcinoma.
Guo, J; Han, S; Li, Y; Li, YN; O'Driscoll, CM; Shi, X; Shi, Y; Sun, D; Wang, L; Yang, L; Zou, Y, 2023
)
2.01

Effects

ExcerptReferenceRelevance
"Melarsoprol has been used for many decades."( Cost-effectiveness analysis of alternative treatments of African gambiense trypanosomiasis in Uganda.
Carrín, G; Cattand, PD; Evans, D; Kuzoe, FA; Politi, C,
)
0.85

Treatment

Melarsoprol treatment was feared for its side effects. Treatment with melarsopol in two cases and eflornithine in one case led to complete recovery.

ExcerptReferenceRelevance
"Melarsoprol treatment was undertaken."( Polysomnography as a diagnosis and post-treatment follow-up tool in human African trypanosomiasis: a case study in an infant.
Bandzouzi, B; Bouteille, B; Buguet, A; Cespuglio, R; Mpandzou, G; Ngampo, S; Vincendeau, P, 2011
)
1.09
"Melarsoprol treatment was feared for its side effects."( Drug toxicity and cost as barriers to community participation in HAT control in the Democratic Republic of Congo.
Boelaert, M; Kande Betu Ku Mesu, V; Lefèvre, P; Lubanza, S; Lutumba, P; Robays, J; Van der Stuyft, P, 2007
)
1.06
"Treatment with melarsoprol in two cases and eflornithine in one case led to complete recovery."( [Sleeping sickness in children at Bobo-Dioulasso Hospital Center: apropos of 3 cases].
Bonkoungou, P; Millogo, A; Nacro, B; Sanou, M; Tall, F; Traoré, H; Traoré, S, 1999
)
0.64

Toxicity

ExcerptReferenceRelevance
"The authors consider evident similarities of toxic effects in the treatment of human african trypanosomiasis with Arsobal, and those in the treatment of syphilis with arsenobenzole derivatives."( [Adrenaline in the prevention and treatment of adverse effects of arsobal therapy. Apropos of 776 cases of human African trypanosomiasis caused by T. gambiense in the Health Service of Fontem (U.R. Cameroon)].
Cramet, B; Sina, GC; Suh Bandu, M; Triolo, N,
)
0.13
"2 and experienced significantly fewer cutaneous and neurological adverse effects than did patients who were treated with melarsoprol in 2001 and 2002 (n = 708)."( Eflornithine is safer than melarsoprol for the treatment of second-stage Trypanosoma brucei gambiense human African trypanosomiasis.
Bovier, PA; Chappuis, F; Meussen, A; Stietenroth, K; Udayraj, N, 2005
)
0.83
"Less toxic drugs, lowering financial barriers and improving confidentiality would have considerable impact on the participation in population screening for HAT."( Drug toxicity and cost as barriers to community participation in HAT control in the Democratic Republic of Congo.
Boelaert, M; Kande Betu Ku Mesu, V; Lefèvre, P; Lubanza, S; Lutumba, P; Robays, J; Van der Stuyft, P, 2007
)
0.34

Pharmacokinetics

A large number of patients refractory to melarsoprol treatment was recently reported from northern Uganda and northern Angola. We investigated in northern Angola whether interpatient pharmacokinetic differences influence the outcome of melarsOProl treatment. Mean terminal elimination half-life of melARSoprol was about 35 h.

ExcerptReferenceRelevance
" The 'terminal' elimination rate constant could be determined in six patients and subsequent kinetic calculations showed a three to fourfold variation in plasma clearance and 'terminal' half-life (median 1126 (range 553-2036) ml min-1 and 265 (107-446) h, respectively)."( Pharmacokinetics and adverse reactions after a single dose of pentamidine in patients with Trypanosoma gambiense sleeping sickness.
Bronner, U; Doua, F; Ericsson, O; Gustafsson, LL; Miézan, T; Rais, M; Rombo, L, 1995
)
0.29
" The results of this study are compared with recent pharmacokinetic data from human patients, and discussed in the context of the problem of relapses and reactive encephalopathy occurring after treatment of sleeping sickness."( Pharmacokinetics of melarsoprol in uninfected vervet monkeys.
Auma, JE; Brun, R; Burri, C; Burudi, EM; Onyango, JD, 1994
)
0.61
" Mean terminal elimination half-life of melarsoprol was about 35 h, volume of distribution was about 100 l and total clearance was about 50 ml/min."( Pharmacokinetic properties of the trypanocidal drug melarsoprol.
Baltz, T; Brun, R; Burri, C; Doua, F; Giroud, C; Welker, HA,
)
0.65
" As a large number of patients refractory to melarsoprol treatment was recently reported from northern Uganda and northern Angola, we investigated in northern Angola whether interpatient pharmacokinetic differences influence the outcome of melarsoprol treatment."( Pharmacokinetic investigations in patients from northern Angola refractory to melarsoprol treatment.
Burri, C; Keiser, J, 2001
)
0.8

Compound-Compound Interactions

megazol gel, when used in combination with melarsoprol (3.5%) is capable of curing experimental murine CNS-trypanosomiasis with a one-day treatment.

ExcerptReferenceRelevance
" Susceptibility patterns of sensitive and resistant parasites were evaluated against calcium antagonists of several chemical classes (verapamil, cyproheptidine, desipramine and chlopromazine), alone and in combination with suramin, diminazene aceturate or melarsen oxide cyteamine."( Trypanocidal resistance in Trypanosoma evansi in vitro: effects of verapamil, cyproheptidine, desipramine and chlorpromazine alone and in combination with trypanocides.
Anene, BM; Anika, SM; Chukwu, CC; Ross, CA, 1996
)
0.29
" This megazol gel, when used in combination with melarsoprol (3."( Topical chemotherapy for experimental African trypanosomiasis with cerebral involvement: the use of melarsoprol combined with the 5-nitroimidazole, megazol.
Chauvière, G; Jennings, FW; Murray, M; Viode, C, 1996
)
0.76
" When these gels are used in combination with melarsoprol gel they are capable of curing experimental murine CNS-trypanosomiasis with a one-day treatment."( Topical chemotherapy for experimental murine African CNS-trypanosomiasis: the successful use of the arsenical, melarsoprol, combined with the 5-nitroimidazoles, fexinidazole or MK-436.
Atouguia, JM; Jennings, FW; Murray, M, 1996
)
0.76

Bioavailability

melarsoprol-cyclodextrin complexes are developed to improve tolerability and the bioavailability of the drug. These complexes increase the oral bioavailability, making them effective orally and both curative and nontoxic in doses that are equivalent to those of intravenous melarso.

