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benzonidazole

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Description

Benzonidazole is a nitroimidazole derivative that has been used for the treatment of Chagas disease, a parasitic infection caused by Trypanosoma cruzi. It is typically administered orally and is effective in reducing the parasite load in patients, particularly in the acute phase of the infection. Benzonidazole is thought to exert its effects by inhibiting the parasite's DNA synthesis and mitochondrial function. Its synthesis involves a multi-step process that includes the nitration of 2-nitroimidazole followed by condensation with benzoyl chloride. The drug has been shown to be safe and effective in clinical trials, although some patients may experience side effects such as nausea, vomiting, and skin rash. Despite its importance in Chagas disease treatment, benzonidazole has several limitations, including its long treatment duration, potential for drug resistance, and limited efficacy in the chronic phase of the infection. Research into benzonidazole focuses on developing more effective and safe treatments for Chagas disease, exploring potential new uses for the drug, and investigating its mechanism of action. The importance of research into benzonidazole stems from the significant burden of Chagas disease, particularly in Latin America, and the need for more effective and accessible treatments. Researchers are also investigating potential new uses for benzonidazole, such as its potential as an anti-cancer drug, and its ability to treat other parasitic infections. Overall, benzonidazole is an important drug for the treatment of Chagas disease, but ongoing research is essential to address its limitations and explore its potential in other medical fields.'

benzonidazole: used in treatment of Chagas' disease [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

benznidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitroimidazol-1-yl)acetic acid with the aromatic amino group of benzylamine. Used for treatment of Chagas disease. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID31593
CHEMBL ID110
CHEBI ID133833
SCHEMBL ID45081
SCHEMBL ID22493029
MeSH IDM0055210

Synonyms (100)

Synonym
radanil
rochagan
ro-7-1051
ragonil
benznidazole [inn]
benzonidazole
ccris 2200
ro 71051
2-nitro-n-(phenylmethyl)-1h-imidazole-1-acetamide
brn 0551486
acetamide, n-benzyl-2-(nitroimidazol-1-yl)-
n-benzyl-2-nitro-1-imidazoleacetamide
benznidazolum [inn-latin]
benznidazol [inn-spanish]
nsc 299972
rochagan (tn)
D02489
benznidazole (tn)
benznidazole (usan/inn)
radanil (tn)
22994-85-0
benznidazole
n-benzyl-2-(2-nitroimidazol-1-yl)acetamide
nsc299972
ro 07-1051
n-benzyl-2-nitroimidazole-1-acetamide
1h-imidazole-1-acetamide, 2-nitro-n-(phenylmethyl)-
imidazole-1-acetamide, n-benzyl-2-nitro-
n-benzyl-2-nitroimidazol-1-yl-acetamide
nsc-299972
MLS001332409
MLS001332410
n-benzyl-2-nitro-1h-imidazole-1-acetamide, 97%
NCGC00166238-01
n-benzyl-2-nitro-1h-imidazole-1-acetamide
smr000857153
MLS001360496
benznidazol
benznidazolum
CHEBI:133833 ,
n-benzyl-2-(2-nitro-1h-imidazol-1-yl)acetamide
n-benzyl-2-(2-nitro-1himidazol-1-yl)acetamide
n-benzyl-2-(2-nitro-imidazol-1-yl)-acetamide
bdbm50089916
n-benzyl-2-(2-nitro-imidazol-1-yl)-acetamide (benznidazole)
n-benzyl-2-(2-nitro-1h-imidazol-5-yl)acetamide
ro-07-1051
benzonidazol
CHEMBL110 ,
FT-0662547
cas-22994-85-0
dtxsid9046570 ,
tox21_112364
dtxcid7026570
AKOS015916722
HMS2233G13
S3741
BRD-K56156805-001-05-4
unii-yc42nrj1zd
benznidazole [usan:inn]
yc42nrj1zd ,
HMS3369C11
benznidazole [mart.]
benznidazole [who-dd]
benznidazole [usan]
benznidazole [mi]
benznidazole [who-ip]
benznidazolum [who-ip latin]
benznidazole [orange book]
SCHEMBL45081
NCGC00166238-02
tox21_112364_1
AKOS024283499
SR-01000841264-3
sr-01000841264
AS-68694
J-014932
mmv688773
DB11989
Q425300
pyridinium,1-dodecyl-2-[(hydroxyimino)methyl]-,iodide(1:1)
Z2044771577
mfcd00243089
2-(2-nitroimidazol-1-yl)-n-(phenylmethyl)acetamide
CS-0013411
HY-B1548
CCG-267054
benznidazol (ro 07-1051; ro 71051)
ro 07-1051;ro 71051
C74184
A912716
SCHEMBL22493029
SR-01000841264-4
1h-imidazole-1-acetamide,2-nitro-n-(phenylmethyl)-
1h-imidazole-1-acetamide, 2-nitro-n-(phenylmethyl)- [
benznidazol (inn-spanish)
benznidazole (mart.)
benznidazolum (inn-latin)
p01ca02
EN300-1716737

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Treatment with benzonidazole was begun leading to suppression of parasitemia."( [Reactivation of Trypanosoma cruzi infection in patients with acquired immunodeficiency syndrome].
Coelho, JM; dos Santos, RR; Galhardo, MC; Hasslocher-Moreno, A; Junqueira, AC; Martins, IA; Ribeiro, Rdos S; Vasconcelos, AC; Xavier, SS,
)
0.47

Toxicity

ExcerptReferenceRelevance
" Studies on Nfx and Bz biotransformation, activation to reactive metabolites, and potential mechanisms for their toxic effects were analyzed."( Toxic effects of nifurtimox and benznidazole, two drugs used against American trypanosomiasis (Chagas' disease).
Castro, JA; Diaz de Toranzo, EG, 1988
)
0.27
" Benznidazole was less toxic (IC(50)=2000 microM) than prodigiosin (IC(50)=1-20 microM) in V79 cells based on the MTT and NAC assays."( Cytotoxicity of prodigiosin and benznidazole on V79 cells.
da Silva Melo, P; Durán, N; Haun, M, 2000
)
0.31
" This alkylphospholipid was also extremely toxic against intracellular amastigotes of both strains."( Proinflammatory and cytotoxic effects of hexadecylphosphocholine (miltefosine) against drug-resistant strains of Trypanosoma cruzi.
Bozza, MT; Freire-De-Lima, CG; Gibaldi, D; Heise, N; Mendonça-Previato, L; Previato, JO; Saraiva, VB, 2002
)
0.31
" Although toxic effects on growth of colonies were not observed, 75 and 100 microM benznidazole induced an increasing of mitotic recombination events in diploid strain."( Benznidazole-induced genotoxicity in diploid cells of Aspergillus nidulans.
Castro-Prado, MA; Kaneshima, EN, 2005
)
0.33
" The most frequent adverse effects observed in the use of Nfx are: anorexia, loss of weight, psychic alterations, excitability, sleepiness, digestive manifestations such as nausea or vomiting, and occasionally intestinal colic and diarrhoea."( Toxic side effects of drugs used to treat Chagas' disease (American trypanosomiasis).
Bartel, LC; Castro, JA; de Mecca, MM, 2006
)
0.33
" Essential program components guaranteeing feasibility of implementation were information, education, and communication (IEC) at the community and family level; vector control; health staff training; screening and diagnosis; treatment and compliance, including family-based strategies for early detection of adverse events; and logistics."( Feasibility, drug safety, and effectiveness of etiological treatment programs for Chagas disease in Honduras, Guatemala, and Bolivia: 10-year experience of Médecins Sans Frontières.
Albajar Viñas, P; Castillo, S; Chambi, W; Ellman, T; Flevaud, L; Lima, MA; Palma, PP; Parreño, F; Roddy, P; Yun, O, 2009
)
0.35
" Benznidazole-related adverse events were observed in 50."( Feasibility, drug safety, and effectiveness of etiological treatment programs for Chagas disease in Honduras, Guatemala, and Bolivia: 10-year experience of Médecins Sans Frontières.
Albajar Viñas, P; Castillo, S; Chambi, W; Ellman, T; Flevaud, L; Lima, MA; Palma, PP; Parreño, F; Roddy, P; Yun, O, 2009
)
0.35
"These results demonstrate the feasibility of implementing Chagas disease diagnosis and treatment programs in resource-limited settings, including remote rural areas, while addressing the limitations associated with drug-related adverse events."( Feasibility, drug safety, and effectiveness of etiological treatment programs for Chagas disease in Honduras, Guatemala, and Bolivia: 10-year experience of Médecins Sans Frontières.
Albajar Viñas, P; Castillo, S; Chambi, W; Ellman, T; Flevaud, L; Lima, MA; Palma, PP; Parreño, F; Roddy, P; Yun, O, 2009
)
0.35
" Benznidazole is the most commonly used drug for the etiological treatment of the disease although its effectiveness varies according to the phase of the same and toxic side effects are frequent."( Side effects of benznidazole treatment in a cohort of patients with Chagas disease in non-endemic country.
Carrilero, B; Martínez-Lage, L; Murcia, L; Segovia, M, 2011
)
0.37
"The Naranjo algorithm was applied to classify the causality of adverse drug reactions (ADRs)."( Safety of benznidazole use in the treatment of chronic Chagas' disease.
Chambela, MC; de Sousa, AS; do Brasil, PE; Hasslocher-Moreno, AM; Sperandio da Silva, GM; Xavier, SS, 2012
)
0.38
"Up to half of patients with Chagas' disease under benznidazole treatment present adverse drug reactions (ADRs) and up to one-third do not complete standard treatment."( Benznidazole treatment safety: the Médecins Sans Frontières experience in a large cohort of Bolivian patients with Chagas' disease.
Brasil, PEAAD; Brum-Soares, LM; Cubides, JC; Fux, CP; Hasslocher-Moreno, AM; Holanda, MT; Mediano, MFF; Mejía, RA; Sangenis, LHC; Saraiva, RM; Silvestre de Sousa, A; Sperandio da Silva, GM, 2017
)
0.46
"Benznidazole treatment was safe and a large proportion of patients were able to complete a full course of benznidazole treatment under close treatment surveillance."( Benznidazole treatment safety: the Médecins Sans Frontières experience in a large cohort of Bolivian patients with Chagas' disease.
Brasil, PEAAD; Brum-Soares, LM; Cubides, JC; Fux, CP; Hasslocher-Moreno, AM; Holanda, MT; Mediano, MFF; Mejía, RA; Sangenis, LHC; Saraiva, RM; Silvestre de Sousa, A; Sperandio da Silva, GM, 2017
)
0.46
"Etiological treatment of Chagas disease in chronic asymptomatic patients is still in debate and the adverse effects of traditional drugs are one of the main concerns in clinical practice."( Risk factors for treatment interruption and severe adverse effects to benznidazole in adult patients with Chagas disease.
Agreda-Rudenko, D; Cucunubá, ZM; Duque, S; Flórez, C; Herazo, R; Nicholls, RS; Olivera, MJ; Valencia-Hernández, CA, 2017
)
0.46
" A multinomial logistic regression model was used to estimate the probability of severe adverse drug reactions (ADRs)."( Risk factors for treatment interruption and severe adverse effects to benznidazole in adult patients with Chagas disease.
Agreda-Rudenko, D; Cucunubá, ZM; Duque, S; Flórez, C; Herazo, R; Nicholls, RS; Olivera, MJ; Valencia-Hernández, CA, 2017
)
0.46
"We observed 305 adverse reactions in 85 of 99 participants (85."( What to expect and when: benznidazole toxicity in chronic Chagas' disease treatment.
Aldasoro, E; Calvo-Cano, A; Casellas, A; Gascon, J; Pinazo, MJ; Posada, E; Requena-Méndez, A; Sanz, S; Serret, N; Soy, D, 2018
)
0.48
"There is a very high frequency of adverse reactions to benznidazole."( What to expect and when: benznidazole toxicity in chronic Chagas' disease treatment.
Aldasoro, E; Calvo-Cano, A; Casellas, A; Gascon, J; Pinazo, MJ; Posada, E; Requena-Méndez, A; Sanz, S; Serret, N; Soy, D, 2018
)
0.48
"The nucleoside antibiotic tubercidin displays strong activity against different target organisms, but it is notoriously toxic to mammalian cells."( Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
Caljon, G; Campagnaro, GD; de Koning, HP; Hulpia, F; Maes, L; Scortichini, M; Van Calenbergh, S; Van Hecke, K, 2019
)
0.51
" Both drugs present high rates of adverse reactions and treatment discontinuation and there is no consensus regarding the most effective administration schedule for benznidazole or how to prevent and manage treatment toxicity."( Comparison of the toxicity of two treatment schemes with benznidazole for chronic Chagas disease: a prospective cohort study in two Spanish referral centres.
Arsuaga, M; Crespillo-Andújar, C; Díaz-Menéndez, M; López-Vélez, R; Monge-Maillo, B; Norman, F; Pérez-Molina, JA; Trigo, E, 2020
)
0.56
" There were also no differences in adverse reactions rate (55."( Comparison of the toxicity of two treatment schemes with benznidazole for chronic Chagas disease: a prospective cohort study in two Spanish referral centres.
Arsuaga, M; Crespillo-Andújar, C; Díaz-Menéndez, M; López-Vélez, R; Monge-Maillo, B; Norman, F; Pérez-Molina, JA; Trigo, E, 2020
)
0.56
" The MTT assay showed that no statistically significant toxic effects occurred in the developed system, nor significant effects on cell viability."( ZIF-8 as a promising drug delivery system for benznidazole: development, characterization, in vitro dialysis release and cytotoxicity.
da Silva Nascimento, DDS; de Albuquerque Wanderley Sales, V; de Moura Ferraz, LR; de Souza Pereira, JJ; Ferreira, AS; Júnior, SA; Rolim, LA; Rolim-Neto, PJ; Silva, JYR; Tabosa, AÉGA, 2020
)
0.56
" However, adverse drug reactions (ADR) are common and frequently cause patients to discontinue treatment."( Mitigation of benznidazole toxicity and oxidative stress following ascorbic acid supplementation in an adult traveller with chronic indeterminate Chagas' disease.
Breynaert, A; De Bruyne, T; Hermans, N; Huits, R; Truyens, C; Van Den Broucke, S; Van Esbroeck, M; Van Herreweghe, M, 2022
)
0.72
" Diagnostic tools, treatment protocols, seroconversion rates and adverse events were investigated."( Monotherapy and combination chemotherapy for Chagas disease treatment: a systematic review of clinical efficacy and safety based on randomized controlled trials.
Cardoso Santos, E; Dias Novaes, R; Lima, GDA; Oliveira Silva, R; Santana Nogueira, S; Vilela Gonçalves, R, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" It was found that the effectiveness of these compounds in producing pharmacokinetic effects correlated directly with their lipophilicity, viz."( Nitroimidazoles as modifiers of nitrosourea pharmacokinetics.
Lee, FY; Workman, P, 1984
)
0.27
" Pharmacokinetic behaviour was linear except at high doses in mice."( Preclinical pharmacokinetics of benznidazole.
Owen, LN; Twentyman, PR; Walton, MI; White, RA; Workman, P, 1984
)
0.27
"Prospective population pharmacokinetic (PK) cohort study in children 2-12 years old with Chagas disease treated with oral benznidazole 5-8 mg/kg/day BID for 60 days."( Population pharmacokinetic study of benznidazole in pediatric Chagas disease suggests efficacy despite lower plasma concentrations than in adults.
Altcheh, J; Ballering, G; Bisio, M; García-Bournissen, F; Giglio, N; Koren, G; Marson, ME; Mastrantonio, G; Moroni, S; Moscatelli, G, 2014
)
0.4
" Furthermore, we demonstrated the application of the method in a preclinical pharmacokinetic study after administration of a single oral dose of BNZ in Wistar rats."( Rapid and sensitive ultra-high-pressure liquid chromatography method for quantification of antichagasic benznidazole in plasma: application in a preclinical pharmacokinetic study.
Davanço, MG; de Campos, ML; Peccinini, RG, 2015
)
0.42
"The aim of the present study was to build a population pharmacokinetic (popPK) model to characterize benznidazole (BNZ) pharmacokinetics in adults with chronic Chagas disease."( Population pharmacokinetics of benznidazole in adult patients with Chagas disease.
Aldasoro, E; Gascón, J; Guerrero, L; Mejía, T; Posada, E; Serret, N; Soy, D; Urbina, JA, 2015
)
0.42
" The pharmacokinetic parameters demonstrated that the extended-release tablets prolonged drug release from the pharmaceutical matrix and provided an increase in the maintenance of the drug concentrationin vivo, which would allow the frequency of administration to be reduced."( Benznidazole Extended-Release Tablets for Improved Treatment of Chagas Disease: Preclinical Pharmacokinetic Study.
Alzate, AH; Campos, ML; Davanço, MG; Padilha, EC; Peccinini, RG; Rolim, LA; Rolim-Neto, PJ; Rosa, TA, 2016
)
0.43
" In this study, BNZ tissue biodistribution in a murine model and its pharmacokinetic profile in plasma were monitored."( Pharmacokinetics and Tissue Distribution of Benznidazole after Oral Administration in Mice.
Cardoso, JM; Carneiro, CM; Correa-Oliveira, R; Fonseca, KD; Mathias, FA; Molina, I; Moreira da Silva, R; Perin, L; Reis, LE; Vieira, PM, 2017
)
0.46
" The pharmacokinetic analysis of benznidazole was evaluated via non-linear mixed-effects modelling using the NONMEN program."( Population pharmacokinetics and biodistribution of benznidazole in mice.
Balthazar Nardotto, GH; Correa-Oliveira, R; da Silva Fonseca, K; Fernanda Rodrigues Bastos Mendes, T; Martins Carneiro, C; Melo de Abreu Vieira, P; Molina, I; Oliveira Paiva, B; Perin, L; Pinto, L, 2020
)
0.56
"Our results demonstrate that mouse weight allometrically influences benznidazole clearance; the AUC curve and the highest plasma concentration are dose proportional; benznidazole does not influence its own metabolism; its tissue distribution is limited; and the standard treatment regimen for Chagas' disease in mice (100 mg/kg/day for 20 days) is inadequate from a pharmacokinetic standpoint, as are the other regimens tested in this study (100 mg/kg/day for 40 days, 200 mg/kg/day for 20 days and 40 mg/kg/day for 20 or 40 days)."( Population pharmacokinetics and biodistribution of benznidazole in mice.
Balthazar Nardotto, GH; Correa-Oliveira, R; da Silva Fonseca, K; Fernanda Rodrigues Bastos Mendes, T; Martins Carneiro, C; Melo de Abreu Vieira, P; Molina, I; Oliveira Paiva, B; Perin, L; Pinto, L, 2020
)
0.56
" The population pharmacokinetic model developed here can allow optimization of the dosing regimen of benznidazole to treat experimental Chagas' disease."( Population pharmacokinetics and biodistribution of benznidazole in mice.
Balthazar Nardotto, GH; Correa-Oliveira, R; da Silva Fonseca, K; Fernanda Rodrigues Bastos Mendes, T; Martins Carneiro, C; Melo de Abreu Vieira, P; Molina, I; Oliveira Paiva, B; Perin, L; Pinto, L, 2020
)
0.56
"The present study aimed to establish a population pharmacokinetic (PopPK) modeling of benznidazole (BZD) in Brazilian patients with chronic Chagas disease."( Population pharmacokinetic modeling of benznidazole in Brazilian patients with chronic Chagas disease.
Bedor, DCG; Frade, VP; Ghilard, FR; Moreira, CHV; Oliveira, CDL; Sabino, EC; Sanches, C, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" In the present study, the effects of benznidazole (BZ) therapy in combination with the iron chelator desferrioxamine (DFO) on the development of infection in mice inoculated with Trypanosoma cruzi Y strain have been investigated."( Trypanosoma cruzi: effect of benznidazole therapy combined with the iron chelator desferrioxamine in infected mice.
Arantes, JM; Bahia, MT; Carneiro, CM; de Abreu Vieira, PM; de Lana, M; Francisco, AF; Martins, HR; Pedrosa, ML; Silva, M; Tafuri, WL; Veloso, VM, 2008
)
0.35
"The present work aimed to investigate the curative effect of benznidazole (BZL) in combination with other patented drugs [nifurtimox (NFX), posaconazole (POS) or AmBisome(®) (AMB)] in mice acutely or chronically infected with either a BZL-susceptible (Tulahuen) or a BZL-partially-resistant (Y) strain of Trypanosoma cruzi."( Evaluation of benznidazole treatment combined with nifurtimox, posaconazole or AmBisome® in mice infected with Trypanosoma cruzi strains.