ExcerptReferenceRelevance
" The aim of our work was to develop melarsoprol-cyclodextrin complexes in order to improve the tolerability and the bioavailability of melarsoprol."( Melarsoprol-cyclodextrins inclusion complexes.
Astier, A; Fries, I; Gibaud, S; Mutzenhardt, P; Zirar, SB, 2005
)
2.05
" These complexes increase the oral bioavailability of melarsoprol making them effective orally and both curative and nontoxic in doses that are equivalent to those of intravenous melarsoprol."( An alternative form of melarsoprol in sleeping sickness.
Kennedy, PG, 2012
)
0.94
" The 7-nitroquinoxalin-2-one and 5-nitroindazole scaffold derivatives 58 and 35, respectively, are particularly interesting because of their established oral bioavailability in mice."( Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.
Arán, VJ; Dardonville, C; Kaiser, M, 2012
)
0.38
" Our compound optimization that has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly potent, orally bioavailable inhibitor of trypanosome replication."( Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
Behera, R; Edwards, P; Guyett, PJ; Karver, CE; Mensa-Wilmot, K; Patel, G; Pollastri, MP; Roncal, NE; Sullenberger, C, 2013
)
0.39

Dosage Studied

The higher frequency of relapses in 1994 to 1997 was associated with an incremental dosage regimen of melarsoprol. The introduction of the combination of nifurtimox and eflornithine (NECT) has accelerated the shift from melar's to the best treatment available.

ExcerptRelevanceReference
" Optimum dosage and duration of therapy, modes of administration and potential for large scale use are discussed."( Advances in sleeping sickness therapy.
Van Nieuwenhove, S, 1992
)
0.28
" A (donor) mouse, infected for 28 days, is dosed with a drug, or combination of drugs, and samples of blood, cerebral cortex, choroid plexus and lining of ventricle are injected into clean (recipient) mice."( Screening compounds for sleeping sickness therapy without relapse.
Ormerod, WE; Raseroka, BH, 1988
)
0.27
" Two other goats appeared to be cured with this dosage of suramin but later developed abnormal central nervous system (CNS) signs and parasitaemia."( Experimental infection of goats with Trypanosoma brucei ssp. and effects of treatment with suramin and Mel-B.
Chumo, DA; Muriithi, RM; Mwangi, J; Reardon, MJ; Towett, S; Wellde, BT, 1989
)
0.28
" The prolonged elimination of pentamidine seems inconsistent with the present recommended dosage regimen of pentamidine for treatment of trypanosomiasis of 7 to 10 parenteral doses given once daily or every second day."( Pharmacokinetics and adverse reactions after a single dose of pentamidine in patients with Trypanosoma gambiense sleeping sickness.
Bronner, U; Doua, F; Ericsson, O; Gustafsson, LL; Miézan, T; Rais, M; Rombo, L, 1995
)
0.29
" The remaining animal in this group, that displayed persistent antigenaemia, had been treated with a sub-curative drug dosage level."( Trypanosoma brucei rhodesiense: use of an antigen detection enzyme immunoassay for evaluation of response to chemotherapy in infected vervet monkeys (Cercopithecus aethiops).
Gichuki, CW; Nantulya, VM; Sayer, PD, 1994
)
0.29
" Dose-response experiments with melarsoprol (10(-7) to 10(-9) mol/L) were performed over 96 hours."( Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines.
Gabrilove, JL; Jakubowski, A; König, A; Pandolfi, PP; Rivi, R; Warrell, RP; Wrazel, L, 1997
)
0.89
" The higher frequency of relapses in 1994 to 1997 was associated with an incremental dosage regimen of melarsoprol."( Trypanosomiasis relapse after melarsoprol therapy, Democratic Republic of Congo, 1982-2001.
Mpia, B; Pépin, J, 2005
)
0.83
" injections separated by 1-week intervals, but with graded dosing (1."( Randomized controlled trial of three regimens of melarsoprol in the treatment of Trypanosoma brucei gambiense trypanosomiasis.
Mpia, B; Pépin, J, 2006
)
0.59
" rhodesiense in vivo, curing three of four infected mice dosed intraperitoneally at 5 mg/kg x 4 days."( Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
Bakunov, SA; Bakunova, SM; Barzcz, T; Brun, R; Chen, H; Jones, SK; Kumar, EV; Patrick, DA; Tidwell, RR; Wenzler, T; Werbovetz, KA, 2009
)
0.35
" A combination chemotherapy, eflornithine alongside nifurtimox, has been introduced to decrease the time frame and overall dosing of eflornithine and reducing the risk of drug resistance emerging."( Potential new drugs for human African trypanosomiasis: some progress at last.
Barrett, MP, 2010
)
0.36
" The introduction of the combination of nifurtimox and eflornithine (NECT) has accelerated the shift from melarsoprol to the best treatment available, due to reduced dosage and treatment time for eflornithine that has significantly lessened the cost and improved the burden of logistics encountered during treatment and distribution."( Update on field use of the available drugs for the chemotherapy of human African trypanosomiasis.
Diarra, A; Franco, J; Jannin, J; Postigo, JA; Simarro, PP, 2012
)
0.59
" 28DAP010 showed efficacy similar to that of DB829 in dose-response studies in mouse models of first- and second-stage African sleeping sickness."( In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness.
Boykin, DW; Braissant, O; Brun, R; Ismail, MA; Patrick, DA; Tidwell, RR; Wang, MZ; Wenzler, T; Yang, S, 2014
)
0.4
"We have shown that drug dose-response can be evaluated using bioluminescence imaging and confirmed quantification of tissue parasite load using qPCR."( A sensitive and reproducible in vivo imaging mouse model for evaluation of drugs against late-stage human African trypanosomiasis.
Bradley, B; Burrell-Saward, H; Croft, SL; Rodgers, J; Ward, TH, 2015
)
0.42
"Current treatments for Human African Trypanosomiasis (HAT) are limited in their application, have undesirable dosing regimens and unsatisfactory toxicities highlighting the need for the development of a safer drug pipeline."( Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
Arroo, RRJ; Bhambra, AS; Burrell-Saward, H; Edgar, M; Elsegood, MRJ; Krystof, V; Li, Y; Weaver, GW; Yardley, V, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
triazinesCompounds based on a triazine skeleton.
[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]

Bioassays (378)