Carlier, Y; Cencig, S; Coltel, N; Truyens, C, 2012
)
0.38
" In order to improve the drug armamentarium against Chagas' disease, in the present study we describe the synthesis of the compound 3-chloro-7-methoxy-2-(methylsulfonyl) quinoxaline (quinoxaline 4) and its activity, alone or in combination with benznidazole, against Trypanosoma cruzi in vitro."( A quinoxaline derivative as a potent chemotherapeutic agent, alone or in combination with benznidazole, against Trypanosoma cruzi.
Corrêa, AG; Nakamura, CV; Rodrigues, JH; Sangi, DP; Ueda-Nakamura, T, 2014
)
0.4
" Enalapril alone or in combination with benznidazole did not change the number of circulating parasites, but reduced cardiac leukocyte recruitment and total collagen in the cardiac tissue."( Enalapril in Combination with Benznidazole Reduces Cardiac Inflammation and Creatine Kinases in Mice Chronically Infected with Trypanosoma cruzi.
de Paula Costa, G; Horta, AL; Leite, AL; Natali, AJ; Neves, CA; Penitente, AR; Shrestha, D; Talvani, A, 2015
)
0.42
" With the aim of finding new therapeutic approaches, in vitro and in vivo anti-Trypanosoma cruzi activity of vitamin C alone and combined with benznidazole were investigated."( Anti-parasitic effect of vitamin C alone and in combination with benznidazole against Trypanosoma cruzi.
Batlle, A; Demaria, A; Frank, FM; Lombardo, ME; Puente, V, 2018
)
0.48
" Two mechanisms of action may be postulated for vitamin C: a lethal pro-oxidant effect on the parasite when used alone, and an antioxidant effect, when combined with benznidazole."( Anti-parasitic effect of vitamin C alone and in combination with benznidazole against Trypanosoma cruzi.
Batlle, A; Demaria, A; Frank, FM; Lombardo, ME; Puente, V, 2018
)
0.48
"Clove and ginger EOs, administered alone and in combination with BZ, promoted suppression of parasitemia (p < 0."( Essential oils from Syzygium aromaticum and Zingiber officinale, administered alone or in combination with benznidazole, reduce the parasite load in mice orally inoculated with Trypanosoma cruzi II.
de Abreu, AP; de Ornelas Toledo, MJ; de Souza Fernandes, N; Lucas da Silva, HF; Sarto, MPM; Zanusso Junior, G, 2021
)
0.62
"Benznidazole induced effective antiparasitic response, regardless of treatment duration, dose, or combination with fosravuconazole, and was well tolerated in adult patients with chronic Chagas disease."( New regimens of benznidazole monotherapy and in combination with fosravuconazole for treatment of Chagas disease (BENDITA): a phase 2, double-blind, randomised trial.
Almeida, IC; Alonso-Vega, C; Barboza, T; Barreira, F; Bilbe, G; Blum, B; Correia, E; Garcia, W; Gascón, J; Ortiz, L; Parrado, R; Ramirez, JC; Ribeiro, I; Sosa-Estani, S; Strub-Wourgaft, N; Torrico, F; Vaillant, M, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
"Effervescent tablets produced using an inclusion complex of BNZ with CD suggest a possible improvement in the bioavailability of BNZ, and this could represent a relevant advance in Chagas therapy."( Development of effervescent tablets containing benzonidazole complexed with cyclodextrin.
Bahia, MT; Costa, GH; Cunha-Filho, MS; de Sá Barreto, LC; Maximiano, FP, 2011
)
0.63
" These promising results, supported by the in silico prediction of high bioavailability and less potential risk than benznidazole, reveal several tetrahydroquinolines as prototypes of potential antichagasic drugs."( Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
Escario, JA; Fonseca-Berzal, C; Gómez-Barrio, A; Kouznetsov, VV; Merchán Arenas, DR; Romero Bohórquez, AR, 2013
)
0.39
" Taken together, the results demonstrated that the studied derivatives had optimal properties for bioavailability and oral absorption."( Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
Alba-Soto, CD; Briñón, MC; Gualdesi, MS; Novoa, MM; Raviolo, MA; Solana, ME, 2013
)
0.39
" Thus, the aim of this study was to evaluate the impact of stoichiometric and non-stoichiometric BZL-cyclodextrins (CDs) complexes on the bioavailability of BZL."( Effects of benznidazole:cyclodextrin complexes on the drug bioavailability upon oral administration to rats.
Bombardiere, ME; Leonardi, D; Salomon, CJ, 2013
)
0.39
" These results, supported by the in silico prediction of a good oral bioavailability and a suitable risk profile, propose the 4-amino-7-chloroquinoline scaffold as a potential template for designing trypanocidal prototypes."( In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
Escario, JA; Fonseca-Berzal, C; Gómez-Barrio, A; Kouznetsov, VV; Rojas Ruiz, FA, 2014
)
0.4
"This work aims to develop novel benznidazole (BZN) solid dispersions (SD) to improve its solubility and bioavailability properties."( Development of novel benznidazole formulations: physicochemical characterization and in vivo evaluation on parasitemia reduction in Chagas disease.
Arán, VJ; Escario, JA; Fonseca-Berzal, C; Gómez-Barrio, A; Palmeiro-Roldán, R; Torrado-Durán, S; Torrado-Santiago, S, 2014
)
0.4
" The bioavailability of BNZ was adequate in the administration of extended-release tablets; however, with the administration of the pediatric tablet, the bioavailability was lower than with other tablets, which showed that the clinical use of this formulation should be monitored."( Benznidazole Extended-Release Tablets for Improved Treatment of Chagas Disease: Preclinical Pharmacokinetic Study.
Alzate, AH; Campos, ML; Davanço, MG; Padilha, EC; Peccinini, RG; Rolim, LA; Rolim-Neto, PJ; Rosa, TA, 2016
)
0.43
"Benznidazole (BNZ), the only commercialized antichagasic drug, and the antifungal compound posaconazole (PCZ) have shown synergistic action in the therapy of Chagas disease, however both active pharmaceutical ingredients (APIs) exhibit low aqueous solubility potentially limiting their bioavailability and therapeutic efficacy."( Enhancement of dissolution rate through eutectic mixture and solid solution of posaconazole and benznidazole.
de La Roca Soares, MF; de Medeiros Vieira, ACQ; Figueirêdo, CBM; Lee, PI; Nadvorny, D; Rolim Neto, PJ; Soares Sobrinho, JL, 2017
)
0.46
" Thus, the present SD system has the advantage of presenting a fixed-dese combination of two synergistic antichagasic agents PCZ and BNZ together in amorphous form stabilized in the PVPVA matrix with enhanced dissolution, potentially improving their bioavailability and therapeutic activity in treating Chagas disease."( Enhanced delivery of fixed-dose combination of synergistic antichagasic agents posaconazole-benznidazole based on amorphous solid dispersions.
Figueirêdo, CBM; Lee, PI; Nadvorny, D; Rolim Neto, PJ; Schver, GCRM; Soares Sobrinho, JL; Soares, MFR; Vieira, ACQM, 2018
)
0.48
" The present work reviews in detail the formulation and in-vitro/in-vivo analysis of different nanoformulations of nifurtimox and benznidazole in order to enhance their solubility, dissolution, bioavailability and trypanocidal activity."( Nanocarriers for effective delivery of benznidazole and nifurtimox in the treatment of chagas disease: A review.
Arrúa, EC; Bedogni, GR; Okulik, NB; Salomon, CJ; Seremeta, KP, 2019
)
0.51
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" Self-emulsifying drug delivery systems (SEDDS) may improve bioavailability of drugs such as BZ, which have poor water solubility and low permeability."( Benznidazole self-emulsifying delivery system: A novel alternative dosage form for Chagas disease treatment.
Bahia, MT; Gonçalves, KR; Mazzeti, AL; Mosqueira, VCF; Oliveira, LT; Schaun, GC, 2020
)
0.56
" Moreover, the relative oral bioavailability of the novel benznidazole microparticles showed that the area under the curve for the microencapsulated drug was 10."( A Novel Prototype Device for Microencapsulation of Benznidazole: In Vitro/In Vivo Studies.
Barrera, MG; Lamas, MC; Leonardi, D; Salomón, CJ; Tejada, G, 2020
)
0.56
" The dissolution studies corroborated that a pH sensitive Drug Delivery System capable of vectorizing the release of BNZ was developed, may leading to the improvement in the bioavailability of BNZ."( ZIF-8 as a promising drug delivery system for benznidazole: development, characterization, in vitro dialysis release and cytotoxicity.
da Silva Nascimento, DDS; de Albuquerque Wanderley Sales, V; de Moura Ferraz, LR; de Souza Pereira, JJ; Ferreira, AS; Júnior, SA; Rolim, LA; Rolim-Neto, PJ; Silva, JYR; Tabosa, AÉGA, 2020
)
0.56
" However, the Cur therapeutic limitation is its bioavailability and new Cur nanomedicine formulations are developed to overcome this obstacle."( Dual chemotherapy with benznidazole at suboptimal dose plus curcumin nanoparticles mitigates Trypanosoma cruzi-elicited chronic cardiomyopathy.
Corral, RS; Hernández, M; Pérez Caballero, E; Santamaría, MH; Wicz, S, 2021
)
0.62
" These systems ensure high patient acceptability and direct access to the systemic circulation, improving drug bioavailability and toxicological profile."( Development and characterization of thermopressed polyvinyl alcohol films for buccal delivery of benznidazole.
Amaral, BR; Argenta, DF; Caon, T; Enumo, A; Kroth, R; Parize, AL; Rauber, GS; Rebelatto, ERL; Saatkamp, RH, 2021
)
0.62
" Benznidazole, approved by FDA, is a drug of choice but its poor aqueous solubility may lead to a low bioavailability and efficacy."( Improving the oral delivery of benznidazole nanoparticles by optimizing the formulation parameters through a design of experiment and optimization strategy.
Arrua, EC; Goicoechea, H; Hartwig, O; Lehr, CM; Loretz, B; Murgia, X; Salomon, CJ, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" These corresponded to 600 or 900 mg/day of allopurinol for 60 days and benznidazole or nifurtimox at conventional dosage regimens."( Therapeutic efficacy of allopurinol in patients with chronic Chagas' disease.
Gallerano, RH; Marr, JJ; Sosa, RR, 1990
)
0.28
" Of 77 patients studied, 27 were treated with nifurtimox and 26 with benznidazole in the dosage of 5 m/kg/day for 30 consecutive days, and 24 received a placebo in tablets similar to benznidazole."( [Comparative controlled study on the use of benznidazole, nifurtimox and placebo, in the chronic form of Chagas' disease, in a field area with interrupted transmission. I. Preliminary evaluation].
Coura, JR; de Abreu, LL; Petana, W; Willcox, HP,
)
0.13
" The in vivo administration of the thiol drugs, at dosage regimes available in literature, was able to markedly prevent the BZ prolongation effect on the sleeping time."( Prevention of benznidazole-induced prolonging effect on the pentobarbital sleeping time of rats using different thiol-containing compounds.
Bernacchi, AS; Castro, JA; Montalto de Mecca, M,
)
0.13
" Nevertheless, the cytotoxic effect of miltefosine against intracellular amastigotes was independent of the amount of NO produced by the infected macrophages since the same dose-response curves for miltefosine were observed when the NO production was blocked by the NO synthase inhibitor N(G)-monomethyl-L-arginine monoacetate."( Proinflammatory and cytotoxic effects of hexadecylphosphocholine (miltefosine) against drug-resistant strains of Trypanosoma cruzi.
Bozza, MT; Freire-De-Lima, CG; Gibaldi, D; Heise, N; Mendonça-Previato, L; Previato, JO; Saraiva, VB, 2002
)
0.31
"4 mg/ml), which precludes the preparation of liquid dosage forms, in particular, parenteral formulations."( Development of parenteral formulations and evaluation of the biological activity of the trypanocide drug benznidazole.
Bassani, G; Lamas, MC; Leonardi, D; Nocito, I; Pascutti, F; Salomón, CJ; Serra, E; Villaggi, L, 2006
)
0.33
" Chronic model of the disease showed that both canthin-6-one (1) and the alkaloidal extract at the above dosage induced 80-100% animal survival compared to untreated controls."( Effects of canthin-6-one alkaloids from Zanthoxylum chiloperone on Trypanosoma cruzi-infected mice.
de Arias, AR; de Bilbao, NV; Ferreira, ME; Fournet, A; Hocquemiller, R; Lagoutte, D; Nakayama, H; Poupon, E; Schinini, A; Serna, E; Soriano-Agatón, F, 2007
)
0.34
" The plasma exposure profiles for each compound following a single oral dose in mice and estimated exposure parameters after repeated twice-daily dosing for 20 days are also presented."( Pharmacological characterization, structural studies, and in vivo activities of anti-Chagas disease lead compounds derived from tipifarnib.
Bahia, MT; Buckner, FS; Charman, SA; Chatelain, E; Chennamaneni, NK; Gelb, MH; Hulverson, MA; Laydbak, JU; Lepesheva, GI; Scandale, I; Shackleford, DM; Suryadevara, PK; Verlinde, CL; White, KL, 2012
)
0.38
" Despite of the large number of pediatric patients infected, there are no commercial liquid dosage forms available to treat this trypanosomiasis."( Efficacy of novel benznidazole solutions during the experimental infection with Trypanosoma cruzi.
Bottasso, E; Lamas, MC; Manarin, R; Revelli, S; Salomón, CJ; Serra, E, 2013
)
0.39
" cruzi infection after once daily oral dosing at 20, 50 and 100 mg/kg for 5 days."( Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
Alexander, PW; Best, WM; Charman, SA; Chatelain, E; Diao, H; Gregg, AD; Keenan, M; Kerfoot, M; Khong, A; Ryan, E; Scandale, I; Shackleford, DM; Thompson, RC; von Geldern, TW; White, KL, 2013
)
0.39
" Therefore, the dosage of anti-Tc13Tul antibodies may be useful as a methodology complementary to CS to evaluate chagasic patients undergoing chemotherapy with benznidazole."( Use of an enzyme-linked immunosorbent assay that utilizes the Tc13Tul antigen of Trypanosoma cruzi to monitor patients after treatment with benznidazole.
Bruballa, AC; De Rissio, AM; Garavaglia, PA; García, GA; Irazu, LE; Riarte, A; Rodríguez, MA; Ruiz, AM; Santamaría, AL, 2013
)
0.39
" Real samples of human breast milk from patients in treatment with BNZ were dosed to support the validation process of the method."( A simple and efficient HPLC method for benznidazole dosage in human breast milk.
Altcheh, J; García-Bournissen, F; Marson, ME; Mastrantonio, G; Padró, JM; Reta, MR, 2013
)
0.39
" Reducing the overall dosage of BZ or NFX by using an intermittent (once every 5 days) schedule or combining 5 daily doses of POS with 7 intermittent doses of BZ also provided approximately 100% cure."( New, combined, and reduced dosing treatment protocols cure Trypanosoma cruzi infection in mice.
Bustamante, JM; Craft, JM; Crowe, BD; Ketchie, SA; Tarleton, RL, 2014
)
0.4
"To investigate the direct and indirect photodegradation of BNZ and to evaluate the interference of the excipients used in the forms dosage solid as well as to shed light on the chemical structure of the degradation products obtained."( A study of photostability and compatibility of the anti-chagas drug Benznidazole with pharmaceutics excipients.
Ferraz, LR; Figueirêdo, CB; Lima Leite, AC; Lyra, MA; Neves de Lima, ÁA; Peixoto, MS; Rolim Neto, PJ; Rolim, LA; Santos, FL; Soares-Sobrinho, JL, 2015
)
0.42
" The indirect photodegradation of BNZ was carried out using physical mixtures with 13 pharmaceutical excipients commonly used in the preparation of solid dosage forms."( A study of photostability and compatibility of the anti-chagas drug Benznidazole with pharmaceutics excipients.
Ferraz, LR; Figueirêdo, CB; Lima Leite, AC; Lyra, MA; Neves de Lima, ÁA; Peixoto, MS; Rolim Neto, PJ; Rolim, LA; Santos, FL; Soares-Sobrinho, JL, 2015
)
0.42
" cruzi infection after once daily oral dosing for 20 days at 20 mg/kg 6 and 10 mg/kg (S)-7."( Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
Abbott, MJ; Alexander, PW; Best, WM; Botero, A; Campbell, M; Chaplin, JH; Charman, SA; Chatelain, E; Chiu, FC; Cornwall, S; Keenan, M; Khong, A; Koltun, M; Morizzi, J; Perez, C; Ryan, E; Scandale, I; Shackleford, DM; Thompson, RA; von Geldern, TW; White, KL, 2013
)
0.39
" cruzi infection, with oral dosing in chow for 28 days at doses from 3 to 50 mg/kg of body weight."( Reversible cysteine protease inhibitors show promise for a Chagas disease cure.
Beaulieu, C; Black, WC; Isabel, E; Massé, F; Mellon, C; Methot, N; Nath-Chowdhury, M; Ndao, M; Nicoll-Griffith, DA; Vasquez-Camargo, F, 2014
)
0.4
" Pharmacokinetic data suggested that biological efficacy most likely resides with the sulfone metabolite (or subsequent reactive metabolites formed following reduction of the nitro group) following administration of either the sulfoxide or the sulfone and that prolonged plasma exposure over the 24-h dosing window is required to achieve high cure rates."( Antitrypanosomal activity of fexinidazole metabolites, potential new drug candidates for Chagas disease.
Bahia, MT; Caldas, IS; Charman, SA; Chatelain, E; Diniz, Lde F; Gonçalves, KR; Koltun, M; Marques, LF; Mazzeti, AL; Mota, LW; Nascimento, AF; Saunders, J; Scandale, I; Shackleford, DM; Talvani, A; White, KL, 2014
)
0.4
" Later on, simulations were performed to generate BNZ concentration-time course profiles for different dosage regimens."( Population pharmacokinetics of benznidazole in adult patients with Chagas disease.
Aldasoro, E; Gascón, J; Guerrero, L; Mejía, T; Posada, E; Serret, N; Soy, D; Urbina, JA, 2015
)
0.42
" The activities of the benznidazole/itraconazole combinations were compared with the results from those receiving the same dosage of each individual drug."( Benznidazole/Itraconazole Combination Treatment Enhances Anti-Trypanosoma cruzi Activity in Experimental Chagas Disease.
Assíria Fontes Martins, T; Bahia, MT; Caldas, IS; Caldas, S; da Silva do Nascimento, ÁF; de Andrade, IM; de Figueiredo Diniz, L; Mazzeti, AL; Ribeiro, I, 2015
)
0.42
" In the current study, we sought to identify a dosing regimen of posaconazole that could permanently clear Trypanosoma cruzi from mice with experimental Chagas disease."( Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease.
Glynne, R; Groessl, T; Khare, S; Liu, X; Molteni, V; Rivera, I; Stinson, M; Supek, F; Tuntland, T; Wen, B; Yeh, V, 2015
)
0.42
" In short, the quantification of BNZ and ITZ by analysis of mixtures had shown to be efficient and cost-effective alternative for determination of these drugs in a pharmaceutical dosage form."( Simultaneous determination of benznidazole and itraconazole using spectrophotometry applied to the analysis of mixture: A tool for quality control in the development of formulations.
Cunha-Filho, MS; Infante, CM; Pinho, LA; Sá-Barreto, LC, 2016
)
0.43
" Since dosage may influence ADE, we aimed to assess Bzl efficacy in terms of parasiticidal and anti-inflammatory activity, using doses lower than those previously reported."( Low-dose benznidazole treatment results in parasite clearance and attenuates heart inflammatory reaction in an experimental model of infection with a highly virulent Trypanosoma cruzi strain.
Cevey, ÁC; Goren, NB; Mirkin, GA; Penas, FN, 2016
)
0.43
" We have adapted a continuous enzymatic assay to a medium-throughput format and carried out a primary screening of both collections, followed by construction and analysis of dose-response curves of the most promising hits."( Novel scaffolds for inhibition of Cruzipain identified from high-throughput screening of anti-kinetoplastid chemical boxes.
Agüero, F; Alvarez, VE; Cazzulo, JJ; Karpiak, J; Landaburu, LU; Madauss, KP; Salas-Sarduy, E, 2017
)
0.46
" Benznidazole is still the drug of choice in many countries to treat it in spite of its dosage regimen and adverse side effects such as such as allergic dermatitis, peripheral neuropathy and anorexia."( Elucidating the impact of low doses of nano-formulated benznidazole in acute experimental Chagas disease.
Arrúa, EC; Esteva, MI; Fichera, LE; Rial, MS; Salomon, CJ; Scalise, ML, 2017
)
0.46
" PCR analysis of blood samples taken after induction of immunosuppression showed that a dosage of 25 mg/kg/day rendered 40% of the mice PCR-negative."( Elucidating the impact of low doses of nano-formulated benznidazole in acute experimental Chagas disease.
Arrúa, EC; Esteva, MI; Fichera, LE; Rial, MS; Salomon, CJ; Scalise, ML, 2017
)
0.46
" cruzi acute infections in immunosuppressed and non-immunosuppressed mice and provides further evidence for the optimization of dosage regimens to treat Chagas disease."( Elucidating the impact of low doses of nano-formulated benznidazole in acute experimental Chagas disease.
Arrúa, EC; Esteva, MI; Fichera, LE; Rial, MS; Salomon, CJ; Scalise, ML, 2017
)
0.46
" Optimised dosing schedules and/or new drugs are urgently needed."( Safety Profile of Benznidazole in the Treatment of Chronic Chagas Disease: Experience of a Referral Centre and Systematic Literature Review with Meta-Analysis.
Crespillo-Andújar, C; López-Polín, A; López-Vélez, R; Monge-Maillo, B; Norman, F; Pérez-Molina, JA; Venanzi-Rullo, E, 2018
)
0.48
"Two hundred mice were divided into five groups according to benznidazole dosing regimens: (1) 100 mg/kg/day for 20 days; (2) 100 mg/kg/day for 40 days; (3) 200 mg/kg/day for 20 days; (4) 40 mg/kg/day for 20 days; or (5) 40 mg/kg/day for 40 days."( Population pharmacokinetics and biodistribution of benznidazole in mice.
Balthazar Nardotto, GH; Correa-Oliveira, R; da Silva Fonseca, K; Fernanda Rodrigues Bastos Mendes, T; Martins Carneiro, C; Melo de Abreu Vieira, P; Molina, I; Oliveira Paiva, B; Perin, L; Pinto, L, 2020
)
0.56
" The population pharmacokinetic model developed here can allow optimization of the dosing regimen of benznidazole to treat experimental Chagas' disease."( Population pharmacokinetics and biodistribution of benznidazole in mice.
Balthazar Nardotto, GH; Correa-Oliveira, R; da Silva Fonseca, K; Fernanda Rodrigues Bastos Mendes, T; Martins Carneiro, C; Melo de Abreu Vieira, P; Molina, I; Oliveira Paiva, B; Perin, L; Pinto, L, 2020
)
0.56
" Considering our previous data on solubility, together with these on efficacy, this new liquid formulation represents a promising alternative for the treatment of Chagas disease, particularly in cases when dosing poses a challenge, as in infants."( Benznidazole/Poloxamer 407 Solid Dispersion as a New Strategy to Improve the Treatment of Experimental Trypanosoma cruzi Infection.
Bermúdez, JM; Cid, AG; Davies, C; Micheloud, JF; Negrette, OS; Parada, LA; Ragone, PG; Simonazzi, A, 2020
)
0.56
" Dose-response curves were calculated for each time point after addition of test compounds, revealing how EC50 values first decreased over the time of drug exposure, and then leveled off."( Non-invasive monitoring of drug action: A new live in vitro assay design for Chagas' disease drug discovery.
Braissant, O; Fesser, AF; Kaiser, M; Kelly, JM; Mäser, P; Olmo, F, 2020
)
0.56
" Following initial profiling, a first proof-of-concept in vivo study was undertaken, in which once daily oral dosing of a 7-substituted 2-nitroimidazooxazine analogue suppressed blood parasitemia to low or undetectable levels, although sterile cure was not achieved."( Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Avery, VM; Charman, SA; Chatelain, E; Cornwall, S; Denny, WA; Francisco, AF; Keenan, M; Kelly, JM; Marshall, AJ; O'Connor, PD; Perez, CJ; Read, KD; Riley, J; Sykes, ML; Thompson, AM; Thompson, RCA; White, KL; Zulfiqar, B, 2020
)
0.56
" To both avoid off-target side effects and reduce the necessary dosage of BNZ, we packaged the drug within poly(ethylene glycol)-block-poly(propylene sulfide) polymersomes (BNZ-PSs)."( Nanocarrier-enhanced intracellular delivery of benznidazole for treatment of Trypanosoma cruzi infection.
Engman, DM; Falk, BA; Li, X; Martinez, SJ; Olson, CL; Romano, PS; Scariot, DB; Scott, EA; Yi, S, 2021
)
0.62
" Thus, this work aimed to develop a novel DDS based on BNZ and the ZIF-8 to use it in development of prolonged-release dosage forms to alternative treatment of Chagas disease."( Benznidazole in vitro dissolution release from a pH-sensitive drug delivery system using Zif-8 as a carrier.
da Silva Nascimento, DDS; de Moura Ferraz, LR; Ferreira, AS; Junior, SA; Rolim, LA; Rolim-Neto, PJ; Silva, JYR; Tabosa, AÉGA, 2021
)
0.62
" Although these studies suggest that rigorously timed and more potent dosing regimen may be needed to achieve an immediate benefit of prophylaxis, additional studies would be needed to determine if drug prophylaxis reduced disease severity despite this failure to prevent new infections."( Prophylactic low-dose, bi-weekly benznidazole treatment fails to prevent Trypanosoma cruzi infection in dogs under intense transmission pressure.
Auckland, LD; Busselman, RE; Bustamante, JM; Collins, S; Hamer, SA; Malcolm, EL; Padilla, AM; Saunders, AB; Tarleton, RL; White, B; Wilson, BF, 2022
)
0.72
"5-fold that of previously used daily dosing protocols, provided the best chance to obtain parasitological cure."( Frequency Variation and Dose Modification of Benznidazole Administration for the Treatment of Trypanosoma cruzi Infection in Mice, Dogs, and Nonhuman Primates.
Auckland, LD; Bustamante, JM; Hamer, SA; Hodo, CL; McCain, S; Saunders, AB; Tarleton, RL; Wang, W; White, BE; Wilkerson, GK, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antiprotozoal drugAny antimicrobial drug which is used to treat or prevent protozoal infections.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
imidazolesA five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton.
C-nitro compoundA nitro compound having the nitro group (-NO2) attached to a carbon atom.
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency5.62340.044717.8581100.0000AID485294
thioredoxin reductaseRattus norvegicus (Norway rat)Potency79.43280.100020.879379.4328AID588453
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency38.90180.01237.983543.2770AID1645841
gemininHomo sapiens (human)Potency17.78280.004611.374133.4983AID624297
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Glyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)IC50 (µMol)50.00006.00007.33338.0000AID75731
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)100.00000.00011.774010.0000AID1381720
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)98.20000.00011.753610.0000AID1381724
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)77.80000.00002.015110.0000AID1381723
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)100.00000.00002.800510.0000AID1381721
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)100.00000.00002.398310.0000AID1381722
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)100.00000.00091.901410.0000AID1381719
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Aurora kinase BHomo sapiens (human)IC50 (µMol)100.00000.00030.96349.8000AID1381725
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (156)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
microtubule cytoskeleton organizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of cytokine productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glucose metabolic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
glycolytic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of endopeptidase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
regulation of macroautophagyGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
negative regulation of translationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing of cells of another organismGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of type I interferon productionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-trans-nitrosylationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein stabilizationGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
defense response to fungusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
neuron apoptotic processGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
killing by host of symbiont cellsGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cellular response to type II interferonGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIAurora kinase BHomo sapiens (human)
mitotic cell cycleAurora kinase BHomo sapiens (human)
mitotic cytokinesisAurora kinase BHomo sapiens (human)
negative regulation of B cell apoptotic processAurora kinase BHomo sapiens (human)
protein phosphorylationAurora kinase BHomo sapiens (human)
spindle organizationAurora kinase BHomo sapiens (human)
attachment of spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
abscissionAurora kinase BHomo sapiens (human)
negative regulation of protein bindingAurora kinase BHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseAurora kinase BHomo sapiens (human)
negative regulation of cytokinesisAurora kinase BHomo sapiens (human)
positive regulation of cytokinesisAurora kinase BHomo sapiens (human)
protein localization to kinetochoreAurora kinase BHomo sapiens (human)
cellular response to UVAurora kinase BHomo sapiens (human)
cleavage furrow formationAurora kinase BHomo sapiens (human)
post-translational protein modificationAurora kinase BHomo sapiens (human)
cell cycle G2/M phase transitionAurora kinase BHomo sapiens (human)
mitotic cytokinesis checkpoint signalingAurora kinase BHomo sapiens (human)
negative regulation of innate immune responseAurora kinase BHomo sapiens (human)
protein autophosphorylationAurora kinase BHomo sapiens (human)
mitotic spindle midzone assemblyAurora kinase BHomo sapiens (human)
positive regulation of telomerase activityAurora kinase BHomo sapiens (human)
regulation of chromosome segregationAurora kinase BHomo sapiens (human)
positive regulation of mitotic sister chromatid segregationAurora kinase BHomo sapiens (human)
positive regulation of mitotic cell cycle spindle assembly checkpointAurora kinase BHomo sapiens (human)
mitotic spindle assemblyAurora kinase BHomo sapiens (human)
negative regulation of cGAS/STING signaling pathwayAurora kinase BHomo sapiens (human)
regulation of signal transduction by p53 class mediatorAurora kinase BHomo sapiens (human)
positive regulation of mitotic sister chromatid separationAurora kinase BHomo sapiens (human)
positive regulation of attachment of mitotic spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
positive regulation of mitotic cytokinesisAurora kinase BHomo sapiens (human)
positive regulation of telomere cappingAurora kinase BHomo sapiens (human)
positive regulation of lateral attachment of mitotic spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
mitotic spindle organizationAurora kinase BHomo sapiens (human)
regulation of cytokinesisAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (79)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
glyceraldehyde-3-phosphate dehydrogenase (NAD+) (phosphorylating) activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
peptidyl-cysteine S-nitrosylase activityGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
identical protein bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NADP bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
NAD bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
disordered domain specific bindingGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein serine/threonine kinase activityAurora kinase BHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase BHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase BHomo sapiens (human)
protein bindingAurora kinase BHomo sapiens (human)
ATP bindingAurora kinase BHomo sapiens (human)
kinase bindingAurora kinase BHomo sapiens (human)
protein serine kinase activityAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (45)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
nucleusGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
lipid dropletGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
plasma membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
microtubule cytoskeletonGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
nuclear membraneGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
vesicleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
intracellular membrane-bounded organelleGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
perinuclear region of cytoplasmGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
extracellular exosomeGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
GAIT complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
ribonucleoprotein complexGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
cytosolGlyceraldehyde-3-phosphate dehydrogenaseHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
kinetochoreAurora kinase BHomo sapiens (human)
condensed chromosome, centromeric regionAurora kinase BHomo sapiens (human)
nucleusAurora kinase BHomo sapiens (human)
nucleoplasmAurora kinase BHomo sapiens (human)
spindleAurora kinase BHomo sapiens (human)
cytosolAurora kinase BHomo sapiens (human)
chromocenterAurora kinase BHomo sapiens (human)
microtubule cytoskeletonAurora kinase BHomo sapiens (human)
midbodyAurora kinase BHomo sapiens (human)
chromosome passenger complexAurora kinase BHomo sapiens (human)
mitotic spindle poleAurora kinase BHomo sapiens (human)
mitotic spindle midzoneAurora kinase BHomo sapiens (human)
kinetochoreAurora kinase BHomo sapiens (human)
spindle pole centrosomeAurora kinase BHomo sapiens (human)
spindle microtubuleAurora kinase BHomo sapiens (human)
spindle midzoneAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1875)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1687779Selectivity index, ratio of GI50 for human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay to IC50 for antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in African gr2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID547274Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG2 at 7 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID707764Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in BALB/c mouse model of acute Chagas disease assessed as reduction parasitemia at 5 mg/kg/day, ip administered for 5 consecutive days starting on day 7 post i2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID341607Antimicrobial activity against Babesia divergens 42012007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1281434Induction of apoptosis in trypamostigote form of Trypanosoma cruzi Y assessed as late apoptotic cells at 25 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry relative to untreated control2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID426304Antiparasitic activity against Trichomonas vaginalis GT3 trophozoites after 48 hrs by Hill culture method2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles.
AID576949Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as reduction in parasite specific antibodies at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection measur2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1518999Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as effect on PR interval at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measur2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID576831Antitrypanosomal activity against Trypanosoma cruzi infected in african green monkey Vero cells assessed as reduction of parasite infection rate at IC25 after 10 days2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1854942Induction of cell death in Trypanosoma cruzi Y epimastigotes assessed as early apoptotic cells at 125 uM incubated for 24 hrs by Annexin V/7-AAD staining based flow cytometric analysis (Rvb = 0.11 %)2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1683675Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on ASG/GOT level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1240904Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by inverted microscope analysis2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.
AID1615012Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID776316Antiparasitic activity against Trypanosoma cruzi amastigotes after 3 days by fluorescence assay2013European journal of medicinal chemistry, Nov, Volume: 69Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents.
AID263381Unspecific cytotoxicity against murine J774 macrophages at 1 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID1543105Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in LLC-MK2-ATCC CCL7 cells assessed as reduction in parasite growth incubated for 24 hrs by Alamar blue dye based assay2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Structure-activity relationship study of antitrypanosomal chalcone derivatives using multivariate analysis.
AID1603753Antitrypanosomal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 6 epimastigotes measured after 72 hrs by Neubauer hemocytometer2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID576102Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Vomiting at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID367083Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen C2C4 containing lacZ gene in rat L6 cells after 4 days2009Bioorganic & medicinal chemistry letters, Feb-01, Volume: 19, Issue:3
Synthesis, in vitro antitrypanosomal and antibacterial activity of phenoxy, phenylthio or benzyloxy substituted quinolones.
AID364956Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 assessed as inhibition of epimastigotes growth after 5 days by MTT assay relative to control2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Furoxan-, alkylnitrate-derivatives and related compounds as anti-trypanosomatid agents: mechanism of action studies.
AID596493Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 amastigotes2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Marinoquinolines A-F, pyrroloquinolines from Ohtaekwangia kribbensis (Bacteroidetes).
AID1584768Antiparasitic activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes infected in Swiss Webster mouse assessed as protection against parasite-induced mortality at 100 mg/kg, po sid via gavage administered for 5 consecutive days starting fr2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID213669In vitro growth inhibition of epimastigotes of Trypanosoma cruzi2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Toxic effects of natural piperine and its derivatives on epimastigotes and amastigotes of Trypanosoma cruzi.
AID1706434Cytotoxicity against rat 3T3 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID396021Antimicrobial activity against Trypanosoma cruzi genotype 20 and genotype 19 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1498335Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1812898Antitrypanosomal activity against Trypanosoma cruzi infected in mouse C2C12 cells incubated for 2 days by DAPI staining based microscopic analysis2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
AID1615030Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypomastigotes derived from infected Balb/c mouse2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID337138Antitrypanosomal activity against Trypanosoma cruzi 13379 CL5 after 48 hrs
AID1403392Trypanocidal activity against infected Swiss Webster mouse derived bloodstream form of Trypanosoma cruzi Y after 24 hrs by cell-titer-glo assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1592306Selectivity index, ratio of CC50 for mouse J774.A1 cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi MHOM/MX/1994/INC5 epimastigotes
AID1361362Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood assessed as parasite lysis at 10 ug/ml after 24 hrs by optical microscopic method relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.
AID576830Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for epimastigote of Trypanosoma cruzi Maracay2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1686727Genotoxicity in Salmonella typhimurium in presence of metabolic activation by SOS/umu test2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1403410Therapeutic index, ratio of CC50 for Swiss Webster mouse cardiomyocytes to IC50 for Trypanosoma cruzi Y intracellular amastigotes infected in Swiss Webster mouse cardiomyocytes2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID285209Mortality rate in Trypanosoma cruzi Y infected IL12 knock out C57BL/6 mouse Chagas disease model at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1498349Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1403391Trypanocidal activity against Trypanosoma cruzi Y trypomastigotes infected in monkey LLC-MK2 cells after 24 hrs by cell-titer-glo assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1498232Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in heart tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starti2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID456260Antitrypanosomal activity against Trypanosoma cruzi 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.
AID726229Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 256 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID576828Antitrypanosomal activity against epimastigote of Trypanosoma cruzi Maracay after 72 hrs2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1281412Cytotoxicity against BALB/c mouse splenocytes assessed as highest non-toxic concentration causing >90 % incorporation of [3H]-thymidine after 24 hrs by beta counting method2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID344432Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 1 mM after 4 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1072682Antitrypanosomal activity against Trypanosoma cruzi Y metacyclic trypomastigotes isolated from infected LLC-MK2 cells assessed as parasite viability after 24 hrs by neubauer chamber analysis2014European journal of medicinal chemistry, Mar-21, Volume: 75Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death.
AID1154403Antitrypanosomal activity against blood stage trypomastigote form of Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction of blood parasitemia at 100 mg/kg, po qd administered for 5 days relative to control2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
AID1278153Selectivity index, ratio of CC50 for mouse NCTC-292 cells to IC50 for Trypanosoma cruzi Y amastigotes2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.
AID1603771Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 6 amastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1432287Growth inhibition of Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells at 20 uM after 48 hrs relative to control2017European journal of medicinal chemistry, Mar-10, Volume: 128Design and synthesis of a new series of 3,5-disubstituted isoxazoles active against Trypanosoma cruzi and Leishmania amazonensis.
AID1615127Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID364961Antileishmanial activity against Leishmania pifanoi MHOM/VE/57/LV135 assessed as parasite viability after 5 days by MTT assay2008Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
Furoxan-, alkylnitrate-derivatives and related compounds as anti-trypanosomatid agents: mechanism of action studies.
AID1613510Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured o2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1588483Antiparasitic activity against Trypanosoma cruzi amastigote infected in African green monkey Vero cells decrease in parasite viability measured at day 3 of post infection by red fluorescent protein based fluorescence method2019Bioorganic & medicinal chemistry, 08-15, Volume: 27, Issue:16
Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii.
AID1879377Antitrypanosomal activity against intracellular Trypanosoma cruzi Tulahuen amastigotes expressing CL2 beta-galactosidase in human MRC5 cells assessed as parasite growth inhibition using chlorophenol red beta-D-galactopyranoside as substrate treated for 7 2022European journal of medicinal chemistry, Mar-05, Volume: 231N
AID1569971Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi trypomastigotes after 24 hrs by Neubauer chamber method2019European journal of medicinal chemistry, Oct-15, Volume: 1802-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity.
AID1233721Antiparasite activity against Trypanosoma cruzi Tulahuen expressing beta-galactosidase assessed as growth inhibition incubated for 96 hrs by CPRG dye based assay2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery.
AID1070006Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 2 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1238029Cytotoxicity against BALB/c mouse peritoneal macrophages incubated for 24 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1074378Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for amastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID774787Antiprotozoal activity against Trypanosoma cruzi 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.
AID1616165In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection and measured up t2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID284137Trypanocidal activity in Swiss albino mouse inoculated with Trypanosoma cruzi Y blood trypomastigotes assessed as parasitaemia reduction administered after 7th day of inoculation at 250 mg/kg, po after 6 hrs relative to control2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and trypanocidal activity of ent-kaurane glycosides.
AID392009Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected Swiss mouse assessed as reduction in circulating trypomastigotes antibody level at 200 mg/kg/day, po after 60 days postinfection2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1519001Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as effect on heart rate at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measure2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID285215Antimicrobial activity against Trypanosoma cruzi Y infected IL12 knock out C57BL/6 mouse Chagas disease model assessed as percent of cured mouse at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1072683Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes assessed as inhibition of parasite proliferation after 5 days by hemocytometer analysis2014European journal of medicinal chemistry, Mar-21, Volume: 75Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death.
AID1164933Induction of apoptosis in human monocytes assessed as late apoptotic cells using Annexin V/propidium iodide by flow cytometry (Rvb = 0.27 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1773691Selectivity index, ratio of CC50 for cytotoxicity against mouse C2C12 cells to EC50 for trypanocidal activity against Trypanosoma cruzi C-I/72 infected in mouse C2C12 cells2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
Structure-Based Optimization of Quinazolines as Cruzain and
AID1300857Activity at recombinant His-tagged Trypanosoma brucei NTR assessed as oxidation of NADH/min/mg of protein after 5 mins by spectrophotometric analysis2016European journal of medicinal chemistry, Jul-19, Volume: 117Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.
AID1498311Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1766960Selectivity index, ratio of CC50 for cytotoxicity against mouse NCTC clone 929 cells to IC50 for trypomastigote forms of Trypanosoma cruzi Y infected in LLC-MK2 cells
AID677564Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 amastigotes2012Journal 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.
AID1615038Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 p2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1633358Antitrypanosomal activity against Trypanosoma cruzi Dm28c trypomastigotes infected in African green monkey Vero cells incubated for 24 hrs by luciferase-luminescence based assay
AID1124783Cytotoxicity against human HepG2 cells by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1687708Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as reduction in parasitemia at 50 mg/kg, po treated 10 days post infection for 7 consecutive days by Neubauer chamber counting method relative to control2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1707635Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC-5 SV2 cells2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of a collection of purine-like C-nucleosides as antikinetoplastid agents.