Assay IDTitleYearJournalArticle
AID473009Inhibition of Plasmodium falciparum recombinant falcipain-2 using Cbz-Leu-Arg-AMC as substrate by standard fluorescence assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.
AID445251Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID562497Ratio of IC50 for Trypanosoma brucei brucei AT1KO to IC50 for Trypanosoma brucei brucei BS2212009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID432043Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID1653744Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID252603In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain; 2/42005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID441748Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream Trypanosoma brucei rhodesiense STIB 9002010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.
AID1298167Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense.
AID401637Antitrypanosomal activity against Trypanosoma brucei rhodesiense2005Journal of natural products, May, Volume: 68, Issue:5
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.
AID274293Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB9002006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.
AID690543Antiprotozoal activity against Trypanosoma brucei rhodesiense bloodstream forms2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
2-Alkynoic fatty acids inhibit topoisomerase IB from Leishmania donovani.
AID341603Antileishmanial activity against Leishmania donovani MHOM-ET-67/L82 amastigotes by axenic assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1143877Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay2014European journal of medicinal chemistry, Jun-23, Volume: 81Antiprotozoal activity and DNA binding of N-substituted N-phenylbenzamide and 1,3-diphenylurea bisguanidines.
AID595451Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by microplate reader assay2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Didemnidines A and B, indole spermidine alkaloids from the New Zealand ascidian Didemnum sp.
AID213470In vitro antitrypanosomal activity against Trypanosoma brucei rhodesiense2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.
AID1163239Metabolic stability in mouse liver microsomes assessed as compound remaining after 15 mins by UPLC analysis2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID756886Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID1614005Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by Alamar Blue dye-based fluorometric analysis2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
AID378569Antitrypanosomal activity against Trypanosoma brucei rhodesiense trypomastigotes2005Journal of natural products, Mar, Volume: 68, Issue:3
Ambigol C and 2,4-dichlorobenzoic acid, natural products produced by the terrestrial cyanobacterium Fischerella ambigua.
AID1193503Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream forms of Trypanosoma brucei rhodesiense STIB 9002015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Anti-trypanosomal cadinanes synthesized by transannular cyclization of the natural sesquiterpene lactone nobilin.
AID336752Antitrypanosomal activity against Trypanosoma brucei rhodesiense KETRI 243 isolate after 48 hrs2003Journal of natural products, Mar, Volume: 66, Issue:3
Trypanocidal diarylheptanoids from Aframomum letestuianum.
AID1480088Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 48 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID389449Cytotoxicity against rat L6 cells2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID1193547Selectivity index, ratio of CC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
AID341599Antiplasmodial activity against Plasmodium falciparum K12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
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
AID1336733Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 bloodstream forms2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity.
AID644365Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by alamar blue assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Synthesis and antimalarial and antituberculosis activities of a series of natural and unnatural 4-methoxy-6-styryl-pyran-2-ones, dihydro analogues and photo-dimers.
AID1156608Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 3 days by Alamar blue assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID372439Antitrypanosomal activity against tbat1 knockout Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID497468Trypanocidal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Antiprotozoal steroidal saponins from the marine sponge Pandaros acanthifolium.
AID1480086Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 16 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID1193502Cytotoxicity against rat L6 cells2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Anti-trypanosomal cadinanes synthesized by transannular cyclization of the natural sesquiterpene lactone nobilin.
AID1336732Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms isolated from patient after 70 hrs by microplate alamar blue assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity.
AID418754Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as survival and aparasitemic condition at 8 mg/kg, ip administered from day 3 to day 6 postinfection measured after 60 days postinfect2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID677563Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents.
AID303261Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 in blood2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Synthesis and evaluation of antiparasitic activities of new 4-[5-(4-phenoxyphenyl)-2H-pyrazol-3-yl]morpholine derivatives.
AID1776165Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 assessed as inhibition of parasite growth incubated for 72 hrs by Alamar blue dye-based fluorometric analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Spirombandakamine A
AID248819Inhibitory concentration in vitro against blood stream Trypanosoma brucei rhodesiense incubated for 72 hr at 37 degree C2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID404599Selectivity index, Ratio of IC50 for L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 92008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.
AID756887Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as reduction of parasitemia relapse at 5 mg/kg, ip qd for 4 days2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID333758Antitrypanosomal activity against Trypanosoma brucei rhodesiense2004Journal of natural products, Dec, Volume: 67, Issue:12
Ancistrobenomine a, the first naphthylisoquinoline oxygenated at Me-3, and related 5,1'-coupled alkaloids, from the "new" plant species ancistrocladusbenomensis.
AID765725Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar blue assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID1578098Antitrypanosomal activity against Trypanosoma brucei rhodesiense2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1480084Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 2 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID1713354Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes by alamar blue staining-based fluorometric analysis2016European journal of medicinal chemistry, Nov-10, Volume: 123Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.
AID475980Cytotoxicity against rat L6 cells2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
AID1501229Antiprotozoal activity against blood stream form of Trypanosoma brucei rhodesiense STIB900 after 72 hrs by alamar blue assay2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antiprotozoal Linear Furanosesterterpenoids from the Marine Sponge Ircinia oros.
AID389450Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream trypomastigotes2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID748437Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes after 72 hrs by Alamar blue assay2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.
AID274295Antiprotozoal activity against chloroquine-, pyrimethamine-resistant Plasmodium falciparum K12006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.
AID1196797Antitrypanosomal activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar Blue assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID433913Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue based microplate assay2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis of a series of N6-substituted adenosines with activity against trypanosomatid parasites.
AID419759Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as parasite free mouse survival at 2 mg/kg, ip administered for 4 consecutive days from day 3 to 6 postinfection measured up to 60 days2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID1156609Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID1163232Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID21446550% antitrypanosomal activity against Trypanosoma rhodesiense2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp.
AID635852Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by resazurin-based spectrophotometric assay2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents.
AID215328Evaluated in vitro for antitrypanosomal activity against Trypanosoma brucei2002Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.
AID264014Cytotoxicity against J774.1 cell line after 48 hrs2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
AID1483953Antiprotozoal activity against patient derived Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 72 hrs by Alamar Blue assay2017Journal of natural products, 02-24, Volume: 80, Issue:2
Dioncophyllines C
AID253516In vitro inhibitory concentration against blood stream Trypanosoma brucei brucei AT1 wild type incubated for 72 h at 37 degree C2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID235941In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as cured/infected; 4/42005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1578097Antitrypanosomal activity against Leishmania donovani2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID341606Antimicrobial activity against Babesia divergens 1903B2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1578095Antitrypanosomal activity against Trypanosoma cruzi after 48 hrs by [3H]-hypoxanthine incorporation assay2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID286669Antitrypanosomal activity against Trypanosoma brucei rhodesiense2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.