AID1196789Toxicity in Balb/c mouse at 15 mg/kg/day, ip measured after 5 to 10 days2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID753034Cytotoxicity against human fibroblasts assessed as growth inhibition after 24 hrs by MTT assay2013European journal of medicinal chemistry, Jun, Volume: 64Ligand-based design, synthesis, and experimental evaluation of novel benzofuroxan derivatives as anti-Trypanosoma cruzi agents.
AID1174778Trypanocidal activity against intracellular amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 in african green monkey Vero cells2015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1699437Selectivity index, ratio of IC50 for cytotoxicity against rat L6 cells to IC50 for growth inhibition of amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells2020Journal of natural products, 11-25, Volume: 83, Issue:11
Pyridine-4(1
AID1348368Antitrypanosomal activity against beta-galactosidase expressing nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as decrease in parasite burden after 168 hrs by spectrophotometric method2018European journal of medicinal chemistry, Jan-01, Volume: 143Novel triazine dimers with potent antitrypanosomal activity.
AID1459244Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as parasite duplication time at 1 to 15 uM supplemented with fresh medium containing compound every 9 to 10 days measured on third week2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID547275Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Y assessed as production of antibody IgG at 7 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1613530Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1686726Genotoxicity in Salmonella typhimurium TA1535/pSK1002 in absence of rat S9 mix incubated for 4 hrs by SOS/umu test2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID671575Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen infected immunosuppressed Swiss mouse assessed as level of parasite in blood at 20 mg/kg, po administered 8 day after post infection qd for 20 days measured after 3 cycles of 2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
AID450067Antitrypanosomal activity against Trypanosoma cruzi epimastigote Y strain after 24 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents.
AID634123Antitrypanosomal activity against Trypanosoma cruzi Tulaheun infected in monkey LLC-MK2 cells after 4 days by beta-galactosidase reporter gene assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Design, synthesis and the effect of 1,2,3-triazole sialylmimetic neoglycoconjugates on Trypanosoma cruzi and its cell surface trans-sialidase.
AID362869Therapeutic index, ID50 for human THP1 cells to ID50 for Trypanosoma cruzi2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
4-nitroacetophenone-derived thiosemicarbazones and their copper(II) complexes with significant in vitro anti-trypanosomal activity.
AID1603868Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum alanine aminotransferase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1603758Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 62019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1854941Induction of cell death in Trypanosoma cruzi Y epimastigotes assessed as live cells at 125 uM incubated for 24 hrs by Annexin V/7-AAD staining based flow cytometric analysis (Rvb = 98.6 %)2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1399452Antitrypanosomal activity against Trypanosoma brucei Lister 427 bloodstream forms after 48 hrs by resazurin dye based fluorescence assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.
AID1055185Cytotoxicity against African green monkey Vero cells after 72 hrs by flow cytometric analysis2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID547252Antimicrobial activity against Trypanosoma cruzi Berenice-78 infected in mongrel dog assessed as suppression of microbial proliferation at 12 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1869516Antitrypanosomal activity against Trypanosoma cruzi epimastigotes assessed as parasite growth inhibition measured after 24 hrs by CellTiter-glo luminescence assay2022Journal of natural products, 07-22, Volume: 85, Issue:7
Phytohabitols A-C, δ-Lactone-Terminated Polyketides from an Actinomycete of the Genus
AID1244474Selectivity index, ratio of LC50 for human U937 cells to EC50 for intracellular amastigotes of Trypanosoma cruzi Tulahuen2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids.
AID1687781Selectivity index, ratio of GI50 for mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay to IC50 for antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in African2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID580576Antitrypanosomal activity against Trypanosoma cruzi Y infected in C57BL/6 mouse assessed as mean survival time at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID536025Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y assessed as viability after 11 days by trypan blue exclusion assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID1498175Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID213672Inhibitory activity against Trypanosoma cruzi2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani.
AID1615023Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1683680Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on ALP level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1682935Hepatotoxicity in BALB/c mouse infected with blood trypomastigote form of Trypanosoma cruzi strain Y assessed as ALT level in plasma at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-infection and measured on 16th day pos2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1055183Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for intracellular amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN32013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1613535Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infe2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1188733Cytotoxicity against human HepG2 cells after 48 hrs by2014European journal of medicinal chemistry, Oct-30, Volume: 862-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.
AID1518973Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as decrease in body weight at 30 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured at 150 days post infectio2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1164929Trypanocidal activity against epimastigote forms of Trypanosoma cruzi Punta Lobos after 24 hrs2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1687709Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as increase in body weight at 10 mg/kg, po treated 10 days post infection measured on day 19 (Rvb = -1.8%)2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1720858Cytotoxicity against albino Swiss mouse Peritoneal macrophages in absence of mouse blood incubated for 24 hrs in absence of mouse blood by PrestoBlue dye based fluorescence assay2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Strategies towards potent trypanocidal drugs: Application of Rh-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulation and nitroalkene reactions for the synthesis of substituted quinones and their evaluation against Trypanosoma cruzi.
AID1615107Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1517425Antitrypanosomal activity against Trypanosoma brucei bloodstream form assessed as parasite growth inhibition incubated for 72 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID766417Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1615049Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free bone marrow at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1683669Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as reduction in weight at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured up to 145 days post infection2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID396004Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as parasitemia remaining in hemoculture2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID693342Growth inhibition of epimastigote form of Trypanosoma cruzi CL-B5 at 256 uM after 72 hrs by lacZ reporter gene assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1706435Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigotes infected in rat 3T3 cells assessed as reduction in parasite growth incubated for 48 hrs by chlorophenol red-fl-D-galactopyranoside based colorimetric analysis relative to2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1811309Trypanocidal activity against Trypanosoma cruzi ITRI/MX/2018/TH assessed as inhibition of parasite growth measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID371470Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes after 1 day2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Naphthoquinoidal [1,2,3]-triazole, a new structural moiety active against Trypanosoma cruzi.
AID766420Antiparasitic activity against epimastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition after 72 hrs by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1399453Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigote forms infected in monkey LLC-MK2 cells after 24 hrs by CellTiter-Glo luminescent cell viability assay2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.
AID1498253Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post in2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1854943Induction of cell death in Trypanosoma cruzi Y epimastigotes assessed as late apoptotic cells at 125 uM incubated for 24 hrs by Annexin V/7-AAD staining based flow cytometric analysis (Rvb = 0.12 %)2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1422889Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c epimastigotes infected in African green monkey Vero cells2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID1683698Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in BALB/c mouse assessed as reduction in parasitaemia at 20 mg/kg, po for 5 days and measured after 55 days post infection2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID576084Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Edema at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498197Toxicity in Balb/c mouse assessed as reduction in body mass at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection relative to control2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1603820Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free brain in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1275382Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for epimastigote stage of Trypanosoma cruzi Dm28c2016European journal of medicinal chemistry, Feb-15, Volume: 109New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease.
AID1603768Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa; DTU 5 trypomastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID337144Antitrypanosomal activity against Trypanosoma cruzi M6241CL6 after 48 hrs
AID1351074Cytotoxicity against human U2OS cells assessed as reduction in cell viability2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID265553Antitrypanosomatid activity against Trypanosoma cruzi Tulahuen 2 epimastigote form at 25 uM2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
2H-benzimidazole 1,3-dioxide derivatives: a new family of water-soluble anti-trypanosomatid agents.
AID547509Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG2 at 12 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1615097Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infe2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID577160Toxicity in Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as changes in liver SGOT enzyme levels at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection by hematoxylin-eosin staining2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1422859Antitrypanosomal activity against Trypanosoma cruzi Tulahuen intracellular amastigote harboring beta-galactosidase infected in mouse NIH/3T3 cells after 96 hrs by CPRG reagent based assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.
AID1616173In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily for 5 days with 2 days interval for 3 cycles and measured 9 days post-infec2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1498233Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in lung tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days startin2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID710879Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 24 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID285212Effect on survival in Trypanosoma cruzi Y infected IL12 knock out C57BL/6 mouse Chagas disease model assessed as mean survival time at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID576103Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Diarrhea at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID779137Prodrug conversion assessed as Trypanosoma brucei brucei recombinant his-tagged nitroreductase-mediated NADH oxidization by spectrophotometric analysis2013Bioorganic & 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.
AID1074918Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in BALB/c mouse assessed as reduction in parasite specific antibodies level at 1 mg/kg/day, ip treated from day 5 to day 10 post-infection measured from day 30 to day 120 pos2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1339473Antitrypanosomal activity against Trypanosoma cruzi MHOM/BR/OO/Y trypomastigotes infected in CD1 mouse peritoneal macrophages after 3 days2017Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4
Antiprotozoal glutathione derivatives with flagellar membrane binding activity against T. brucei rhodesiense.
AID666686Selectivity index, ratio of IC50 for mouse J774 cells to IC50 for bloodstream form of Trypanosoma cruzi trypomastigote2012European journal of medicinal chemistry, Aug, Volume: 54Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.
AID1164930Trypanocidal activity against epimastigote forms of Trypanosoma cruzi Queretaro after 24 hrs2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1849826Cytotoxicity against monkey LLC-MK2 cells assessed as reduction in cell viability incubated for 96 hrs by trypan blue assay2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
AID1381715Cytotoxicity against human U2OS cells assessed as decrease in viable cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1379741Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes2017European journal of medicinal chemistry, Nov-10, Volume: 140Synthesis and 2D-QSAR studies of neolignan-based diaryl-tetrahydrofuran and -furan analogues with remarkable activity against Trypanosoma cruzi and assessment of the trypanothione reductase activity.
AID1294227Selectivity index, ratio of LC50 for mouse L929 cells to IC50 for Trypanosoma cruzi CL-B5 lacZ amastigotes in mouse L929 cells2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1639038Antitrypanosomal activity against tdTomato red expressing Trypanosoma cruzi CL amastigotes infected in gamma-irradiated African green monkey Vero cells after 72 hrs by fluorescence assay2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi.
AID1065847Trypanocidal activity against Trypanosoma cruzi Y infected in BALB/c mouse assessed as mouse survival at 100 mg/kg treated from day 2 to day 9 post-infection2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Design, synthesis, and evaluation of hydroxamic acid derivatives as promising agents for the management of Chagas disease.
AID580593Antitrypanosomal activity against Trypanosoma cruzi Y infected in B-lymphocyte knockout C57BL/6 mouse assessed as increase in survival of mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID337143Antitrypanosomal activity against Trypanosoma cruzi MIL4CL10 after 48 hrs
AID1683676Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on LDH level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID396005Antimicrobial activity against Trypanosoma cruzi genotype 19 and genotype 39 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1064594Antiparasitic activity against epimastigote form of Trypanosoma cruzi Y after 96 hrs by hemocytometry2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents.
AID1587055Cytotoxicity against mouse 3T3 cells infected with Trypanosoma cruzi Tulahuen amastigotes assessed as disruption of cell monolayer at 50 times EC50 supplemented with fresh medium containing compound every 4 days for 16 days followed by compound washout an2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID580665Antitrypanosomal activity against Trypanosoma cruzi Y infected in B-lymphocyte knockout C57BL/6 mouse assessed as number of mouse with reactivation of infection at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 22 days post inf2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1603765Trypanocidal activity against Trypanosoma cruzi trypomastigote form infected in African green monkey Vero cells assessed as ratio of infected cells at 50 uM measured after 72 hrs by Giemsa staining based assay relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID213636Effective dose required against Trypanosoma cruzi in bloodstream2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.
AID666683Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse2012European journal of medicinal chemistry, Aug, Volume: 54Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.
AID1498178Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615033Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells assessed as reduction in number of amastigotes per infected cells at log -0.41 to 1.7 after 72 hrs by Giemsa-staining based2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1584762Trypanocidal activity against Trypanosoma cruzi Y strain intracellular amastigotes infected in mouse cardiac cells assessed as parasite death after 168 hrs by Giemsa-staining based assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID378743Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss albino mouse assessed as mortality rate at 100 mg/kg, po daily for 4 days assessed after 6 to 9 days1999Journal of natural products, Feb, Volume: 62, Issue:2
Biological activities of 7-epiclusianone.
AID1238020Selectivity index, ratio of EC50 for BALB/c mouse peritoneal macrophages to EC50 for Leishmania amazonensis MPRO/BR/1972/M1841-LV-79 promastigotes2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1422891Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c amastigotes infected in African green monkey Vero cells2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID1519003Cytotoxicity against African green monkey Vero cells at 0.5 to 20 uM after 72 hrs by propidium iodide staining based flow cytometric analysis2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID564779Antitrypanosomal activity against Trypanosoma cruzi Columbian bloodstream forms infected in C3H mouse assessed as survival of mouse at 100 mg/kg/day, ip administered 5 days postinfection for 10 consecutive days measured after 31 days2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1603878Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum lactate dehydrogenase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting fro2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1686741Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen epimastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID315106Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 amastigotes 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.
AID1518975Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as decrease in body weight at 15 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured at 150 days post infectio2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID576951Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as reduction in parasite specific antibodies at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection measur2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1683660Inhibition of mitochondrial membrane potential in Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) epimastigote form at IC25 concentration after 72 hrs by Rho (FITC-A) staining based flow cytometric analysis2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1055182Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for extracellular trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN32013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1202577Selectivity index, ratio of IC50 for human LL24 cells to IC50 for Trypanosoma cruzi Silvio X10 cl1 epimastigote forms2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1687712Toxicity in C3H mouse infected with Trypanosoma cruzi trypomastigotes assessed as mortality at 10 to 50 mg/kg, po treated 10 days post infection for 7 consecutive days2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID669383Cytotoxicity against Balb/c mouse peritoneal macrophages after 24 hrs by MTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
AID1228672Antileishmanial activity against promastigote stage of Leishmania infantum MHOM/BR/1972/LD assessed as reduction of cell viability after 48 hrs by MTT assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Anti-parasitic Guanidine and Pyrimidine Alkaloids from the Marine Sponge Monanchora arbuscula.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1678868Antitrypanosomal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes assessed as lysis of parasite in absence of mouse blood incubated for 24 hrs by Neubauer chamber method2020RSC medicinal chemistry, Oct-01, Volume: 11, Issue:10
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: redox and biological implications.
AID1854932Selectivity index, ratio of EC50 for Cytotoxicity against monkey LLC-MK2 cells to EC50 for antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in monkey LLC-MK2 cells2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1613485Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells assessed as reduction in infected cells after 72 hrs by Giemsa-staining based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1613567Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID613449Selectivity index, ratio of CC50 for african green monkey COS7 cells to IC50 for intracellular amastigotes form of Trypanosoma cruzi2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID1164937Induction of apoptosis in human platelets assessed as late apoptotic cells after 10 mins using Annexin V/propidium iodide by flow cytometry (Rvb = 0.02 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1422888Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID1587054Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells assessed as relapse time at 12.5 times EC50 supplemented with fresh medium containing compound every 4 days for 16 days followed by compound washout and m2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID1244577Cytotoxicity against BALB/c mouse splenocytes assessed as maximum non-toxic concentration by measuring [3H]-thymidine incorporation after 24 hrs by liquid scintillation counting2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1584731Therapeutic index, ratio EC50 for human MRC5 SV2 cells to EC50 for Trypanosoma cruzi Tulahuen CL2 intracellular amastigotes2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1312164Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y at 25 uM measured after 24 hrs using propidium iodide by neubauer chamber method relative to control2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi.
AID580581Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as increase in survival of mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1613476Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1615061Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post in2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603748Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as reduction in serum Ig-G level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days startin2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1351076Antitrypanosomal activity against Trypanosoma cruzi Y Tc2 amastigotes infected in human U2OS cells up to 200 uM after 72 hrs by Draq5 staining based HCS analysis relative to control2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID426309Antiparasitic activity against Giardia intestinalis IMSS:0696 trophozoites after 48 hrs by Hill culture method2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles.
AID502042Antimicrobial activity against epimastigotes form of Trypanosoma cruzi MHOM/MX/1994/Ninoa after 72 hrs2010Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
Design, synthesis, and in vitro antiprotozoal, antimycobacterial activities of N-{2-[(7-chloroquinolin-4-yl)amino]ethyl}ureas.
AID1603756Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 52019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1074928Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi (IRHOD/CO/2008/SN3) amastigotes2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID563570Toxicity in CH3/He(H-2k) mouse assessed as mortality at cumulative dose of 100 mg/kg, po measured after 48 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID282994Antiparasitic activity against Trypanosoma brucei rhodesiense STIB900 blood stream form2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate.
AID677310Trypanosomicidal activity against Trypanosoma cruzi epimastigotes assessed as change in ethanol metabolite excretion after 96 hrs by NMR analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1383434Selectivity index, ratio of LC50 for Swiss Webster mouse cardiac cells by prestoblue assay to EC50 for bloodstream trypomastigote stage of Trypanosoma cruzi Y measured after 24 hrs2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1264445Cytotoxicity against rat L6 cells after 6 days by resazurin staining based fluorescence plate reader assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID263384Antitrypanosomal activity against Trypanosoma cruzi amastigotes at 1 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID1686723Antitrypanosomal activity against Trypanosoma cruzi infected in African green monkey Vero cells assessed as reduction in number of trypomastigotes measured up to 10 days by Giemsa staining based hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1507437Selectivity index, ratio of LC50 for cytotoxicity against Swiss albino mouse peritoneal macrophages to IC50 for Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Y isolated from parasite infected Albino Swiss mouse2017European journal of medicinal chemistry, Aug-18, Volume: 136Rhodium-catalyzed C-H bond activation for the synthesis of quinonoid compounds: Significant Anti-Trypanosoma cruzi activities and electrochemical studies of functionalized quinones.
AID1398306Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigote forms harboring LacZ infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric method2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates.
AID1381724Inhibition of human microsomal CYP3A4 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
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.
AID1683715Antitrypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 (DTU I) amastigote form infected in Vero cells assessed as parasite growth inhibition incubated for 72 hrs by Giemsa-staining based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID396587Trypanocidal activity against Trypanosoma cruzi CL-B5 clone epimastigotes expressing lacZ gene after 72 hrs at 28 degC2008European journal of medicinal chemistry, Sep, Volume: 43, Issue:9
Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: in silico, in vitro and in vivo activity studies.
AID1699436Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 70 hrs by resazurin dye based inverted microscopic analysis2020Journal of natural products, 11-25, Volume: 83, Issue:11
Pyridine-4(1
AID707775Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in african green monkey Vero cells assessed as inhibition of infection rate at IC25 level 0.5 to 10 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1603759Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 amastigote forms measured after 72 hrs by Giemsa staining based assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1686743Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen promastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1854957Induction of mitochondrial membrane potential loss in Trypanosoma cruzi Y epimastigotes at 125 uM incubated for 24 hrs by Rhodamine 123 staining based flow cytometric analysis relative to control2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1603862Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum uric acid level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 70 pos2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
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.
AID1277387Antiparasitic activity against Trypanosoma cruzi Tulahuen trypomastigotes infected in rat L6 cells using chromogenic substrate beta-D-galactopyranoside after 96 hrs by beta-galactosidase assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Highly improved antiparasitic activity after introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors.
AID1184290Selectivity index, ratio of IC50 for human U2OS cells to IC50 for intracellular Trypanosoma cruzi2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a]benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi.
AID1603760Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi MHOM/Pe/2011/Arequipa; DTU 5 isolated from parasite infected BALB/c Albino mouse cardiac cells after 24 hrs by Neubauer chamber based cell counting method2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID576077Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of agranulocytosis after 2nd week of treatment2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1198733Cytotoxicity against human U937 cells assessed as cell viability after 72 hrs by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93An efficient synthesis of new caffeine-based chalcones, pyrazolines and pyrazolo[3,4-b][1,4]diazepines as potential antimalarial, antitrypanosomal and antileishmanial agents.
AID1678865Antitrypanosomal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes assessed as lysis of parasite in presence of 5 % mouse blood incubated for 24 hrs by Neubauer chamber method2020RSC medicinal chemistry, Oct-01, Volume: 11, Issue:10
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: redox and biological implications.
AID1498171Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes after 48 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID669300Cytotoxicity against monkey LLC-MK2 cells after 96 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID576094Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Arthritis at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1294224Cytotoxicity against mouse L929 cells after 48 hrs by resazurin assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID576099Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Dysphagia at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID341604Antimicrobial activity against Giardia duodenalis WB2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1690286Antitrypanosomal activity against Trypanosoma cruzi CL amastigotes overexpressing tdTomato red fluorescent protein infected in gamma-irradiated African green monkey Vero cells assessed as reduction in parasite growth measured 3 days post-infection by fluo2020European journal of medicinal chemistry, Apr-01, Volume: 191Synthesis and in vitro evaluation of new 5-substituted 6-nitroimidazooxazoles as antikinetoplastid agents.
AID1603841Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum alkaline phosphatase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1498242Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in lung tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days startin2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1519008Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as reduction in skeletal tissue inflammation at 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infect2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1483952Antiprotozoal activity against trypomastigote stage of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells using preincubated for 96 hrs by CPRG/Nonidet-based inverted microscopy2017Journal of natural products, 02-24, Volume: 80, Issue:2
Dioncophyllines C
AID1616179Toxicity in Swiss Webster mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as body weight loss at 100 mg/kg, po administered once daily for 5 days with 2 days interval for 3 cycles2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID303263Antiparasitic activity against Trypanosoma cruzi Tulahuen T4 in amastigotes 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.
AID1064591Cytotoxicity against monkey LLC-MK2 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents.
AID1470756Trypanocidal activity against bloodstream form of Trypanosoma cruzi INC-5 infected in NIH mouse assessed as reduction in parasitemia at 100 mg/kg, po measured up to 6 hrs post dose by microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1780972Trypanocidal activity against Trypanosoma cruzi CL-Luc-Neon amastigotes infected in BSR cells assessed as inhibition of parasite growth at 20 times IC50 incubated for 20 days measured after 10 days of compound wash out by epifluorescence microscopy analys2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1608338Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes after 24 hrs2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis of quinones with highlighted biological applications: A critical update on the strategies towards bioactive compounds with emphasis on lapachones.
AID1238027Anti-trypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth inhibition incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1615045Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free muscle at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection foll2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID580575Antitrypanosomal activity against Trypanosoma cruzi Y infected in C57BL/6 mouse assessed as increase in survival of mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1584759Antiparasitic activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes infected in Swiss Webster mouse assessed as protection against parasite-induced mortality at 25 mg/kg, po bid via gavage administered for 5 consecutive days starting fro2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1508579Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Balb/c mouse assessed as reduction in blood parasitaemia at 100 mg/kg, po qd administered for 5 consecutive days starting from day 5 post infection measu2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1508581Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Balb/c mouse assessed as reduction in blood parasitaemia at 100 mg/kg, po qd administered for 5 consecutive days starting from day 5 post infection measu2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1486935Antiprotozoal activity against Leishmania mexicana MHOM/MX/ISETGS incubated for 72 hrs by Neubauer chamber based cell counting method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID548281Antimicrobial activity against Trypanosoma brucei NfxR12010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID547247Toxicity in mongrel dog infected with Trypanosoma cruzi Y assessed as weight loss at 12 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 6 months2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1615021Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1294226Selectivity index, ratio of LC50 for mouse L929 cells to IC50 for Trypanosoma cruzi CL-B5 lacZ epimastigotes in mouse L929 cells2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1615052Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free heart at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1851972Solubility of compound in water at 0.1 M HCl at pH 1 by LC-UV analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1321005Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Y infected in human U2OS cells after 96 hrs by Draq5 staining-based high content screening assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.
AID1686746Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi NS3 promastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1074924Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in African green monkey Vero cells assessed as reduction in infection rate at IC25 treated for 12 hrs followed by compound-washout measured after 10 days by microscopic analy2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1723649Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Expanding the scope of synthetic 1,2,4-trioxanes towards Trypanosoma cruzi and Leishmania donovani.
AID1403390Cytotoxicity activity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by cell-titer-glo assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID766423Selectivity index, ratio of LC50 for mouse NCTC-929 cells to IC50 for epimastigotes of Trypanosoma cruzi CL Brener2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID213643The compound was evaluated for its inhibitory activity against Trypanosoma cruzi2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Squalamine analogues as potential anti-trypanosomal and anti-leishmanial compounds.
AID669384Selectivity index, ratio of IC50 for Balb/c mouse peritoneal macrophages to IC50 for epimastigotes of Trypanosoma cruzi2012Journal of natural products, May-25, Volume: 75, Issue:5
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
AID1706437Selectivity index, ratio of IC50 for cytotoxicity against rat 3T3 cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigotes infected in rat 3T3 cells2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1653747Selectivity 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 Trypanosoma cruzi Tulahuen C4 trypomastigotes infected in rat L6 cells assessed a2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID1615099Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infect2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1613561Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID593266Antiparasitic activity against Trypanosoma cruzi amastigotes infected in gamma-irradiated vero cells assessed as growth inhibition by fluorescence assay2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Synthesis and biological evaluation of new 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase.
AID1403402Trypanocidal activity against Trypanosoma cruzi CL trypomastigotes infected in monkey LLC-MK2 cells after 24 hrs by luminescent assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1624261Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 harboring beta-galactosidase infected in human MRC5 cells after 7 days by resazurin dye-based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID756893Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID766416Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 0.5 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1686729Antitrypanosomal activity against Trypanosoma cruzi Arequipa amastigote forms infected in African green monkey Vero cells incubated for 72 hrs by Giemsa staining based micrscopy2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1070009Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 16 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1055181Trypanocidal activity against amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as inhibition of parasite infection rate at IC25 preincubated for 12 hrs followed by compound washout measured after 2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1603864Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum creatine kinase muscle to brain ratio level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1682936Renal toxicity in BALB/c mouse infected with blood trypomastigote form of Trypanosoma cruzi strain Y assessed as creatinine level in plasma at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-infection and measured on 16th 2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1198533Trypanocidal activity against GFP expressing Trypanosoma cruzi Y C57BL/6J mouse acute model of trypanosomal infection assessed as reduction in parasitemia at 100 mg/kg/day, ip measured at 10,14 and 20 days post infection2015European journal of medicinal chemistry, Mar-26, Volume: 93Computer-guided drug repurposing: identification of trypanocidal activity of clofazimine, benidipine and saquinavir.
AID1403406Trypanocidal activity against Trypanosoma cruzi Dm28c intracellular amastigotes infected in African green monkey Vero cells after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID576090Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Weakness at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1720857Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Albino Swiss mouse assessed as lysis of parasite in absence of mouse blood incubated for 24 hrs by Neubauer chamber method2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Strategies towards potent trypanocidal drugs: Application of Rh-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulation and nitroalkene reactions for the synthesis of substituted quinones and their evaluation against Trypanosoma cruzi.
AID1498263Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in urea level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 122018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1462701Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 intracellular amastigotes infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Lead selection of antiparasitic compounds from a focused library of benzenesulfonyl derivatives of heterocycles.
AID356388Antitrypanosomal activity against Trypanosoma cruzi2003Journal 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.
AID1054899Cytotoxicity against mouse NCTC-929 cells assessed as reduction of cell viability after 24 hrs by resazurin dye-based fluorometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
In vitro and in vivo antileishmanial and trypanocidal studies of new N-benzene- and N-naphthalenesulfonamide derivatives.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1124787Safety index, ratio of IC50 for human HepG2 cells to IC50 for epimastigote stage of Trypanosoma brucei 29-132014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1074927Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi (IRHOD/CO/2008/SN3) epimastigotes2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1683710Antitrypanosomal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen (DTU VI) blood stream trypomastigote form assessed as parasite growth inhibition incubated for 24 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID396582Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Pyrimido[1,2-a]quinoxaline 6-oxide and phenazine 5,10-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi.
AID1140926Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Sylvio X-10 amastigotes2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.
AID1275387Toxicity in acute chagas BALB/c mouse model infected with trypomastigotes stage of Trypanosoma cruzi strain CL Brener assessed as mortality at 50 mg/kg/day, po administered for 14 days started on day 9 post infection measured at 30 to 60 days2016European journal of medicinal chemistry, Feb-15, Volume: 109New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease.
AID1578093Antitrypanosomal activity against Trypanosoma cruzi2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1755138Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse NIH/3T3 cells assessed as parasite growth inhibition incubated for 4 days in glucose rich DMEM medium2021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Synthesis, biochemical, and biological evaluation of C2 linkage derivatives of amino sugars, inhibitors of glucokinase from Trypanosoma cruzi.
AID1124785Safety index, ratio of IC50 for human HepG2 cells to IC50 for procyclic stage of Trypanosoma brucei 4272014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1615102Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 81 pos2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1498327Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1493588Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigote forms infected in human U937 cells after 72 hrs by beta-galactosidase reporter gene assay
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
AID1603840Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum total bilirubin level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID335550Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 containing galactosidase gene in rat L6 cells after 4 days2002Journal of natural products, Aug, Volume: 65, Issue:8
Ancistrocongolines A-D, new naphthylisoquinoline alkaloids from ancistrocladus congolensis.
AID1686738Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Arequipa epimastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1154399Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Y in BALB/c mouse peritoneal macrophages assessed as reduction of number of intracellular parasites per 100 cells after 4 days by hematoxylin/eosin staining-based optical microscopic 2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
AID710877Cytotoxicity against BALB/c mouse splenocytes assessed as highest nontoxic concentration by measuring [3H]-thymidine incorporation after 24 hrs by beta-radiation counting2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID1603866Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum aspartate aminotransferase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days startin2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1669166Selectivity index, ratio of EC50 for cytotoxicity against rat H9C2 cells to EC50 for antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in rat H9C2 cells2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from
AID1432288Trypanocidal activity against Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells after 48 hrs2017European journal of medicinal chemistry, Mar-10, Volume: 128Design and synthesis of a new series of 3,5-disubstituted isoxazoles active against Trypanosoma cruzi and Leishmania amazonensis.
AID1846641Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 trypomastigote expressing beta-galactosidase infected in rat L6 cells assessed as parasite growth inhibition measured after 96 hrs in presence of CPRG/Nonidet by inverted microscopy2021Journal 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.
AID1498174Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID707766Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in BALB/c mouse model of acute Chagas disease assessed as reduction parasitemia at 5 mg/kg/day, ip administered for 5 consecutive days starting on day 7 post i2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1498279Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in uric acid level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on d2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1687713Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as physically healthy with shiny appearance at 10 mg/kg, po treated 10 days post infection measured on day 192020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID396007Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as parasitemia remaining by ELISA2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID464871Antiparasitic activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.
AID1613466Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes after 48 to 72 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1603883Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum total bilirubin level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1633352Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes resazurin dye based assay
AID344434Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.5 mM after 24 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1498234Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in muscle tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days start2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID392015Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected Swiss mouse assessed as prevention of muscle inflammatory infiltrates at 200 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID764117Selectivity index, ratio of IC50 for human FN1 fibroblasts to IC50 for epimastigotes of Trypanosoma cruzi Y2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
5-Nitro-2-furfuriliden derivatives as potential anti-Trypanosoma cruzi agents: design, synthesis, bioactivity evaluation, cytotoxicity and exploratory data analysis.
AID1070003Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1518974Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as decrease in body weight at 30 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured at 150 days post infectio2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1613479Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID693360Growth inhibition of epimastigote form of Trypanosoma cruzi CL-B5 after 72 hrs by lacZ reporter gene assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1061028Antimicrobial activity against Trypanosoma cruzi2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
AID1070014Antimicrobial activity against epimastigote stage of Trypanosoma cruzi CL Brener assessed as growth inhibition after 72 hrs by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1191155Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents.
AID756892Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahuen C2C42013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.
AID1518968Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as change in QRS morphology at 30 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measured 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID547245Toxicity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as weight loss at 12 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID580577Antitrypanosomal activity against Trypanosoma cruzi Y infected in C57BL/6 mouse assessed as cure rate in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1062787Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 infected in Swiss mouse assessed as mouse survival at 100 mg/kg, po qd administered on day 8 post-infection measured on same day by microscopic analysis2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
AID1766958Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite growth inhibition by resazurin assay
AID1498194Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 up to 0.5 mg/ml in presence of S9 fraction by SOS/umu assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID764120Selectivity index, ratio of IC50 for mouse J774 cells to IC50 for epimastigotes of Trypanosoma cruzi Y2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
5-Nitro-2-furfuriliden derivatives as potential anti-Trypanosoma cruzi agents: design, synthesis, bioactivity evaluation, cytotoxicity and exploratory data analysis.
AID1254442Antiparasitic activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction of parasitemia at 100 mg/kg, po qd administered for 5 days measured on day 10 post infection relative to vehicle-treated 2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1498276Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in uric acid level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID563565Cytotoxicity against Swiss-Webster mouse assessed as effect on creatine kinase at 100 mg/kg/day measured after 14 days postinfection2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1501885Selectivity index, ratio of IC50 for mouse NCTC-929 cells to IC50 for Trypanosoma cruzi Y trypomastigotes2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID1686739Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Arequipa amastigotes forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID396009Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as parasitemia remaining by FC-ALTA2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1501891Antitrypanosomal activity against Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction in blood parasitemia at 100 mg/kg, po administered every day starting on day 5 post infection measured on day 8 post infection2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID1294228Antichagasic activity against Trypanosoma cruzi Tulahuen amastigotes in mouse L929 cells assessed as growth inhibition after 96 hrs by beta galactosidase reporter gene assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1699435Growth inhibition of amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells assessed as reduction in parasitic growth incubated for 96 hra by CPRG/Nonidet reagent based inverted microscopic analysis2020Journal of natural products, 11-25, Volume: 83, Issue:11
Pyridine-4(1
AID710881Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction of blood parasite level at 250 umol/kg, po qd for 5 days2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID1498295Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 16 post 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1062983Trypanocidal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse L929 cells assessed as parasite growth inhibition after 7 days by beta-galactosidase assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of the antiparasitic activity of bis-(arylmethylidene) cycloalkanones.
AID1202572Anti-trypanosomal activity against Trypanosoma cruzi Y epimastigote forms assessed as inhibition of parasite growth after 72 hrs by microplate reader based assay2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID274746Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 trypomastigotes in L6 cells2007Journal of natural products, Jan, Volume: 70, Issue:1
Limonoid orthoacetates and antiprotozoal compounds from the roots of Pseudocedrela kotschyi.
AID1074382Antitrypanosomal activity against epimastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as parasite growth inhibition after 72 hrs by Neubauer hemocytometric chamber analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID1498285Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID547270Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG2 at 12 mg/kg, po BID for 90 days measured up to 30 days by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1155753Trypanocidal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes infected in rat L6 cells after 4 days2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.
AID564778Antitrypanosomal activity against Trypanosoma cruzi Columbian bloodstream forms infected in C3H mouse assessed as decrease in parasite load at 100 mg/kg/day, ip administered 5 days postinfection for 10 consecutive days measured after 31 days2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1487117Cytotoxicity against mouse J774 cells incubated for 24 hrs by resazurin dye based fluorescence assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and biological evaluation of 2-methyl-1H-benzimidazole-5-carbohydrazides derivatives as modifiers of redox homeostasis of Trypanosoma cruzi.
AID564745Toxicity in female Swiss-Webster mouse assessed as mortality at cumulative dose of 200 mg/kg, ip measured after 48 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1615115Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1849825Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y amastigotes infected in monkey LLC-MK2 cells assessed as parasite growth inhibition incubated for 5 days by Neubauer hemocytometer based fluorescence spectrophotometer method2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
AID563562Antitrypanosomal activity against Trypanosoma cruzi Y bloodstream forms infected in Swiss-Webster mouse assessed as decrease in parasite load at 100 mg/kg/day, po administered 5 days postinfection for 10 alternate days measured after 31 days2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID762754Cytotoxicity against C57BL/6 mouse spleen cells after 24 hrs using propidium iodide by flow cytometry2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Molecular design, synthesis and biological evaluation of 1,4-dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity.
AID214467Compound was evaluated for anti-parasitic activity against Trypanosoma cruzi2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
AID1603829Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free spleen in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID564764Antitrypanosomal activity against Trypanosoma cruzi Columbian bloodstream forms infected in C3H mouse assessed as decrease in parasite load at 100 mg/kg/day, ip administered 21 days postinfection measured on day 462010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1548466Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom
AID1278151Cytotoxicity against mouse NCTC-929 cells assessed as cell viability after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.
AID1578097Antitrypanosomal activity against Leishmania donovani2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1254437Selectivity index, ratio of CC50 for human J774 cells to IC50 for bloodstream trypomastigote stage of Trypanosoma cruzi Y2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID576832Antitrypanosomal activity against Trypanosoma cruzi infected in african green monkey Vero cells assessed as reduction of amastigote number per infected cell at IC25 after 10 days relative to control2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1686736Antitrypanosomal activity against Trypanosoma cruzi SN3 trypomastigote froms infected in mouse blood incubated for 24 hrs by Neubauer chamber based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1062982Cytotoxicity against mouse L929 cells after 96 hrs by Alamar blue assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of the antiparasitic activity of bis-(arylmethylidene) cycloalkanones.
AID576083Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Palmar-plantar rash at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID392014Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected Swiss mouse assessed as prevention of heart inflammatory infiltrates at 200 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID249624Percentage delyse against amastigote forms of Y strain of Trypanosoma cruzi at 2 uM2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
AID1355404Antiprotozoal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by CPRG/Nonidet-based photometric method2018Journal of natural products, 06-22, Volume: 81, Issue:6
Phytochemical Study of Salvia leriifolia Roots: Rearranged Abietane Diterpenoids with Antiprotozoal Activity.
AID1361363Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood assessed as reduction in parasite lysis after 24 hrs by optical microscopic method2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.
AID1683717Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in Vero cells assessed as parasite growth inhibition incubated for 72 hrs by Giemsa-staining based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1615109Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID229349Ratio of inhibitory concentration to that of reference drug was determined2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds.
AID707762Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in BALB/c mouse model of chronic Chagas disease subjected to 3 cycles of immunosuppression with 50 mg/kg cyclophosphamide monohydrate for 3 consecutive weeks a2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID564080Antitrypanosomal activity against Trypanosoma cruzi 956 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1381726Cytotoxicity against human WI38 cells after 48 hrs by CellTiter-Glo assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1245596Toxicity in Balb/c mouse at 13 mg/kg/day, ip2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID344431Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.5 mM after 4 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID613445Trypanocidal activity against bloodstream trypomastigote form of Trypanosoma cruzi after 24 hrs2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID564765Hepatotoxicity in Swiss-Webster mouse assessed as effect on GPT level at 25 mg/kg/day, ip administered 21 days postinfection measured on day 1202010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID266614Antitrypanosomal activity against Trypanosoma cruzi2006Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14
Design, synthesis and evaluation of novel uracil amino acid conjugates for the inhibition of Trypanosoma cruzi dUTPase.
AID1329378Antileishmanial activity against Leishmania infantum MHOM/BR/1972/LD amastigote forms infected in BALB/c mouse peritoneal macrophages assessed as reduction in parasite viability after 120 hrs by giemsa staining based light microscopy2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID1519002Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as effect on heart rate duration at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection an2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1459246Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as effect on parasite motility at 1 to 15 uM supplemented with fresh medium containing compound every 9 to 10 days measured on third week2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID1351073Antitrypanosomal activity against Trypanosoma cruzi Y Tc2 amastigotes infected in human U2OS cells after 72 hrs by Draq5 staining based HCS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID1202573Anti-trypanosomal activity against Trypanosoma cruzi Silvio X10 cl1 epimastigote forms assessed as inhibition of parasite growth after 72 hrs by microplate reader based assay2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1603737Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free adipose tissue in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting fr2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1238028Selectivity index, ratio of EC50 for BALB/c mouse peritoneal macrophages to EC50 for Trypanosoma cruzi Y epimastigotes2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1584758Antiparasitic activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes infected in Swiss Webster mouse assessed as decrease in parasitemia at 100 mg/kg, po sid via gavage administered for 5 consecutive days measured at day 8 post infection 2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1140993Antitrypanosomal activity against Trypanosoma cruzi CL Brener infected in BALB/c mouse assessed as peak of maximum parasitemia at 192 umol/kg/day, po for 14 days administered in saline and tween 80 measured up to 60 days relative to control2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.
AID1603948Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as reduction in serum Ig-G level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days startin2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1565132Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for intracellular amastigote stage of luciferase expressing Trypanosoma cruzi Dm28c infected in Vero cells2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1275388Antitrypanosomal activity against trypomastigotes stage of Trypanosoma cruzi strain CL Brener infected in acute chagas BALB/c mouse model assessed as survival rate at 50 mg/kg/day, po administered for 14 days started on day 9 post infection measured at 302016European journal of medicinal chemistry, Feb-15, Volume: 109New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease.
AID1074926Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi (IRHOD/CO/2008/SN3) trypomastigotes2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID728171Cytotoxicity against mouse NIH/3T3 cells2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID632297Antitrypanosomal activity against blood stream form of Trypanosoma cruzi Tulahuen C4 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.
AID1612897Selectivity index, ratio of CC50 for human U2OS cells to EC50 for Trypanosoma cruzi Y infected in human U2OS cells2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of new potent hits against intracellular Trypanosoma cruzi by QSAR-based virtual screening.
AID582595Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C2C4 trypomastigote after 48 hrs2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.
AID1612898Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 96 hrs2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of new potent hits against intracellular Trypanosoma cruzi by QSAR-based virtual screening.