AID597077Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 72 hrs by microplate fluorimetry2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Antiparasitic compounds from Cupania cinerea with activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense.
AID1306906Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 900 bloodstream forms2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead.
AID322077Cytotoxicity against human HL60 cells2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
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]
AID303244Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations.
AID1062627Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID1612294Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 72 hrs by Alamar blue staining-based fluorometric analysis2018Journal of natural products, 10-26, Volume: 81, Issue:10
Methionine-Containing Rhabdopeptide/Xenortide-like Peptides from Heterologous Expression of the Biosynthetic Gene Cluster kj12ABC in Escherichia coli.
AID341602Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C42007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID419754Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream Trypanosoma brucei rhodesiense STIB9002009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID562491Antitrypanosomal activity against Trypanosoma brucei brucei AT1KO by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID300098Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID274299Survival of NMRI mouse infected with Trypanosoma brucei brucei at 0.5 mg/kg, ip2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.
AID432059Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected NMRI mouse assessed mean survival time at 4 mg/kg, ip dosed for 4 days2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID1068803Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition after 70 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Activity of diimidazoline amides against African trypanosomiasis.
AID322076Antimicrobial activity against Trypanosoma brucei brucei clone 427-221a after 48 hrs2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
AID1240950Toxicity in late-stage human african trypanosomiasis patient assessed as mortality rate following 10-day schedule2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.
AID562487Antitrypanosomal activity against Trypanosoma brucei gambiense K03048 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID596419Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes).
AID1062626Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID1410115Antiplasmodial activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote after 72 hrs by Alamar blue assay2018Journal of natural products, 04-27, Volume: 81, Issue:4
Mbandakamine-Type Naphthylisoquinoline Dimers and Related Alkaloids from the Central African Liana Ancistrocladus ealaensis with Antiparasitic and Antileukemic Activities.
AID1126157Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB9002014Journal of natural products, Apr-25, Volume: 77, Issue:4
Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4.
AID1163241Metabolic stability in mouse plasma assessed as compound remaining after 1 hr2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID582593Antitrypanosomal activity against Trypanosoma brucei rhodesiense ST1B900 trypomastigote infected in NMR1 mouse assessed as inhibition of parasitemia at 50 mg/kg, ip administered on day 3 post infection for 4 days2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.
AID1068802Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
Activity of diimidazoline amides against African trypanosomiasis.
AID1254914Antitrypanosomal activity against bloodstream trypomastigote forms of Trypanosoma brucei rhodesiense STIB 900 assessed as inhibition of growth2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID765718Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID616288Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes stage forms incubated for 72 hrs by Alamar blue staining based fluorometric assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Antimalarial β-carbolines from the New Zealand ascidian Pseudodistoma opacum.
AID251291In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain, measured as survival days (control 7 days)2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID404598Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.
AID1779353Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 incubated for 70 hrs by resazurin dye-based fluorometric analysis2021European journal of medicinal chemistry, Oct-05, Volume: 221Synthesis, in vitro antiprotozoal activity, molecular docking and molecular dynamics studies of some new monocationic guanidinobenzimidazoles.
AID372430Antileishmanial activity against Leishmania donovani MHOMET-67/L82 amastigotes infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID1177050Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID562486Antitrypanosomal activity against melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID400721Cytotoxicity against human HT-29 cells1998Journal of natural products, May, Volume: 61, Issue:5
Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers.
AID671047Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by Alamar blue growth inhibition assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Discovery of nitroheterocycles active against African trypanosomes. In vitro screening and preliminary SAR studies.
AID692982Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
AID264012Inhibition of Trypanosoma brucei rhodesiense rhodesain at 200 uM2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
AID482888Inhibition of human liver cathepsin B at 100 uM2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID1500573Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by Alamar Blue assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID311643Antiparasitic activity against Trypanosoma brucei rhodesiense by Alamar blue assay2007Journal of natural products, Oct, Volume: 70, Issue:10
Antiprotozoal polyacetylenes from the Tanzanian medicinal plant Cussonia zimmermannii.
AID482887Antitrypanosomal activity against Trypanosoma brucei brucei2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID341604Antimicrobial activity against Giardia duodenalis WB2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1313991Antiparasitic activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 assessed as growth inhibition after 72 hrs by resazurin assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense.
AID562495Ratio of IC50 for Trypanosoma brucei gambiense ITMAP141267 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9032009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1062624Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as decrease in parasitemia at 5 mg/kg, ip qd administered for 4 days measured once per week until 60 days by microscopic analysis2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID432044Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID378568Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes2005Journal of natural products, Mar, Volume: 68, Issue:3
Ambigol C and 2,4-dichlorobenzoic acid, natural products produced by the terrestrial cyanobacterium Fischerella ambigua.
AID482885Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain at 100 uM2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID439872Antimicrobial activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote forms2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
AID774788Antiprotozoal activity against Trypanosoma brucei rhodesiense assessed as parasite growth inhibition2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives.
AID562498Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for Trypanosoma brucei gambiense STIB9302009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1546292Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 amastigotes assessed as growth inhibition after 72 hrs by Alamar Blue dye-based fluorometric analysis2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
A new chemotype with promise against Trypanosoma cruzi.
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]
AID1743672Trypanocidal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes incubated for 72 hrs by Alamar blue assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Palladium-catalysed synthesis of arylnaphthoquinones as antiprotozoal and antimycobacterial agents.
AID404375Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.
AID723217Trypanocidal activity against Trypanosoma brucei rhodesiense Z310 after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro.
AID322078Selectivity index, ratio of EC50 for HL60 cells to EC50 for Trypanosoma brucei brucei clone 427-221a2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
AID644196Antitrypanosomal activity against blood stream form of Trypanosoma brucei after 69 hrs by resazurin-based fluorescence assay2012Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
Quinol derivatives as potential trypanocidal agents.
AID384321Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB9002008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity.
AID710596Antitrypanosomal activity against trypomastigote form of Trypanosoma brucei rhodesiense STIB 900 assessed as growth inhibition after 72 hrs by microplate fluorometry2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
AID1271906Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue assay2016European journal of medicinal chemistry, Jan-27, Volume: 108Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.
AID1240903Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream forms of Trypanosoma brucei rhodesiense STIB 9002015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.
AID692981Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms assessed as reduction in cell viability after 70 hrs by alamar blue assay2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
1-Aryl-4-nitro-1H-imidazoles, a new promising series for the treatment of human African trypanosomiasis.