AID548110Antiparasitic activity against Trypanosoma cruzi T2 epimastigotes assessed as growth inhibition at 25 uM after 5 days2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
AID1181597Antimicrobial activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by microscopic analysis2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei.
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]
AID1683714Antitrypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 (DTU I) epimastigote form assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1381692Antileishmanial activity against Leishmania infantum amastigote form after 72 hrs by steady-Glo reagent based assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1615043Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free heart at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1486938Cytotoxicity against African green monkey Vero cells incubated for 24 to 48 hrs by SRB assay2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID1615055Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free spleen at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection foll2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID677214Trypanosomicidal activity against Trypanosoma cruzi infected in Vero cells assessed as reduction in trypomastigotes in culture medium after 10 days by Giemsa staining method2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
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.
AID1415707Octanol/water partition coefficient, log P of the compound2017MedChemComm, May-01, Volume: 8, Issue:5
Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.
AID1498330Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID728170Selectivity index, ratio of EC50 for mouse NIH/3T3 cells to EC50 for Trypanosoma cruzi trypomastigote2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID1616182Cytotoxicity against Swiss mouse primary cardiac cells assessed as reduction in cell viability incubated for 24 hrs by PrestoBlue dye based colorimetry2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID576939Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as mouse mortality at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1399455Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigote forms infected in rat H9c2 cells assessed as reduction in infected cells after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.
AID1498273Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in uric acid level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on d2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1517428Antitrypanosomal activity against Trypanosoma cruzi strain Y trypomastigotes infected in human HG39 cells by TaqMan probe based RT-PCR analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
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.
AID564744Toxicity in CH3/He(H-2k) mouse assessed as mortality at cumulative dose of 200 mg/kg, ip measured after 48 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID392010Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected Swiss mouse assessed as reduction in circulating trypomastigotes antibody level at 200 mg/kg/day, po after 90 days postinfection2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1686742Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID707774Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in african green monkey Vero cells assessed as inhibition of intracellular amastigotes replication at IC25 level 0.5 to 10 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1603821Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free brain in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1381721Inhibition of human microsomal CYP2C9 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID564078Antitrypanosomal activity against Trypanosoma cruzi 855 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID547273Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG at 7 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID445551Antitrypanosomal activity against Trypanosoma cruzi CL Brener epimastigotes assessed as parasite viability after 5 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Anti-trypanosomatid benzofuroxans and deoxygenated analogues: synthesis using polymer-supported triphenylphosphine, biological evaluation and mechanism of action studies.
AID1613469Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes after 48 to 72 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1312166Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi CA-I/72 infected in mouse C2C12 cells at 10 uM measured after 3 days by DAPI staining-based assay relative to control2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi.
AID1381719Inhibition of human ERG incubated for 2 hrs by fluorescence polarisation assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1498290Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infe2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1164935Induction of apoptosis in human platelets assessed as viable cells after 10 mins using Annexin V/propidium iodide by flow cytometry (Rvb = 89.61 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1683671Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as reduction in survival at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured up to 145 days post infection2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID753403Cytotoxicity against peritoneal macrophage after 24 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID1507197Cytotoxicity against mouse NCTC-929 cells assessed as reduction in cell viability after 48 hrs by resazurin dye-based assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID1498300Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 81 pos2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID623721Trypanocidal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen expressing beta-galactosidase infected in mouse L929 cells after 7 days by microplate reader analysis2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds.
AID660266Trypanocidal activity against bloodstream form of Trypanosoma cruzi Y isolated from albino mouse blood after 24 hrs by neubauer chamber analysis2012European journal of medicinal chemistry, Jun, Volume: 52On the search for potential anti-Trypanosoma cruzi drugs: synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactions.
AID1603738Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free adipose tissue in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1615116Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603752Cytotoxicity against African green monkey Vero cells measured after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID656218Cytotoxicity against african green monkey Vero cells after 3 days2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Phosphonium lipocations as antiparasitic agents.
AID1272503Trypanocidal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes after 5 days2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity.
AID575883Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of hypersensitivity on day 7 to 102010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498173Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1498320Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1439208Selectivity index, ratio of CC50 for human U2OS cells to EC50 for Trypanosoma cruzi Y amastigote forms infected in human U2OS cells2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols.
AID575885Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of myalgias2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1683673Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on total bilirubin level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treat2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1811310Cytotoxicity against mouse J774.2 cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based assay2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID547278Antitrypanosomal activity against Trypanosoma cruzi Y infected in mongrel dog assessed as reduction in IL10 production in right atrium at 12 mg/kg, po BID after 180 days by semiquantitative RT-PCR2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1074930Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) trypomastigotes infected in Balb/c albino mouse after 24 hrs by Neubauer chamber counting analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1501230Antiprotozoal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by CPRG/Nonidet-based inverted microscopy2017Journal of natural products, 09-22, Volume: 80, Issue:9
Antiprotozoal Linear Furanosesterterpenoids from the Marine Sponge Ircinia oros.
AID632303Ratio of benznidazole IC50 to compound IC50 for Trypanosoma cruzi Tulahuen C4 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.
AID727320Antiparasitic activity against Trypanosoma cruzi Tulahuen C2C4 expressing beta-galactosidase infected in rat L6 cells after 96 hrs2013Journal 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.
AID1592301Antitrypanosomal activity against Trypanosoma cruzi MHOM/MX/1994/INC5 epimastigotes assessed as metabolic inhibition at 10 ug/ml after 24 hrs by MTT assay relative to control
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1683709Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID576081Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Petechial rash at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID597248Antitrypanosomal activity against Trypanosoma cruzi CL Brener clone infected in BALB/c mouse assessed as reduction of microbial antibody level at 50 mg/kg/day, po after 90 days by Wilconxon test2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.
AID1508585Toxicity in Balb/c mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as behavioral alteration at 100 mg/kg, po qd administered for 5 consecutive days starting from day 5 post infection2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID580587Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as increase in survival of mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1383428Selectivity index, ratio of LC50 for mouse L929 cells by Alamarblue assay to EC50 for Trypanosoma cruzi Tulahuen trypomastigote forms2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1061026Antimicrobial activity against Trypanosoma cruzi CL amastigotes infected in african green monkey Vero cells measured on day 3 by fluorescence assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
New insights into molecular recognition of 1,1-bisphosphonic acids by farnesyl diphosphate synthase.
AID1683693Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in BALB/c mouse assessed as parasite free organ tissue ratio at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured u2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1503431Antitrypanosomal activity against Trypanosoma cruzi Tulahuen intracellular amastigotes transfected with beta-galactosidase infected in human U937 cells incubated for 72 hrs by spectrophotometry2017European journal of medicinal chemistry, Dec-01, Volume: 141Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities.
AID1383439Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Swiss Webster mouse assessed as mouse survival at 100 mg/kg, po administered daily on day 5 to 9 measured daily until 30 days post dose relative to contr2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1683679Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on urea level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1517443Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi Y infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID337140Antitrypanosomal activity against Trypanosoma cruzi 13379 CL8 after 48 hrs
AID1055168Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as lymphocytic infiltration in portal tracts at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light 2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID580588Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as mean survival time at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID344427Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.1 mM after 1 hr by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID596810Antitrypanosomal activity against metacyclic forms of Trypanosoma cruzi infected in vero cells assessed as decrease in trypomastigotes at IC25 concentration after 12 hrs2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID1854933Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth inhibition measured after 24 hrs by hemocytometer chamber based analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID362800Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 in rat L6 cells2008Journal of natural products, Sep, Volume: 71, Issue:9
Antiprotozoal activities of heterocyclic-substituted xanthones from the marine-derived fungus Chaetomium sp.
AID1234671Antiparasitic activity against Trypanosoma cruzi strain CL Brener epimastigotes after 12 days by ELISA reader2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Enzymatic synthesis of bile acid derivatives and biological evaluation against Trypanosoma cruzi.
AID1329376Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigote forms infected in monkey LLC-MK2 cells assessed as reduction in parasite viability after 24 hrs by resazurin assay2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID690544Antiprotozoal activity against intracellular Trypanosoma cruzi amastigotes in rat L6 cells2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
2-Alkynoic fatty acids inhibit topoisomerase IB from Leishmania donovani.
AID1603757Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 12019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1381713Cytotoxicity against human THP1 cells assessed as decrease in viable cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID576082Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Itching at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID564076Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
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]
AID726228Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 128 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
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).
AID1613547Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID337149Antitrypanosomal activity against Trypanosoma cruzi R107 after 48 hrs
AID1682938Antitrypanosomal activity against blood trypomastigote form of Trypanosoma cruzi strain Y infected in BALB/c mouse assessed as reduction in amastigote nest in host heart at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-i2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID669298Antitrypanosomal activity against Trypanosoma cruzi Y trymastigotes infected in monkey LLC-MK2 cells after 24 hrs by Brenner counter method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID447814Cytotoxicity against BALB/c mouse splenocytes after 24 hrs by [3H]thymidine incorporation assay2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Ruthenium complexes endowed with potent anti-Trypanosoma cruzi activity: Synthesis, biological characterization and structure-activity relationships.
AID1070005Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 1 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1501897Antitrypanosomal activity against Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction in blood parasitemia at 100 mg/kg/day, ip dosed administered for 10 consecutive days starting on day 5 post infection measured on day 14 post infection re2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID1432599Cytotoxicity against mouse L929 cells after 96 hrs by alamar blue assay2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Synthesis and biological evaluation of potential inhibitors of the cysteine proteases cruzain and rhodesain designed by molecular simplification.
AID1124784Antimicrobial activity against procyclic stage of Trypanosoma brucei 427 after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1868691Antitrypanosomal activity against nifurtimox-sensitive Tulahuen CL2 amastigotes expressing beta galactosidase infected in human MRC5 cells assessed as inhibition of parasite growth using chlorophenol red beta-D-galactopyranoside as substrate and measured 2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID1682933Reduction in inflammatory cell infiltration in heart of BALB/c mouse infected with blood trypomastigote form of Trypanosoma cruzi strain Y at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-infection and measured on 16th d2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID344440Aqueous solubility at pH 6.52008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1171005Effect on lipid composition in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells at 5 uM incubated for 24 hrs by GC-MS method2014Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.
AID1706436Inhibition of Trypanosoma cruzi Tulahuen C4 strain CYP51 expressed in Escherichia coli by fluorescence based assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1565126Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by measuring ATP level after 72 hrs by Celltiter-Glo assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1603949Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on glycerol excretion at IC50 after 72 hrs by H NMR method relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1706433Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigotes infected in rat 3T3 cells assessed as reduction in parasite growth incubated for 48 hrs by chlorophenol red-fl-D-galactopyranoside based colorimetric analysis2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1667421Antitrypanosomal activity against Trypanosoma cruzi2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Discovery of 4-((1-(1H-imidazol-2-yl)alkoxy)methyl)pyridines as a new class of Trypanosoma cruzi growth inhibitors.
AID1067358Antimicrobial activity against epimastigote stage of Trypanosoma cruzi MHOM/MX/1994/Ninoa clinical isolate after 72 hrs by Neubauer chamber analysis2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.
AID1140925Antitrypanosomal activity against Trypanosoma cruzi Sylvio X-10 amastigotes infected in African green monkey Vero cells assessed as eradication of amastigotes after 72 hrs by Giemsa staining-based assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.
AID1281413Trypanocidal activity against epimastigote form of Trypanosoma cruzi Dm28c after 11 days by neubauer chamber method2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID1400237Cytotoxicity against human THP1 cells after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Synthesis and SAR of new isoxazole-triazole bis-heterocyclic compounds as analogues of natural lignans with antiparasitic activity.
AID1615100Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 16 post 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1498282Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in uric acid level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on d2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1519004Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as reduction in parasite burden in blood at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infe2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID580582Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as mean survival time at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1055144Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as interstitial hemorrhage at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light microscopic analys2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1615037Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 p2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID726611Inhibition of Trypanosoma cruzi farnesyl diphosphate synthase assessed as incorporation of [4-14C]IPP measured at 37 degC2013European journal of medicinal chemistry, Feb, Volume: 60Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.
AID1546272Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells incubated for 7 days by chlorophenol red beta-D-galactopyranoside substrate based spectrophotometric assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Structure-activity relationship of 4-azaindole-2-piperidine derivatives as agents against Trypanosoma cruzi.
AID1278148Antiparasitic activity against amastigote stage of Trypanosoma cruzi Y2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.
AID1615063Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured o2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID285208Mortality rate in Trypanosoma cruzi Y infected IFN-gamma knock out C57BL/6 mouse Chagas disease model at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1569970Cytotoxicity against Balb/c mouse splenocyte assessed as reduction in cell viability after 24 hrs by [3H]thymidine incorporation based beta scintillation counting analysis2019European journal of medicinal chemistry, Oct-15, Volume: 1802-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity.
AID1174783Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN32015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1633357Selectivity index, ratio of CC50 for mouse RAW264.7 cells to IC50 for Trypanosoma cruzi Y epimastigotes
AID710595Antitrypanosomal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells assessed as growth inhibition after 92 hrs by inverted microscopy2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID762346Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes infected in rat L6 cells after 96 hrs by beta-galactosidase reporter gene 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.
AID1498292Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infect2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID564079Antitrypanosomal activity against Trypanosoma cruzi 875 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1603869Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum total bilirubin level in chronic phase at 20 mg/kg/day administered for 5 consecutive days starting from day 76 p2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1633351Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes after 48 hrs by resazurin dye based assay
AID344441Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss mouse assessed as survivality at 385 umol/kg, po after 15 consecutive days2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1055187Trypanocidal activity against intracellular amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells after 72 hrs by Giemsa staining assay2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1615062Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured o2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID337135Antitrypanosomal activity against Trypanosoma cruzi Z2 after 48 hrs
AID1164931Induction of apoptosis in human monocytes assessed as viable cells using Annexin V/propidium iodide by flow cytometry (Rvb = 97.53 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1739884Antitrypanosomal activity against Trypanosoma cruzi (MHOM/CH/00/Tulahuen C2, lacZ) amastigotes infected in HFF-1 cells assessed as reduction in parasite growth at 150 uM incubated for 120 hrs by CPRG/Igepal substrate based photometric method relative to c2020European journal of medicinal chemistry, Sep-01, Volume: 201Discovery of highly potent and selective antiparasitic new oxadiazole and hydroxy-oxindole small molecule hybrids.
AID1236979Induction of reactive oxygen species formation in human HT1080 cells at 10 to 50 M by fluorometric analysis2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and biological evaluation of quinones derived from natural product komaroviquinone as anti-Trypanosoma cruzi agents.
AID309301Antitrypanosomal activity against Trypanosoma cruzi after 72 hrs2007Bioorganic & 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.
AID580589Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as cure rate in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1616128Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 amastigotes infected in human MRC5 SV2 cells incubated for 7 days by chlorophenol red beta-D-galactopyranoside substrate based spectrophotometric assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1541612Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells measured after 96 hrs by inverted microscopy analysis2019Journal of natural products, 12-27, Volume: 82, Issue:12
Structure, Biosynthesis, and Bioactivity of Photoditritide from
AID1616184Antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in Swiss mouse primary cardiac cells incubated for 168 hrs with media replenishment for every 48 hrs followed by compound washout and measured after 168 hrs by light microscopic me2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID596809Antitrypanosomal activity against metacyclic forms of Trypanosoma cruzi infected in vero cells assessed as inhibition of infection at IC25 concentration after 12 hrs2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID1234672Antiparasitic activity against Trypanosoma cruzi strain CL Brener epimastigotes at 300 uM after 12 days by ELISA reader2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Enzymatic synthesis of bile acid derivatives and biological evaluation against Trypanosoma cruzi.
AID396014Antimicrobial activity against Trypanosoma cruzi 1 and Trypanosoma cruzi 2 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID547271Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG at 7 mg/kg, po BID for 90 days measured up to 30 days by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID669305Antitrypanosomal activity against Trypanosoma cruzi Y trymastigotes infected in monkey LLC-MK2 cells after 24 hrs by Brenner counter method in presence of beta-hydroxycopalic2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID1124786Antimicrobial activity against epimastigote stage of Trypanosoma brucei 29-13 after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1498359Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as reduction in mitochondrial membrane potential at IC25 after 72 hrs by Rho123 staining based flow cytometry relative to control2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1067350Antimicrobial activity against Giardia intestinalis IMSS:0696:1 incubated for 48 hrs followed by compound washout measured after 48 hrs2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.
AID1613495Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free adipose tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infect2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID707768Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in BALB/c mouse model of acute Chagas disease assessed as reduction parasitemia at 5 mg/kg/day, ip administered for 5 consecutive days starting on day 7 post i2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1603822Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free oesophagus in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1723647Antitrypanosomal activity against Trypanosoma cruzi epimastigotes2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Expanding the scope of synthetic 1,2,4-trioxanes towards Trypanosoma cruzi and Leishmania donovani.
AID1062981Selectivity index, ratio of CC50 for mouse L929 cells to IC50 for Trypanosoma cruzi Tulahuen amastigotes2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of the antiparasitic activity of bis-(arylmethylidene) cycloalkanones.
AID664488Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells after 96 hrs by spectrophotometric analysis2012Journal 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.
AID598285Antitrypanosomal activity against Trypanosoma cruzi MHOM/MX/1994/Ninoa epimastigotes after 72 hrs by neubauer chamber2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID1156606Antiparasitic activity against Leishmania amazonensis infected in CD-1 mouse macrophages after 72 hrs by spectrophotometric analysis2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID580667Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as reactivation of parasite in mouse at 20 mg/kg/day, po administered twice daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID392020Antitrypanosomal activity against Trypanosoma cruzi Colombiana infected Swiss mouse assessed as prevention of heart inflammatory infiltrates at 120 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1498308Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID344428Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.5 mM after 1 hr by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1238026Selectivity index, ratio of EC50 for BALB/c mouse peritoneal macrophages to EC50 for Leishmania infantum MHOM/BR/72 amastigotes2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1254936Antichagasic activity against firefly luciferase expressing trypamastigote forms of transgenic Trypanosoma cruzi Y infected in Balb/c mouse assessed as reduction in parasite level at 15 mg/kg/day, ip dosed for 10 days by luciferase reporter gene assay2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1294231Cytotoxicity against mouse Cardiomyocytes after 48 hrs by Prestoblue assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1613484Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypomastigotes derived from infected Balb/c albino mouse2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID337134Antitrypanosomal activity against Trypanosoma cruzi Z1 after 48 hrs
AID548112Inhibition of Trypanosoma cruzi triosephosphate isomerase at 100 uM after 2 hrs2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
AID1244472Trypanocidal activity against intracellular amastigotes of Trypanosoma cruzi Tulahuen infected in human U937 cells assessed as reduction of viability of intracellular amastigotes by measuring beta-galactosidase activity after 72 hrs by spectrophotometry a2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids.
AID726231Antitrypanosomal activity against Trypanosoma cruzi DM28 epimastigotes at 256 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1074931Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa staining-based microscopic analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1383429Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y measured after 2 hrs by light microscopic analysis2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1519013Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as body weight gain at 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured up to 120 days post infection2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1615014Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes derived from infected Balb/c mouse after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1587047Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells after 6 days by beta galactosidase reporter assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID1613483Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID547256Antimicrobial activity against Trypanosoma cruzi Berenice-78 infected in mongrel dog assessed as survival of dog at 12 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1264449Leishmanicidal activity against promastigote stage of Leishmania infantum MCAN/ES/92/BCN722 after 48 hrs by acid phosphatase based assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID214976In vitro Trypanosoma cruzi (TC)2001Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
Design, synthesis, and biological evaluation of a series of simple and novel potential antimalarial compounds.
AID1851971Solubility of compound in water at pH 7 by LC-UV analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID537132Antileishmanial activity against promastigotes of Leishmania amazonensis WHO/BR/00/LT0016 after 18 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1603754Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigotes measured after 72 hrs by Neubauer hemocytometer2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1174781Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for epimastigote Trypanosoma cruzi IRHOD/CO/2008/SN32015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1603856Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum total bilirubin level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 po2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID580583Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as cure rate in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1498258Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured o2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID323758Antiparasitic activity against Trypanosoma cruzi Y trypomastigotes2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
AID373285Antitrypanosomal activity against Trypanosoma cruzi bloodstream trypomastigote infected in BALB/c mouse assessed as antibodies at 50 mg/kg, po after 60 days by colorimetric method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In vitro and in vivo antitrypanosomatid activity of 5-nitroindazoles.
AID1683713Antitrypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 (DTU I) blood stream trypomastigote form assessed as parasite growth inhibition incubated for 24 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1518997Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as QRS morphology at 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measured at 170 day2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID626316Antiparasitic activity against trypomastigotes of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs2011Bioorganic & 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).
AID1603741Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes assessed as decrease in serum alkaline phosphatase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting fro2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID265557Antitrypanosomatid activity against Trypanosoma cruzi Y epimastigote form2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
2H-benzimidazole 1,3-dioxide derivatives: a new family of water-soluble anti-trypanosomatid agents.