AID509507Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 at 4.8 ug/mL by microplate alamar blue assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and preliminary bioactivity assays of 3,4-dichloro-5-(omega-hydroxyalkylamino)-2(5H)-furanones.
AID235934In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as survival days (control 7 days); ND is not determined2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID418759Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 8 mg/kg, ip administered from day 3 to day 6 postinfection2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID473011Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain by standard fluorescence assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.
AID400720Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 9001998Journal of natural products, May, Volume: 61, Issue:5
Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers.
AID1359978Antitrypanosomal activity against Trypanosoma brucei gambiense GUTat 3.1 after 72 hrs by Alamar Blue assay2018European journal of medicinal chemistry, Jun-25, Volume: 154Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent.
AID231796Ratio of cytotoxicity against L6 cells to that of antitrypanosomal activity against Trypanosoma brucei rhodesiense2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.
AID351792Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
AID260370Antiprotozoal activity against Trypanosoma brucei brucei GVR352006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines.
AID341607Antimicrobial activity against Babesia divergens 42012007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID247964Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1306903Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by Alamar blue assay2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead.
AID432049Cytotoxicity against rat L6 cells2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID351791Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by alamar blue assay2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
AID445257Toxicity in NMRI mouse infected with Trypanosoma brucei rhodesiense STIB900 assessed as survival at 8 mg/kg, ip after administered for 4 consecutive days from day 3 postinfection measured after 7 to 30 days2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID1728297Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002021European journal of medicinal chemistry, Jan-15, Volume: 210Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities.
AID634012Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 72 hrs by serial dilution Alamar blue assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds.
AID418755Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as survival and aparasitemic condition at 2 mg/kg, ip administered from day 3 to day 6 postinfection measured after 60 days postinfect2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID666698Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
AID1298168Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense.
AID1405620Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigote after 72 hrs by Alamar Blue assay2018European journal of medicinal chemistry, Aug-05, Volume: 156Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents.
AID1177591Antiparasitic activity against Trypanosoma brucei rhodesiense STIB9002014Journal of natural products, Aug-22, Volume: 77, Issue:8
Xenortide Biosynthesis by Entomopathogenic Xenorhabdus nematophila.
AID260369Antiprotozoal activity against Leishmania donovani MHOM/ET/L82/LV92006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID765716Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 2 mg/kg, ip administered for 4 days2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID562484Antitrypanosomal activity against wild-type Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID418748Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 70 hrs by alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID335551Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by alamar blue assay2002Journal of natural products, Aug, Volume: 65, Issue:8
Ancistrocongolines A-D, new naphthylisoquinoline alkaloids from ancistrocladus congolensis.
AID475977Inhibition of Trypanosoma brucei brucei recombinant cathepsin B assessed after 5 mins by spectrofluorimetry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
AID106021Tested for cytotoxicity towards human MRC-5 cells2002Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.
AID562489Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID473010Inhibition of Plasmodium falciparum recombinant falcipain-3 by standard fluorescence assay2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.
AID336751Antitrypanosomal activity against Trypanosoma brucei brucei Lab110 EATRO after 48 hrs2003Journal of natural products, Mar, Volume: 66, Issue:3
Trypanocidal diarylheptanoids from Aframomum letestuianum.
AID475975Antitrypanosomal activity against Trypanosoma brucei brucei 427-221a after 40 hrs by bioluminescence assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
AID1348371Cytotoxicity against human MRC5 SV2 cells assessed as decrease in cell viability after 72 hrs by resazurin dye-based fluorometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID341601Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID720847Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 70 hrs by resazurin reduction assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Aminoalkyl derivatives of guanidine diaromatic minor groove binders with antiprotozoal activity.
AID1541166Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes assessed as growth inhibition after 72 hrs by Alamar Blue dye-based fluorometric analysis
AID764882Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom.
AID264016Selectivity index, IC50 for J774.1/IC50 for Trypanosoma brucei brucei2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
AID765710Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as cured animal at 2 mg/kg, ip administered for 4 days2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID552695Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation.
AID316592Antiplasmodial activity against Plasmodium falciparum K1 in [3H]hypoxanthine incorporation assay2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity.
AID1163238Metabolic stability in human liver microsomes assessed as compound remaining after 15 mins by UPLC analysis2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1462698Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote bloodstream form assessed as growth inhibition at 0.8 ug/ml after 72 hrs by resazurin dye-based fluorometric analysis relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Lead selection of antiparasitic compounds from a focused library of benzenesulfonyl derivatives of heterocycles.
AID441747Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.
AID562488Antitrypanosomal activity against Trypanosoma brucei gambiense ITMAP141267 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID728609Antitrypanosomal activity against bloodstream forms of wild type Trypanosoma brucei rhodesiense STIB900 after 70 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).
AID453254Antitrypanosomal activity against Trypanosoma brucei rhodesiense2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.
AID303243Cytotoxicity against rat L6 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations.
AID243451In vitro inhibitory concentration against P2 aminopurine transporter of Trypanosoma brucei brucei 427 adenosine (0.5 uM) uptake in presence of 1 mM inosine2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID300097Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by microplate assay2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals.
AID725218Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by Alamar blue assay2013Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds.
AID562493Ratio of IC50 for melasoprol-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9012009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID621153Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 at pH 7.4 by microplate assay2011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives.
AID756883Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as host mean survival days at 5 mg/kg, ip qd for 4 days2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID215678Minimum concentration producing complete lysis of all trypanosomes within 30 min at 37 degrees C in vitro1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Potential antitrypanosomal agents. 1,N2-Disubstituted 2-amino-5-hydroxy-4-methylnaphtho[1,2-d]thiazolium salts and related compounds.
AID1432876Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and activity of nucleoside-based antiprotozoan compounds.
AID1163240Metabolic stability in human plasma assessed as compound remaining after 1 hr2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID677571Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in presence of tetracycline after 3 days2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents.
AID372438Antitrypanosomal activity against wild type Trypanosoma cruzi BS221 infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID727321Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms incubated for 70 hrs by Alamar blue assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Synthesis and in vitro antimalarial testing of neocryptolepines: SAR study for improved activity by introduction and modifications of side chains at C2 and C11 on indolo[2,3-b]quinolines.
AID373520Antiparasitic activity against Trypanosoma brucei rhodesiense STIB9002009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis and antiparasitic and antifungal evaluation of 2'-arylsubstituted-1H,1'H-[2,5']bisbenzimidazolyl-5-carboxamidines.
AID252610In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as cured/infected; 0/42005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1163231Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1163237Stability of the compound in PBS buffer assessed as recovery at pH 7.4 measured after 24 hrs by UPLC analysis2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID562490Antitrypanosomal activity against Trypanosoma brucei brucei BS221 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID1480085Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 6 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID456259Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in rat L6 cells2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Synthesis, stereoelectronic characterization and antiparasitic activity of new 1-benzenesulfonyl-2-methyl-1,2,3,4-tetrahydroquinolines.
AID1586758Antiprotozoal activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay2018Journal of natural products, 12-28, Volume: 81, Issue:12
Antiprotozoal Isoprenoids from Salvia hydrangea.
AID1617101Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes incubated for 72 hrs by Alamar blue staining-based fluorometric analysis2019Journal of natural products, 11-22, Volume: 82, Issue:11
Ealamines A-H, a Series of Naphthylisoquinolines with the Rare 7,8'-Coupling Site, from the Congolese Liana
AID1727700Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition measured after 70 hrs by Alamar blue assay2021European journal of medicinal chemistry, Jan-01, Volume: 209The discovery of novel antitrypanosomal 4-phenyl-6-(pyridin-3-yl)pyrimidines.
AID1193543Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
AID1653740Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth inhibition measured after 70 hrs by Alamar blue assay2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID562485Antitrypanosomal activity against pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID664487Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Synthesis, biological evaluation, and structure-activity relationships of N-benzoyl-2-hydroxybenzamides as agents active against P. falciparum (K1 strain), Trypanosomes, and Leishmania.
AID1165097Ratio of IC50 for bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase in absence of tetracycline to IC50 for bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I n2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
AID372440Resistance factor, ratio of IC50 for tbat1 knock out Trypanosoma cruzi BS221 to IC50 for wild type Trypanosoma cruzi BS2212007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID562494Ratio of IC50 for Trypanosoma brucei gambiense K03048 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9022009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID764881Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream form of Trypanosoma brucei rhodesiense STIB 9002013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID124568The compound was tested for in vivo activity against a rodent model of Trypanosoma brucei at the specified dose: 5 mg/kg, ip no. of days dosing = 1; All servived1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.
AID626317Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay2011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis).
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID453258Toxicity against rat L6 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.
AID274294Selectivity index, IC50 for L6 cells/ IC50 for Trypanosoma brucei rhodesience2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.
AID21365150% antitrypanosomal activity against Trypanosoma cruzi2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp.
AID552697Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation.
AID779145Antimicrobial activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by Alamar blue assay2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Novel 3-nitro-1H-1,2,4-triazole-based piperazines and 2-amino-1,3-benzothiazoles as antichagasic agents.
AID1462699Antiparasitic activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigote bloodstream form assessed as growth inhibition at 4.8 ug/ml after 72 hrs by resazurin dye-based fluorometric analysis relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Lead selection of antiparasitic compounds from a focused library of benzenesulfonyl derivatives of heterocycles.
AID418760Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 2 mg/kg, ip administered from day 3 to day 6 postinfection2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID401527Antitrypanosomal activity against Trypanosoma brucei rhodesiense2004Journal of natural products, May, Volume: 67, Issue:5
Ancistrotanzanine C and related 5,1'- and 7,3'-coupled naphthylisoquinoline alkaloids from Ancistrocladus tanzaniensis.
AID626322Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream form of Trypanosoma brucei rhodesiense STIB 9002011Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
Biological evaluation of glycosyl-isoindigo derivatives against the pathogenic agents of tropical diseases (malaria, Chagas disease, leishmaniasis and human African trypanosomiasis).
AID728605Antitrypanosomal activity against Trypanosoma brucei gambiense DAL 898R after 70 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).
AID1504891Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by alamar blue staining based fluorescence assay2018Journal of natural products, 01-26, Volume: 81, Issue:1
Antiprotozoal Sesquiterpene Lactones and Other Constituents from Tarchonanthus camphoratus and Schkuhria pinnata.
AID1298166Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 measured after 70 hrs by alamar blue staining based fluorescence analysis2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense.
AID389457Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 2 mg/kg, ip daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID1846640Antiprotozoal activity against patient-derived Trypanosoma brucei rhodesiense STIB assessed as parasite growth inhibition incubated for 70 hrs by resazurin dye based fluorometry2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Synthesis and Biological Evaluation of Natural-Product-Inspired, Aminoalkyl-Substituted 1-Benzopyrans as Novel Antiplasmodial Agents.
AID336753Antitrypanosomal activity against Trypanosoma brucei rhodesiense KETRI 243 As 10-3 isolate after 48 hrs2003Journal of natural products, Mar, Volume: 66, Issue:3
Trypanocidal diarylheptanoids from Aframomum letestuianum.
AID1165096Trypanocidal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase assessed as inhibition of proliferation after 3 days by resazurin assay in presence of tetracycline2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
AID1679082Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 incubated for 70 hrs by Alamar blue dye-based fluorometric analysis2020RSC medicinal chemistry, Dec-17, Volume: 11, Issue:12
Investigation of thiazolyl-benzothiophenamides as potential agents for African sleeping sickness.
AID1163230Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1480087Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 24 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID1176975Antiplasmodial activity against Trypanosoma brucei rhodesiense assessed as growth inhibition2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites.
AID445252Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID1355403Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 70 hrs by Alamar blue assay2018Journal of natural products, 06-22, Volume: 81, Issue:6
Phytochemical Study of Salvia leriifolia Roots: Rearranged Abietane Diterpenoids with Antiprotozoal Activity.
AID384322Cytotoxicity against rat L6 cells2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity.
AID473012Antiplasmodial activity against Plasmodium falciparum W2 by flow cytometry2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1193501Antiprotozoal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by Alamar blue assay2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Anti-trypanosomal cadinanes synthesized by transannular cyclization of the natural sesquiterpene lactone nobilin.
AID482886Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID764884Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by microplate fluorometry2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom.
AID634014Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds.
AID578277Antitrypanosomal activity against TbAT1 and HAPT1-deficient Trypanosoma brucei brucei B48 after 48 hrs by alamar blue assay2011Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5
Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity.
AID322079Selectivity index, ratio of MIC for HL60 cells to MIC for Trypanosoma brucei brucei clone 427-221a2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
AID558400Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID401652Antitrypanosomal activity against Trypanosoma brucei rhodesiense2005Journal of natural products, May, Volume: 68, Issue:5
ent-Dioncophylleine A and related dehydrogenated naphthylisoquinoline alkaloids, the first Asian dioncophyllaceae-type alkaloids, from the "new"plant species Ancistrocladus benomensis.
AID1653746Selectivity index, ratio of IC50 for rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis to IC50 for bloodstream Trypanosoma brucei rhodesiense STIB900 assessed as parasite growth in2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID736793Antitrypanosomal activity against Trypanosoma brucei TC211 after 24 hrs by alamar blue assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID1348367Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB-900 after 72 hrs by resazurin dye-based fluorometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID432054Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected NMRI mouse assessed as infection cure rate at 4 mg/kg, ip dosed for 4 days2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.
AID389464Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 1 mg/kg, ip administered daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID416485Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by microplate assay2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates.
AID315105Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes by microplate assay2008Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity.
AID1614010Selectivity index, ratio of CC50 for rat L6 cels to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
AID248973In vitro inhibitory concentration against intracellular amastigotes of Trypanosoma cruzi in rat skeletal myoblasts incubated for 37 degree C for 4 days2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID736304Antiparasitic activity against Trypanosoma brucei assessed as growth inhibition2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Examination of the mode of action of the almiramide family of natural products against the kinetoplastid parasite Trypanosoma brucei.