AID1470759Trypanocidal activity against bloodstream form of Trypanosoma cruzi NINOA infected in NIH mouse assessed as reduction in parasitemia at 100 mg/kg, po measured up to 6 hrs post dose by microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1196782Inhibition of recombinant full-length Trypanosoma cruzi CYP51 assessed as molar ratio of inhibitor to enzyme which causes 2 fold decrease in enzyme activity in 5 mins by HPLC analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1669167Antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in rat H9C2 rat cells assessed as reduction in number of infected cells at 10 uM after 72 hrs by Hoechst 33342 staining based fluorescence microscopy2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from
AID1055179Trypanocidal activity against trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as inhibition of trypomastigotes released in culture medium at IC25 relative to control2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID249627Percentage delyse against amastigote forms of Y strain of Trypanosoma cruzi at 0.5 uM2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
AID282993Antiparasitic activity against Leishmania donovani MHOM/ET/67/HU3 intracellular amastigotes2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate.
AID677211Selectivity index, ratio of IC50 for Vero cells to IC50 for Trypanosoma cruzi intracellular amastigote infected in Vero cells2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1498338Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID509508Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 infected in rat skeletal myoblast at 4.8 ug/ml after 48 hrs2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and preliminary bioactivity assays of 3,4-dichloro-5-(omega-hydroxyalkylamino)-2(5H)-furanones.
AID1065110Trypanocidal activity against Trypanosoma cruzi CA-I/72 infected in BESM cells assessed as parasite re-emergence at 6.6 uM measured over 20 days of drug treatment2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.
AID738320Antitrypanosomal activity against amastigote form of Trypanosoma cruzi Tulahuen infected in african green monkey Vero cells assessed as decrease in number of intracellular parasites at 0.06 to 0.5 mM treated after removal of parasite on cell supernatant f2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
α-Selective glycosylation affords mucin-related GalNAc amino acids and diketopiperazines active on Trypanosoma cruzi.
AID1496043Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse L929 cells assessed as reduction in infection level at 10 uM after 96 hrs by beta galactosidase reporter assay relative to control2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID1615081Toxicity in Balb/c mouse assessed as reduction in body mass at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection relative to control2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1254439Antiparasitic activity against amastigote stage of Trypanosoma cruzi Y in BALB/c mouse macrophages assessed as decrease in number of infected cells at 50 uM incubated for 6 hrs by Giemsa staining-based optical microscopic analysis2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID396020Antimicrobial activity against Trypanosoma cruzi genotype 39 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID362868Cytotoxicity against human THP1 cells after 48 hrs2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
4-nitroacetophenone-derived thiosemicarbazones and their copper(II) complexes with significant in vitro anti-trypanosomal activity.
AID1188734Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as reduction in viable parasites after 24 hrs by Neubauer chamber counting method2014European journal of medicinal chemistry, Oct-30, Volume: 862-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.
AID1613541Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 81 pos2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1603950Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on acetate excretion at IC50 after 72 hrs by H NMR method relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1055170Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as delocalized hepatic destruction at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light microscopi2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID576088Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Mucositis at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID285211Effect on survival in Trypanosoma cruzi Y infected IFN-gamma knock out C57BL/6 mouse Chagas disease model assessed as mean survival time at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID616289Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 amastigotes stage forms incubated for 96 hrs by beta-galactosidase reporter gene assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Antimalarial β-carbolines from the New Zealand ascidian Pseudodistoma opacum.
AID1498195Toxicity in Balb/c mouse assessed as death at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1612295Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 trypomastigotes infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric 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.
AID1294223Antichagasic activity against Trypanosoma cruzi CL-B5 epimastigotes in mouse L929 cells assessed as growth inhibition after 72 hrs by beta galactosidase reporter gene assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1498198Toxicity in Balb/c mouse assessed as reduction in body mass at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection relative to control2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1507195Growth inhibition of Trypanosoma cruzi clone CL B5 epimastigotes at 25 uM after 72 hrs by beta-galactosidase reporter gene assay relative to control2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID1603831Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as parasite-free stomach in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1498303Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 127 po2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1683659Inhibition of nucleic acid level in Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) epimastigote form at IC25 concentration after 72 hrs by Rho (FITC-A) staining based flow cytometric analysis2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID580602Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as reactivation of parasite in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 11 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1403401Trypanocidal activity against Trypanosoma cruzi Brazil trypomastigotes infected in monkey LLC-MK2 cells after 24 hrs by luminescent assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1615046Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free spleen at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection foll2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1613467Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1383426Cytotoxicity against mouse L929 cells assessed as reduction in cell viability after 96 hrs by Alamarblue assay2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1508573Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Balb/c mouse macrophages assessed as reduction in number of infected cells at 0.5 uM measured after 3 days by hoeschst staining based confocal microscopi2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1713341Anti-chagasic activity against Trypanosoma cruzi Brazil trypomastigotes expressing firefly luciferase infected in BALB/c mouse assessed as reduction in parasitemia at 15 mg/kg/day, ip measured after 10 days by bioluminescence assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.
AID1613554Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1773689Trypanocidal activity against amastigotes form of Trypanosoma cruzi CA-I/72 infected in mouse C2C12 cells assessed as inhibition of parasite replication incubated for 48 hrs by DAPI staining based microscopic analysis2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
Structure-Based Optimization of Quinazolines as Cruzain and
AID564777Antitrypanosomal activity against Trypanosoma cruzi Columbian bloodstream forms infected in C3H mouse assessed as survival of mouse at 100 mg/kg/day, po administered 5 days postinfection for 10 consecutive days measured after 31 days2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1753480Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC-5 SV2 cells assessed as inhibition of parasite growth measured after 7 days by spectrophotometric analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID580594Antitrypanosomal activity against Trypanosoma cruzi Y infected in B-lymphocyte knockout C57BL/6 mouse assessed as mean survival time at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1739885Antitrypanosomal activity against Trypanosoma cruzi (MHOM/CH/00/Tulahuen C2, lacZ) amastigotes infected in HFF-1 cells assessed as reduction in parasite growth at 75 uM incubated for 120 hrs by CPRG/Igepal substrate based photometric method relative to co2020European journal of medicinal chemistry, Sep-01, Volume: 201Discovery of highly potent and selective antiparasitic new oxadiazole and hydroxy-oxindole small molecule hybrids.
AID738323Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen expressing beta galactosidase infected in rhesus monkey LLC-MK2 cells assessed as inhibition of parasite viability treated at 24 hrs post-infection measured after 4 days b2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
α-Selective glycosylation affords mucin-related GalNAc amino acids and diketopiperazines active on Trypanosoma cruzi.
AID753401Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Y trypomastigotes2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID1687700Antitrypanosomal activity against Trypanosoma cruzi epimastigotes measured after 72 hrs by Neubauer hemocytometer counting method2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID576093Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Arthromyalgia at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1615031Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells assessed as reduction in infected cells after 72 hrs by Giemsa-staining based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
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.
AID1498324Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID779143Antimicrobial activity against Trypanosoma cruzi Tulahuen C4 amastigotes infected in rat L6 cells after 96 hrs by beta-galactosidase reporter gene 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.
AID707773Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected in african green monkey Vero cells assessed as inhibition of trypomastigotes level at IC25 level 0.5 to 10 days2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1687782Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID341605Antimicrobial activity against Giardia duodenalis G12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID598287Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID1603749Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum uric acid level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 post i2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1854930Cytotoxicity against monkey LLC-MK2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID707780Toxicity against african green monkey Vero cells2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1753506Antitrypanosomal activity against Trypanosoma cruzi Y bloodstream trypomastigotes assessed as inhibition of parasite growth incubated for 24 hrs by light microscopy2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1615016Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1616177In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as mouse survival at 100 mg/kg, po administered once daily for 5 days with 2 days interval for 3 cycles and measured up to 55 days post-infectio2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1603763Antitrypanosomal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 6 amastigote forms measured after 72 hrs by Giemsa staining based assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID263376Antitrypanosomal activity against Trypanosoma cruzi epimastigotes at 100 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID726610Antiparasitic activity against Trypanosoma cruzi amastigotes infected in gamma-irradiated vero cells assessed as growth inhibition measured after 3 days by fluorescence assay2013European journal of medicinal chemistry, Feb, Volume: 60Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.
AID1236978Antitrypanosomal activity against trypomastigotes stage of Trypanosoma cruzi infected in human HT1080 cells assessed as inhibition of parasite growth after 24 hrs by microscopic analysis2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and biological evaluation of quinones derived from natural product komaroviquinone as anti-Trypanosoma cruzi agents.
AID1780975Antitrypanosomal activity against Trypanosoma cruzi trymastigotes assessed as blockage of trypomastigote infectivity at >100 uM incubated for 6 hrs followed by compound washout further infected in BSR cells for 18 hrs measured after 5 hrs post infection b2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1202574Anti-trypanosomal activity against Trypanosoma cruzi Bug 2149 cl10 epimastigote forms assessed as inhibition of parasite growth after 72 hrs by microplate reader based assay2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1410114Antiplasmodial activity against Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric analysis2018Journal 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.
AID1176976Antitrypanosomal activity against Trypanosoma cruzi 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.
AID1459243Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as maximal parasite density at 15 uM measured after 9 to 10 days by haemocytometric method (Rvb = 45 10'6/ml)2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID563566Hepatotoxicity against Swiss-Webster mouse assessed as GPT at 100 mg/kg/day measured after 14 days postinfection2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1245595Antichagasic activity against trypomastigote stage of Trypanosoma cruzi Brazil infected in Balb/c mouse assessed as reduction in parasite load at 13 mg/kg/day, ip measured after 5 days by luciferase reporter gene assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID1329377Antileishmanial activity against Leishmania infantum MHOM/BR/1972/LD promastigote forms infected in golden hamster assessed as reduction in parasite viability after 48 hrs by MTT assay2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID265556Antitrypanosomatid activity against Trypanosoma cruzi CL Brener epimastigote form2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
2H-benzimidazole 1,3-dioxide derivatives: a new family of water-soluble anti-trypanosomatid agents.
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).
AID707779Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/VO/2008/SN3 epimastigotes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1633355Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
AID635853Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing Lac Z infected in rat L6 cells after 96 hrs by spectrophotometry2011Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
Bis(oxyphenylene)benzimidazoles: a novel class of anti-Plasmodium falciparum agents.
AID1498244Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in spleen tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days start2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1613523Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 p2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID677208Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by flow cytometric analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID362661Antitrypanosomal activity against Trypanosoma cruzi Tulahuen2008Journal of natural products, Sep, Volume: 71, Issue:9
Benzoic acid derivatives from Piper species and their antiparasitic activity.
AID1174777Trypanocidal activity against epimastigote Trypanosoma cruzi IRHOD/CO/2008/SN32015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1517429Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi ARMA 13 cl1 infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID1616170Toxicity in Swiss Webster mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as body weight loss at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection and measured daily up to 40 days post-infecti2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID453255Antitrypanosomal activity against Trypanosoma cruzi2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.
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).
AID362867Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 after 5 days2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
4-nitroacetophenone-derived thiosemicarbazones and their copper(II) complexes with significant in vitro anti-trypanosomal activity.
AID1603852Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum aspartate aminotransferase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID580603Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as occurrence of subpatent level of parasitemia at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post 2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1683682Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on ALT/GPT level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID564735Antitrypanosomal activity against Trypanosoma cruzi RBVIII epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1615101Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 post2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1501879Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes assessed as parasite viability after 24 hrs by resazurin staining-based hemocytometric analysis2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID303387Toxicity in Trypanosoma cruzi Tulahuen 2 infected Swiss mouse model of Chagas disease at 100 mg/kg, po2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.
AID1169288Antitrypanosomal activity against LacZ expressing Trypanosoma cruzi Tuluhaen C2C4 amastigotes2014Journal of natural products, Oct-24, Volume: 77, Issue:10
Antitrypanosomal quinoline alkaloids from the roots of Waltheria indica.
AID1603875Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum uric acid level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 70 pos2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1603769Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 1 amastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID694955Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in rhesus monkey LLC-MK2 cells assessed parasite viability after 24 hrs2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice.
AID547272Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG2 at 7 mg/kg, po BID for 90 days measured up to 30 days by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1074908Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) epimastigotes assessed as disruption of cytoskeleton with disorganization of microtubule structure at IC25 after 96 hrs by transmission electron microscopic analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1713342Anti-chagasic activity against Trypanosoma cruzi Brazil trypomastigotes expressing firefly luciferase infected in BALB/c mouse assessed as reduction in parasitemia at 15 mg/kg/day, ip measured after 5 days by bioluminescence assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.
AID1616186In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection in presence of cy2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1879404Toxicity in acute CD Swiss Webster mouse model infected with Trypanosoma cruzi Y strain assessed as animal survival at 100 mg/kg, po qd for 5 consecutive days measured daily for upto 30 days post-treatment2022European journal of medicinal chemistry, Mar-05, Volume: 231N
AID1616180Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes measured after 24 hrs by Neubauer chamber-based light microscopic analysis2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1062786Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 6 infected in Swiss mouse assessed as mouse survival at 100 mg/kg, po qd administered on day 8 post-infection for 20 days followed by 10 days non-treatment period followed by three cycles of imm2013Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.
AID396018Antimicrobial activity against Trypanosoma cruzi genotype 19 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID693341Growth inhibition of mouse J774 cells at 256 uM after 24 hrs by resazurin reduction assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1613522Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 16 po2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID637700Trypanocidal activity against trypomastigote Trypanosoma cruzi Tulahuen C2C4 infected in L6 cells after 96 hrs by beta-galactosidase reporter gene assay2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anti-protozoal activity of novel dihydropyrrolo[3,4-d][1,2,3]triazoles.
AID1766959Cytotoxicity against mouse NCTC clone 929 cells assessed as reduction in cell viability after 48 hrs by MTT assay
AID656215Cytotoxicity against african green monkey Vero cells at 25 uM after 3 days2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Phosphonium lipocations as antiparasitic agents.
AID1202575Cytotoxicity against human LL24 cells assessed as inhibition of cell growth after 24 hrs by MTT assay2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1851979Antitrypanosomal activity against bioluminescent Trypanosoma cruzi CL Brener trypomastigotes infected in BALB/c mouse assessed as reduction in parasite burden at 100 mg/kg, po administered once daily for 5 days starting from 14 days post infection and mea2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1902913Antitrypanosomal activity against amastigotes form of Trypanosoma cruzi CA-I/72 infected in mouse C2C12 cells assessed as parasite infection level by DAPI staining based microscopic analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against
AID580663Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as number of mouse with reactivated parasite at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post inf2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1757145Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 cells assessed as inhibition of parasite growth incubated for 7 days by chlorophenol red-fl-D-galactopyranoside based spectrophotometric analysis2021European journal of medicinal chemistry, Apr-15, Volume: 216Synthesis and evaluation of 3'-fluorinated 7-deazapurine nucleosides as antikinetoplastid agents.
AID1500575Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 amastigotes infected in rat L6 cells after 96 hrs by CPRG/nonidet-based inverted microscopic analysis2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID768699Trypanocidal activity against epimastigote stage of Trypanosoma cruzi Y after 72 hrs by MTT assay2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates.
AID677303Antitrypanosomal activity against Trypanosoma cruzi infected in BALB/c mouse assessed as reduction in parasitemia at 1 mg/kg, ip dosed for 5 days measured on day 30 post infection2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1503755Antitrypanosomal activity against Trypanosoma cruzi trypomastigote forms infected in rat L6 cells after 96 hrs by CPRG/Nonidet substrate based photometric method2017Journal 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.
AID1381722Inhibition of human microsomal CYP2C19 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1498266Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in urea level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 812018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1164936Induction of apoptosis in human platelets assessed as early apoptotic cells after 10 mins using Annexin V/propidium iodide by flow cytometry (Rvb = 10.30 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1543106Cytotoxicity in mouse NCTC-929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Structure-activity relationship study of antitrypanosomal chalcone derivatives using multivariate analysis.
AID1519000Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as effect on QT interval at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measur2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID396003Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as parasitemia remaining in fresh blood2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1603746Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on parasite glycolytic pathway by measuring change in succinate excretion after 72 hrs by H NMR method2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1055165Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as presence of necrotic cells in portal space at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1074922Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in BALB/c mouse assessed as reduction in parasitemia at 1 mg/kg/day, ip treated from day 5 to day 10 post-infection measured on day 14 post-infection2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1480892Cytotoxicity against mouse J774A.1 cells after 24 to 72 hrs by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID764118Cytotoxicity against human FN1 fibroblasts after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
5-Nitro-2-furfuriliden derivatives as potential anti-Trypanosoma cruzi agents: design, synthesis, bioactivity evaluation, cytotoxicity and exploratory data analysis.
AID1589637Growth inhibition of trypomastigote form of Trypanosoma cruzi Y infected in human U2OS cells measured after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis2019Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
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]
AID1603761Antitrypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 1 amastigote forms measured after 72 hrs by Giemsa staining based assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID598282Antiprotozoan activity against Trichomonas vaginalis GT3 trophozoites after 48 hrs2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID324605Growth inhibition of Trypanosoma cruzi Tulahuen epimastigotes assessed as drug level causing decrease in growth constant2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Trypanosoma cruzi: activities of lapachol and alpha- and beta-lapachone derivatives against epimastigote and trypomastigote forms.
AID337132Antitrypanosomal activity against Trypanosoma cruzi 27R27CL1 after 48 hrs
AID1074376Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as reduction of amastigote number per cell at IC25 preincubated for 12 hrs followed by compound washout measured2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID547253Antimicrobial activity against Trypanosoma cruzi Y infected in mongrel dog assessed as suppression of microbial proliferation at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID396011Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1615096Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1902914Cytotoxicity against mouse C2C12 cells assessed as lethal dose2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against
AID677313Antitrypanosomal activity against Trypanosoma cruzi infected in BALB/c mouse assessed as survival rate at 1 mg/kg, ip dosed for 5 days2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1498208Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 p2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1739879Antitrypanosomal activity against Trypanosoma cruzi (MHOM/CH/00/Tulahuen C2, lacZ) amastigotes infected in HFF-1 cells assessed as reduction in parasite growth incubated for 120 hrs by CPRG/Igepal substrate based photometric method2020European journal of medicinal chemistry, Sep-01, Volume: 201Discovery of highly potent and selective antiparasitic new oxadiazole and hydroxy-oxindole small molecule hybrids.
AID1868687Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based fluorescence analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID1054901Trypanocidal activity against extracellular epimastigote stage of Trypanosoma cruzi CL-B5 assessed as reduction of parasite load after 72 hrs by resazurin dye-based fluorometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
In vitro and in vivo antileishmanial and trypanocidal studies of new N-benzene- and N-naphthalenesulfonamide derivatives.
AID1608321Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Swiss mouse infected with monkey LLC-MK2 cells after 5 days by fluorescence spectrophotometric analysis2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis of quinones with highlighted biological applications: A critical update on the strategies towards bioactive compounds with emphasis on lapachones.
AID1683686Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on uric acid level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID598283Antiprotozoan activity against Entamoeba histolytica HM1-IMSS trophozoites after 48 hrs2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID1780967Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes assessed as inhibition of cellular invasion incubated for 6 hrs in high-glucose DMEM medium followed by compound washout further infected in BSR cells measured after 72 hrs by fluorescenc2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1498333Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1603773Trypanocidal activity against Trypanosoma cruzi trypomastigote form infected in African green monkey Vero cells measured after 48 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID215337In vitro inhibitory affect against Trypanosoma brucei; No data2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID576097Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Epigastralgia at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1613494Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in parasitaemia level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection meas2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID669381Antileishmanial activity against Leishmania chagasi MHOM/BR/1974/PP75 after 72 hrs by MTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
AID1776166Antitrypanosomal activity against amastigote form of Trypanosoma cruzi Tulahuen C4 expressing LacZ infected in rat L6 cells assessed as inhibition of parasite growth incubated for 96 hrs by CPRG/Nonidet reagent based inverted microscopic analysis2021Journal of natural products, 04-23, Volume: 84, Issue:4
Spirombandakamine A
AID1780963Cytotoxicity against golden hamster BSR cells assessed as reduction in cell viability incubated for 72 hrs followed by alamar blue addition further incubated for 6 hrs2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID414762Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth at 10 ug/ml after 24 hrs2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Molecular modeling studies and in vitro bioactivity evaluation of a set of novel 5-nitro-heterocyclic derivatives as anti-T. cruzi agents.