AID710591Selectivity index, ratio of IC50 for rat L6 cells to IC50 for trypomastigote form of Trypanosoma brucei rhodesiense strain STIB 9002012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1165095Trypanocidal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase assessed as inhibition of proliferation after 3 days by resazurin assay in absence of tetracycline2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
AID389451Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB 9002008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID464872Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 bloodstream form2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.
AID303262Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 in procyclic stage2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Synthesis and evaluation of antiparasitic activities of new 4-[5-(4-phenoxyphenyl)-2H-pyrazol-3-yl]morpholine derivatives.
AID637699Trypanocidal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream forms after 72 hrs by resazurin assay2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles.
AID253519In vitro inhibitory concentration against blood stream Trypanosoma brucei brucei AT1 knockout mutant with a non functional P2 transporter incubated for 72 h at 37 degree C2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID445268Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean parasitemia relaps day at 1 mg/kg, ip2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID1163235Solubility of the compound in 10 mM PBS buffer solution at pH7.4 at 3.125 to 200 uM after 2 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID106020In Vitro cytotoxicity on MRC-5 cells2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker.
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID677575Selectivity ratio of IC50 for Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in presence of tetracycline to IC50 for Trypanosoma brucei brucei overexpressing tet-inducible NTR in absence of tetracyclin2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents.
AID756894Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID677572Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing tet-inducible NTR in absence of tetracycline after 3 days2012Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
Novel 3-nitro-1H-1,2,4-triazole-based amides and sulfonamides as potential antitrypanosomal agents.
AID419752Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID300101Cytotoxicity against rat L6 cells after 72 hrs by microplate assay2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID525502Antiparasitic activity against Trypanosoma brucei BSF overexpressing NTR gene after 3 days by Alamar blue assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Exploiting the drug-activating properties of a novel trypanosomal nitroreductase.
AID1165094Trypanocidal activity against wild type bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a assessed as inhibition of proliferation after 3 days by resazurin assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
AID1359979Toxicity in ip dosed mouse measured over 72 hrs2018European journal of medicinal chemistry, Jun-25, Volume: 154Synthesis of proline derived benzenesulfonamides: A potent anti-Trypanosoma brucei gambiense agent.
AID482884Inhibition of Trypanosoma brucei rhodesiense rhodesain after 12 hrs by fluorescence spectroscopy-based on-bead assay2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID303247Selectivity index, ratio for IC50 of rat L6 cells to IC50 of Trypanosoma brucei rhodesiense STIB9002007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID475983Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
AID1143878Selectivity index, ratio of CC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense2014European journal of medicinal chemistry, Jun-23, Volume: 81Antiprotozoal activity and DNA binding of N-substituted N-phenylbenzamide and 1,3-diphenylurea bisguanidines.
AID356389Antitrypanosomal activity against Trypanosoma brucei rhodesiense2003Journal of natural products, Sep, Volume: 66, Issue:9
Ancistrotanzanine A, the first 5,3'-coupled naphthylisoquinoline alkaloid, and two further, 5,8'-linked related compounds from the newly described species Ancistrocladus tanzaniensis.
AID1348066Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 70 hrs by Alamar blue staining-based fluorometric analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis of new 1-benzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities.
AID215356In Vitro inhibition concentration against Trypomastigote form of Trypanosoma brucei2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker.
AID1503756Antitrypanosomal activity against Trypanosoma brucei rhodesiense bloodstream forms after 72 hrs by alamar blue staining based fluorescence assay2017Journal of natural products, 10-27, Volume: 80, Issue:10
Jozilebomines A and B, Naphthylisoquinoline Dimers from the Congolese Liana Ancistrocladus ileboensis, with Antiausterity Activities against the PANC-1 Human Pancreatic Cancer Cell Line.
AID1614009Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
AID1541616Antitrypanosomal activity against Trypanosoma brucei rhodesiense STI B900 measured after 72 hrs by alamar blue dye based fluorimetry analysis2019Journal of natural products, 12-27, Volume: 82, Issue:12
Structure, Biosynthesis, and Bioactivity of Photoditritide from
AID1240908Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.
AID389459Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 1 mg/kg, ip daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID1240902Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by alamar blue assay2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.
AID389462Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 8 mg/kg, ip administered daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID341600Antiplasmodial activity against Plasmodium falciparum NF542007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID264013Trypanocidal activity against Trypanosoma brucei brucei after 48 hrs2006Bioorganic & medicinal chemistry letters, May-15, Volume: 16, Issue:10
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
AID1348366Antitrypanosomal activity against suramin-sensitive Trypanosoma brucei brucei Squib 427 after 72 hrs by resazurin dye-based fluorometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1062629Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 assessed as growth inhibition after 70 hrs by Alamar blue assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID389456Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as cured mouse at 8 mg/kg, ip daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID646379Antitrypanosomal activity against Trypanosoma brucei brucei GVR35 infected in NMRI mouse assessed as increase in survival time at 20 mg/kg, ip qd for 5 days measured after 180 days2012Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
AID562496Ratio of IC50 for Trypanosoma brucei gambiense STIB930 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9042009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID419680Antitrypanosomal activity against Trypanosoma brucei rhodesiense bloodstream trypomastigotes2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase.
AID536810Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB9002010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
QSAR guided synthesis of simplified antiplasmodial analogs of naphthylisoquinoline alkaloids.
AID341605Antimicrobial activity against Giardia duodenalis G12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1432875Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei rhodesiense STIB900 trypomastigotes after 72 hrs by alamar blue assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and activity of nucleoside-based antiprotozoan compounds.
AID1062617Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as mean survival days at 5 mg/kg, ip qd administered for 4 days2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.
AID562492Ratio of IC50 for pentamidine-resistant Trypanosoma brucei rhodesiense STIB900 to IC50 for wild-type Trypanosoma brucei rhodesiense STIB9002009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.
AID419753Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 after 70 hrs by alamar blue assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID728606Antitrypanosomal activity against Trypanosoma brucei gambiense STIB930 after 70 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).
AID1578096Antitrypanosomal activity against Leishmania donovani after 48 hrs by [3H]-hypoxanthine incorporation assay2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID251297In vivo antitrypanosomal activity at a dose of 4*1 mg/kg, i.p., in mice infected with Trypanosoma brucei rhodesiense STIB 900 strain, measured as survival days (control 7 days); ND is not determined2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID418761Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes infected in NMRI mouse assessed as mouse survival at 1 mg/kg, ip administered from day 3 to day 6 postinfection2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID235940In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain; Not determined2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1163236Octanol-phosphate buffer partition coefficient, log D of the compound at pH 7.4 after 2 hrs of shaking after 2 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID445258Toxicity in NMRI mouse infected with Trypanosoma brucei rhodesiense STIB900 assessed as survival at 2 mg/kg, ip after administered for 4 consecutive days from day 3 postinfection measured after 7 to 30 days2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID756895Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID710592Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
AID621158Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives.
AID404597Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 after 72 hrs by microplate alamar blue assay2008Bioorganic & medicinal chemistry, Jun-15, Volume: 16, Issue:12
Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.
AID260371Antiprotozoal activity against Trichomonas vaginalis CMP2006Bioorganic & medicinal chemistry letters, Feb-15, Volume: 16, Issue:4
Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines.
AID728604Antitrypanosomal activity against Trypanosoma brucei gambiense KO48 after 70 hrs by Alamar Blue assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).
AID1480082Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
AID274745Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB9002007Journal of natural products, Jan, Volume: 70, Issue:1
Limonoid orthoacetates and antiprotozoal compounds from the roots of Pseudocedrela kotschyi.
AID482889Inhibition of human liver cathepsin B2009Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
AID1578093Antitrypanosomal activity against Trypanosoma cruzi2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID362548Antiprotozoal activity against Trypanosoma brucei rhodesiense STIB9002008Journal of natural products, Sep, Volume: 71, Issue:9
Antiprotozoal activities of heterocyclic-substituted xanthones from the marine-derived fungus Chaetomium sp.
AID235933In vivo antitrypanosomal activity at a dose of 4*8 mg/kg, i.p., in mice infected with Trypanosoma brucei brucei STIB 795 strain, measured as survival days (control 7 days)2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID632296Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Novel 3-nitro-1H-1,2,4-triazole-based aliphatic and aromatic amines as anti-chagasic agents.
AID728616Antitrypanosomal activity against Trypanosoma brucei brucei 221 after 48 hrs by Cell Titre Glo assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Optimization of chloronitrobenzamides (CNBs) as therapeutic leads for human African trypanosomiasis (HAT).
AID1181596Antimicrobial activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei.
AID578276Antitrypanosomal activity against TbAT1-deficient Trypanosoma brucei brucei after 48 hrs by alamar blue assay2011Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5
Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity.
AID377196Antitrypanosomal activity against Trypanosoma rhodesiense2000Journal of natural products, Aug, Volume: 63, Issue:8
Pelorol from the tropical marine sponge Dactylospongia elegans.
AID372431Trypanocidal activity against Trypanosoma brucei rhodesiense STIB 900 infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID1306904Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay2016Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
Antiprotozoal activity of bicycles featuring a dimethylamino group at their bridgehead.
AID767873Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 by Alamar Blue assay2013Journal of natural products, Sep-27, Volume: 76, Issue:9
Antitrypanosomal triterpenoid with an ε-lactone E-ring from Salvia urmiensis.
AID1728298Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities.
AID351794Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense2009Bioorganic & medicinal chemistry, May-15, Volume: 17, Issue:10
Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
AID418747Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID765724Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB9002013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.
AID1156603Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID419764Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival rate at 1 mg/kg, ip administered 4 consecutive days from day 3 to 6 postinfection2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID483199Antitrypanosomal activity against Trypanosoma brucei brucei 427 bloodstream form after 72 hrs by LILIT method2010Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.
AID759435Resistant factor, ratio of IC50 for bloodstream form of Trypanosoma brucei brucei expressing TbMRPA protein to IC50 for bloodstream form of wild type Trypanosoma brucei 2472013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
N-Benzyloxycarbonyl-S-(2,4-dinitrophenyl)glutathione dibutyl diester is inhibitory to melarsoprol resistant cell lines overexpressing the T. bruceiMRPA transporter.
AID419763Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB900 infected in NMRI mouse assessed as survival rate at 2 mg/kg, ip administered 4 consecutive days from day 3 to 6 postinfection2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.
AID248971Inhibitory concentration in vitro against intracellular amastigotes of Leishmania donovani in rat skeletal myoblasts incubated for 96 hr at 27 degree C2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1455940Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar Blue assay
AID309300Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by Alamar blue assay2007Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli.
AID552696Antitrypanosomal activity against bloodstream form of Trypanosoma brucei s427 after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1
Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation.
AID739090Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei Lister 427 after 48 hrs by hemocytometer2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
AID762348Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 bloodstream form after 70 hrs by Alamar blue assay2013European journal of medicinal chemistry, Aug, Volume: 663-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.
AID1728296Trypanocidal activity against Trypanosoma brucei rhodesiense STIB900 incubated for 70 hrs by Alamar blue assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Preparation of new 1,3-dibenzyl tetrahydropyridinylidene ammonium salts and their antimicrobial and anticellular activities.
AID389463Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB 900 infected acute mouse model assessed as survival time at 2 mg/kg, ip administered daily for 4 days2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.
AID445250Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.
AID1300851Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 trypomastigotes assessed as inhibition of parasite growth after 72 hrs by Alamar blue assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.
AID1169287Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigote forms2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Antitrypanosomal quinoline alkaloids from the roots of Waltheria indica.
AID378201Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 by Alamar blue assay2000Journal of natural products, Nov, Volume: 63, Issue:11
Ancistroealaines A and B, two new bioactive naphthylisoquinolines, and related naphthoic acids from Ancistrocladus ealaensis.
AID400722Selectivity index, ratio of IC50 for human HT29 cells to IC50 for Trypanosoma brucei rhodesiense STIB 9001998Journal of natural products, May, Volume: 61, Issue:5
Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers.
AID527276Trypanocidal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 after 72 hrs2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
2-Hexadecynoic acid inhibits plasmodial FAS-II enzymes and arrests erythrocytic and liver stage Plasmodium infections.
AID661007Antitrypanosomal activity against Trypanosoma brucei brucei TC221 infected in mouse J774.1 cells after 48 hrs by alamar blue assay2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis and structure-activity relationships of new quinolone-type molecules against Trypanosoma brucei.
AID372429Trypanocidal activity against Trypanosoma cruzi Tulahuen C4 trypomastigotes infected in mouse macrophage by reporter dye assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.
AID1578094Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 48 hrs by [3H]-hypoxanthine incorporation assay2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1439212Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 after 72 hrs by Alamar blue assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and antitrypanosomal activities of novel pyridylchalcones.
AID274300Cytotoxicity against L6 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.
AID418749Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma brucei rhodesiense STIB900 trypomastigotes2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity study of pentamidine analogues as antiprotozoal agents.
AID1245578Antiparasitic activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
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]
AID1193546Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 bloodstream forms after 72 hrs by alamar blue assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.
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]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID475976Inhibition of Trypanosoma brucei brucei recombinant rhodesain after 5 mins by spectrofluorimetry2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.
AID634013Cytotoxicity against rat L6 cells2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds.
AID1336738Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity.
AID1199917Antiprotozoal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB900 trypomastigote by alamar-blue assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Antiprotozoal activity and DNA binding of dicationic acridones.
AID441746Antitrypanosomal activity against bloodstream Trypanosoma brucei rhodesiense STIB 900 after 70 hrs by alamar blue assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (432)

TimeframeStudies, This Drug (%)All Drugs %
pre-199080 (18.52)18.7374
1990's65 (15.05)18.2507
2000's130 (30.09)29.6817
2010's143 (33.10)24.3611
2020's14 (3.24)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.02

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 Index57.02 (24.57)
Research Supply Index6.18 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index95.26 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (57.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials21 (4.58%)5.53%
Reviews22 (4.79%)6.00%
Case Studies26 (5.66%)4.05%
Observational0 (0.00%)0.25%
Other390 (84.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Clinical Trial Comparing the Therapeutic Combinations Melarsoprol-Nifurtimox, Melarsoprol-Eflornithine and Eflornithine-Nifurtimox in the Treatment of Gambiense Human African Trypanosomiasis in the Meningo-Encephalitic Phase [NCT00330148]Phase 3435 participants Interventional2001-03-31Terminated
[information is prepared from clinicaltrials.gov, extracted Sep-2024]