AID1164938Induction of apoptosis in human platelets assessed as necrotic cells after 10 mins using Annexin V/propidium iodide by flow cytometry (Rvb = 0.07 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1202551Antimicrobial activity against Leishmania mexicana MHOM/BZ/61/M379 after 24 hrs by haemocytometry2015European journal of medicinal chemistry, , Volume: 96Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
AID396023Antimicrobial activity against Trypanosoma cruzi OPS21 cl11 and Trypanosoma cruzi MAS cl11 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID596806Antitrypanosomal activity against epimastigote form of Trypanosoma cruzi assessed as inhibition of parasite growth2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID1351069Antitrypanosomal activity against Trypanosoma cruzi Silvio X10 cl1 Tc1 epimastigotes measured after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID766428Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 2 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID3334Effective dose required against Trypanosoma cruzi amastigotes in 3T3 Fibroblasts2001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.
AID1238019Anti-leishmanial activity against Leishmania amazonensis MPRO/BR/1972/M1841-LV-79 promastigotes assessed as parasite growth inhibition incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1686724Antitrypanosomal activity against Trypanosoma cruzi infected in African green monkey Vero cells assessed as reduction in number of amastigotes per infected cell measured up to 10 days by Giemsa staining based hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1695262Antitrypanosomal activity against Trypanosoma cruzi infected in rat H9c2 infected with trypomastigotes from parasite-infected monkey LLC-MK2 cells measured after 72 hrs by DRAQ5 DNA dye based microscopic imaging analysis
AID1196788Antichagasic activity against trypomastigote stage of Trypanosoma cruzi Brazil infected in Balb/c mouse assessed as parasite index at 15 mg/kg/day, ip measured after 5 days by luciferase reporter gene assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID677213Trypanosomicidal activity against Trypanosoma cruzi infected in Vero cells assessed as reduction in amastigotes per infected Vero cells after 6 days by Giemsa staining method2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1854931Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in monkey LLC-MK2 cells assessed as reduction in cell death inducing capability incubated for 24 hrs by hemocytometer chamber based analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1498314Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID675026Trypanocidal activity against bloodstream trypomastigotes of Trypanosoma cruzi infected in mouse blood assessed as lytic effect after 24 hrs2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents.
AID1245589Prodrug conversion assessed as Trypanosoma brucei recombinant His-tagged type-1 nitroreductase-mediated drug metabolism by measuring NADH oxidation after 5 mins by spectrophotometric analysis2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID1565127Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Swiss webster mouse cardiac cells assessed as reduction in parasite viability after 24 hrs by Celltiter-Glo assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1184292Antitrypanosomal activity against intracellular Trypanosoma cruzi infected in human U2OS cells assessed as reduction in parasite count at 400 uM after 48 hrs by confocal microscopy2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a]benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi.
AID1615074Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as reduction in DNA and RNA levels at IC25 after 72 hrs by acridine orange staining based flow cytometry relative to control2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1498186Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypamastigotes derived from infected Balb/c albino mouse2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID669304Antitrypanosomal activity against Trypanosoma cruzi Y trymastigotes infected in monkey LLC-MK2 cells after 24 hrs by Brenner counter method in presence of copalic2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID1400236Growth inhibition of Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells after 72 hrs by beta-galactosidase reporter gene assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Synthesis and SAR of new isoxazole-triazole bis-heterocyclic compounds as analogues of natural lignans with antiparasitic activity.
AID1067357Cytotoxicity against African green monkey Vero cells assessed as cell viability after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.
AID1683711Antitrypanosomal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen (DTU VI) epimastigote form assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID344436Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms after 24 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1615040Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free bone marrow at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1683677Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on CK-MB level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1054900Cytotoxicity against mouse J774 cells assessed as reduction of cell viability after 24 hrs by resazurin dye-based fluorometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
In vitro and in vivo antileishmanial and trypanocidal studies of new N-benzene- and N-naphthalenesulfonamide derivatives.
AID1669165Cytotoxicity against rat H9c2 cells after 72 hrs by Hoechst 33342 staining based fluorescence microscopy2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from
AID1432598Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigote forms infected in mouse L929 cells after 96 hrs by chlorophenol red-beta-D-galactopyranoside dye based assay2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Synthesis and biological evaluation of potential inhibitors of the cysteine proteases cruzain and rhodesain designed by molecular simplification.
AID1525222Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes measured after 24 hrs by resazurin dye based assay2019Journal of natural products, 05-24, Volume: 82, Issue:5
Antitrypanosomal Activity of Acetogenins Isolated from the Seeds of Porcelia macrocarpa Is Associated with Alterations in Both Plasma Membrane Electric Potential and Mitochondrial Membrane Potential.
AID1592302Antileishmanial activity against Leishmania mexicana MNYC-BZ/62/M379 promastigotes assessed as growth inhibition measured after 24 hrs by MTT assay
AID426310Antiamnesic activity against Entamoeba histolytica HM-1:IMSS trophozoites after 48 hrs by Hill culture method2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles.
AID1615056Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free stomach at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection fol2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1678869Selectivity index, ratio of LC50 for cytotoxicity against albino Swiss mouse peritoneal macrophages to IC50 for Antitrypanosomal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes assessed as lysis of parasite in absence of mouse bloo2020RSC medicinal chemistry, Oct-01, Volume: 11, Issue:10
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: redox and biological implications.
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.
AID1432290Selectivity index, ratio of CC50 for human THP1 cells to IC50 for Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells2017European journal of medicinal chemistry, Mar-10, Volume: 128Design and synthesis of a new series of 3,5-disubstituted isoxazoles active against Trypanosoma cruzi and Leishmania amazonensis.
AID547250Toxicity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as weight loss at 7 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 6 months2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID677292Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as hepatic destruction in portal tracts at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1615087Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 81 po2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID75731In vitro inhibition of rabbit muscle GAPDH.2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.
AID337145Antitrypanosomal activity against Trypanosoma cruzi 9280CL1 after 48 hrs
AID303379Antitrypanosomal activity against Trypanosoma cruzi CL Brener2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.
AID1498243Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in muscle tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days start2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID753036Antitrypanosomal activity against epimastigote stage of Trypanosoma cruzi Y assessed as parasite growth inhibition after 5 days by spectrophotometric analysis2013European journal of medicinal chemistry, Jun, Volume: 64Ligand-based design, synthesis, and experimental evaluation of novel benzofuroxan derivatives as anti-Trypanosoma cruzi agents.
AID1603871Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum alkaline phosphatase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1586759Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 amastigotes harboring LacZ infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric analysis2018Journal of natural products, 12-28, Volume: 81, Issue:12
Antiprotozoal Isoprenoids from Salvia hydrangea.
AID1613474Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypomastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID766424Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 32 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID736792Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3
Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators.
AID1613562Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1381723Inhibition of human microsomal CYP2D6 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID287715Antitrypanosomatid activity against Trypanosoma cruzi Y epimastigotes assessed as reduction of growth after 5 days2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships.
AID1277887Selectivity index, ratio of IC50 for for mouse C3H cells to IC50 for Trypanosoma cruzi Tulahuen amastigotes infected in mouse C3H cells2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Semisynthesis of new aphidicolin derivatives with high activity against Trypanosoma cruzi.
AID213632Evaluated in vitro for antitrypanosomal activity against Trypanosoma cruzi2002Bioorganic & medicinal chemistry letters, Dec-16, Volume: 12, Issue:24
Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.
AID1383425Cytotoxicity against mouse L929 cells assessed as reduction in cell viability after 96 hrs by light microscopic analysis2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID707778Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/VO/2008/SN3 axenic amastigotes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1196783Inhibition of recombinant full-length Trypanosoma cruzi CYP51 assessed as molar ratio of inhibitor to enzyme which causes 2 fold decrease in enzyme activity in 1 hr by HPLC analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID548108Selectivity for Trypanosoma cruzi triosephosphate isomerase over human triosephosphate isomerase2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
AID1070002Selectivity index, ratio of LC50 for mouse NCTC-929 cells to IC50 for amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1126158Antitrypanosomal activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C42014Journal of natural products, Apr-25, Volume: 77, Issue:4
Antiparasitic chaiyaphumines from entomopathogenic Xenorhabdus sp. PB61.4.
AID576078Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Headache at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID766605Antiparasitic activity against epimastigotes of Trypanosoma cruzi assessed as inhibition of parasite proliferation2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Preparation and antitrypanosomal activity of secochiliolide acid derivatives.
AID1603770Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 1 trypomastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID401651Antitrypanosomal activity against Trypanosoma cruzi in rat L6 cells2005Journal 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.
AID1638039Anti-trypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic analysis2019European journal of medicinal chemistry, Mar-01, Volume: 165Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity.
AID263382Antitrypanosomal activity against Trypanosoma cruzi amastigotes at 100 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID1383432Cytotoxicity against Swiss Webster mouse cardiac cells assessed as reduction in cell viability after 24 hrs by prestoblue assay2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1615114Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1682943Cytotoxicity against monkey LLC-MK2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1603819Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free bone marrow in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting fro2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID401638Antitrypanosomal activity against Trypanosoma cruzi2005Journal of natural products, May, Volume: 68, Issue:5
Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.
AID1697059Cytotoxicity against Balb/c mouse peritoneal macrophage assessed as cell viability measured after 72 hrs by alamar blue assay2020Journal of natural products, 09-25, Volume: 83, Issue:9
Production of Highly Active Antiparasitic Compounds from the Controlled Halogenation of the
AID564746Toxicity in male Swiss-Webster mouse assessed as mortality at cumulative dose of 200 mg/kg, ip measured after 48 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1329379Cytotoxicity against mouse NCTC-929 cells assessed as decrease in cell viability after 48 hrs by MTT assay2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID766426Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 8 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID419679Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in rat L6 cells2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase.
AID344435Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 1 mM after 24 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID669299Antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in monkey LLC-MK2 cells after 96 hrs by Geimsa staining method2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID547508Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG at 12 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID396019Antimicrobial activity against Trypanosoma cruzi genotype 32 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1480897Induction of apoptosis in bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells assessed as necrotic cells at 5 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric method (Rvb = 0.02017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID1202488Trypanosomicidal activity against epimastigote stage of Trypanosoma cruzi CL-B5 after 72 hrs by beta-galactosidase reporter gene assay2015European journal of medicinal chemistry, , Volume: 96Bond-based bilinear indices for computational discovery of novel trypanosomicidal drug-like compounds through virtual screening.
AID1603860Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum urea level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 70 post inf2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1498269Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in urea level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 122018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID337136Antitrypanosomal activity against Trypanosoma cruzi Z2CL4 after 48 hrs
AID1615106Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1613560Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1422886Antitrypanosomal activity against Trypanosoma cruzi Dm28c trypomastigotes infected in African green monkey Vero cells after 24 hrs by CPRG/Nonidet reagent based beta-galactosidase reporter gene assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID693343Growth inhibition of mouse J774 cells at 128 uM after 24 hrs by resazurin reduction assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID575889Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of paresthesias on 4th week of treatment2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID547258Antimicrobial activity against Trypanosoma cruzi Berenice-78 infected in mongrel dog assessed as survival of dog at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1312167Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi CA-I/72 infected in mouse C2C12 cells measured after 3 days by DAPI staining-based assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi.
AID302066Reduction of Leishmania amazonensis 575 infection in mouse peritoneal macrophage at 25 uM after 48 hrs2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides.
AID1294230Antichagasic activity against Trypanosoma cruzi Y strain amastigotes in mouse cardiomyocytes assessed as growth inhibition after 48 hrs by giemsa staining based assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1498238Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in bone marrow tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID263380Unspecific cytotoxicity against murine J774 macrophages at 10 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID1592305Selectivity index, ratio of CC50 for mouse J774.A1 cells to IC50 for antileishmanial activity against Leishmania mexicana MNYC-BZ/62/M379 promastigotes
AID1055178Trypanocidal activity against bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in BALB/c mouse assessed as reduction of circulating parasite burden at 5 mg/kg, ip administered for 5 to 10 days measured 22 to 60 days post-inf2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1712841Selectivity index, ratio of >90% maximum non-toxic concentration for BALB/c mouse splenocyte to IC50 for Trypanosoma cruzi Y strain trypomastigotes2016European journal of medicinal chemistry, Oct-04, Volume: 121New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.
AID1351070Antitrypanosomal activity Trypanosoma cruzi Y Tc2 epimastigotes measured after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID1498206Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection meas2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1498345Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1498259Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured o2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1780962Antiprotozoal activity against Trypanosoma cruzi epimastigotes assessed as inhibition of parasite growth incubated for 72 hrs followed by alamar blue addition further incubated for 24 hrs2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1565135Selectivity index, ratio of CC50 for mouse cardiomyocyte infected with intracellular amastigote stage of Trypanosoma cruzi Y strain to IC50 for amastigote stage of Trypanosoma cruzi Y strain2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1459252Trypanocidal activity against Trypanosoma cruzi RA tripamastigote bloodstream forms infected in Balb/c mouse assessed as mouse survival at 100 mg/kg, po administered on day 9 post infection for 5 consecutive days measured daily during compound dosing up t2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID1613564Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1603839Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum alanine aminotransferase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting fr2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1508559Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells assessed as reduction in parasite motility measured after 24 hrs by neubauer chamber method2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1174796Antiparasitic activity against trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in BALB/c mouse acute chagas disease model assessed as parasite reduction in blood at 5 mg/kg, ip measured on day 40 post infection2015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID598281Antiprotozoan activity against Giardia intestinalis IMSS:0696:1 trophozoites after 48 hrs2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID341599Antiplasmodial activity against Plasmodium falciparum K12007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1686756Antitrypanosomal activity against Trypanosoma cruzi Arequipa trypomastigotes infected in BALB/c mouse assessed as reduction in parasitemia measured during acute phase (days 0 to 40 post infection) at 50 to 100 mg/kg, po dosed on alternating days (7 to 15 2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1613543Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 127 po2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID656216Cytotoxicity against african green monkey Vero cells at 12.5 uM after 3 days2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Phosphonium lipocations as antiparasitic agents.
AID1519014Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as body weight gain at 30 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured up to 120 days post infection2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1633356Selectivity index, ratio of CC50 for mouse RAW264.7 cells to IC50 for Trypanosoma cruzi Dm28c epimastigotes
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.
AID675029Cytotoxicity against african green monkey Vero cells after 24 hrs by MTT assay2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents.
AID1613568Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on d2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID753405Cytotoxicity against human HeLa cells after 24 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID580660Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as occurrence of subpatent level of parasitemia at 20 mg/kg/day, po administered twice daily for 20 consecutive days measured 60 days post 2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1615080Toxicity in Balb/c mouse assessed as reduction in body mass at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection relative to control2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1455941Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells after 96 hrs by beta-galactosidase reporter gene assay
AID1603828Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free spleen in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 82019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1603887Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as depolarization of mitochondrial membrane at IC50 measured after 72 hrs by rhodamine 123 and acridine orange staining based flow cytometry relative to 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID337137Antitrypanosomal activity against Trypanosoma cruzi 13379 CL3 after 48 hrs
AID598286Antimalarial activity against Plasmodium berghei schizonts isolated from parasitized erythrocytes infected Wistar rat measured 16 hrs post compound exposure2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
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.
AID1055167Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as centrilobular destruction of hepatic vein at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light 2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1811311Selectivity index, ratio of CC50 for mouse J774.2 cells to IC50 for Trypanosoma cruzi MHOM/MX/1994/Ninoa2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID564077Antitrypanosomal activity against Trypanosoma cruzi 762 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1753503Toxicity in Swiss webster mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as animal survival at 10 mg/kg, po qd for 5 days treatment started at 6 days post-infection and measured at 34 days post-infection2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1687706Selectivity index, ratio of CC50 African green monkey Vero cells to IC50 for Trypanosoma cruzi amastigotes2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID337148Antitrypanosomal activity against Trypanosoma cruzi A99CL7 after 48 hrs
AID1498254Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection mea2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615079Toxicity in Balb/c mouse assessed as death at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1712840Cytotoxicity against BALB/c mouse splenocyte incubated for 24 hrs by [3H]-thymidine incorporation based counter beta irradiation method2016European journal of medicinal chemistry, Oct-04, Volume: 121New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.
AID1254440Antiparasitic activity against amastigote stage of Trypanosoma cruzi Y in BALB/c mouse macrophages assessed as decrease in number of intracellular amastigotes at 50 uM incubated for 6 hrs by Giemsa staining-based optical microscopic analysis2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID447813Antitrypanosomal activity against Trypanosoma cruzi Y epimastigote form after 11 days by Trypan blue exclusion method2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Ruthenium complexes endowed with potent anti-Trypanosoma cruzi activity: Synthesis, biological characterization and structure-activity relationships.
AID669301Toxicity in human RBC assessed as hemolysis after 3 hrs2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID1281414Trypanocidal activity against trypamostigote form of Trypanosoma cruzi Y infected in African green monkey Vero cells after 24 hrs by neubauer chamber method2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID1299555Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometric method2016Journal of natural products, Feb-26, Volume: 79, Issue:2
Abietane-Type Diterpenoid Amides with Highly Potent and Selective Activity against Leishmania donovani and Trypanosoma cruzi.
AID730420Antitrypanosomal activity against Trypanosoma cruzi Tulahuen TcVI extracellular trypomastigotes forms transfected with beta-galactosidase gene infected in rat L6 cells assessed as inhibition of parasite growth after 4 days2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
AID1254436Cytotoxicity against mouse J774 cells assessed as cell viability after 72 hrs by Alamar Blue assay2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1603825Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free heart in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1613550Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID447812Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigote form after 24 hrs by Trypan blue exclusion method2009Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
Ruthenium complexes endowed with potent anti-Trypanosoma cruzi activity: Synthesis, biological characterization and structure-activity relationships.
AID762758Cytotoxicity against Balb-c mouse 3T3 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Molecular design, synthesis and biological evaluation of 1,4-dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity.
AID1615024Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes derived from infected Balb/c mouse2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID253512Inhibitory concentration against wild-type (427) Trypanosoma brucei2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
AID1507436Cytotoxicity against Swiss albino mouse peritoneal macrophages after 24 hrs by PrestoBlue dye based assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Rhodium-catalyzed C-H bond activation for the synthesis of quinonoid compounds: Significant Anti-Trypanosoma cruzi activities and electrochemical studies of functionalized quinones.
AID1238024Selectivity index, ratio of EC50 for BALB/c mouse peritoneal macrophages to EC50 for Leishmania infantum MHOM/BR/72 promastigotes2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID472780Antitrypanosomal activity against Trypanosoma cruzi tulahuen C4 trypomastigotes infected mouse assessed as decrease in parasite replication at 20 mg/kg/day, ip on days 6 to 11 days post infection after 6 days2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
AID1174779Antiparasitic activity against trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in BALB/c mouse acute chagas disease model assessed as parasite reduction in blood2015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1613534Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID564756Antitrypanosomal activity against Trypanosoma cruzi Y bloodstream forms infected in Swiss-Webster mouse assessed as decrease in parasite load at 100 mg/kg/day, po administered 8 days postinfection measured on day 22010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1264451Selectivity index, ratio of IC50 for rat L6 cells to IC50 for promastigote stage of Leishmania infantum MCAN/ES/92/BCN7222015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1188735Trypanocidal activity against epimastigote forms of Trypanosoma cruzi Y assessed as reduction in viable parasites after 11 days by Neubauer chamber counting method2014European journal of medicinal chemistry, Oct-30, Volume: 862-Pyridyl thiazoles as novel anti-Trypanosoma cruzi agents: structural design, synthesis and pharmacological evaluation.
AID302064Antiprotozoal activity against Trypanosoma cruzi Y in vero cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides.
AID253513Inhibitory concentration against wild-type (427) with NAC Trypanosoma brucei2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.
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.
AID1067349Antimicrobial activity against Trichomonas vaginalis GT3 incubated for 48 hrs followed by compound washout measured after 48 hrs2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.
AID1184288Antitrypanosomal activity against intracellular Trypanosoma cruzi infected in human U2OS cells after 48 hrs by confocal microscopy2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a]benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi.
AID766419Antiparasitic activity against epimastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 32 uM after 72 hrs by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID547246Toxicity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as weight loss at 7 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1480890Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells measured after 24 hrs by neubauer chamber method2017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID1403408Trypanocidal activity against Trypanosoma cruzi Y intracellular amastigotes infected in Swiss Webster mouse cardiomyocytes after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1613556Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID547511Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Y assessed as production of antibody IgG2 at 12 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1238023Anti-leishmanial activity against Leishmania infantum MHOM/BR/72 promastigotes assessed as parasite growth inhibition incubated for 72 hrs by MTT assay2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1351068Antitrypanosomal activity against Trypanosoma cruzi Colombiana Tc1 epimastigotes measured after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID1614019Antiprotozoal activity against Trypanosoma cruzi CL Brener trypomastigotes infected in BALB/c mouse assessed as reduction in parasitemia at 50 mg/kg, ip bid treated for 4 consecutive days starting at 3 days post infection by bioluminescence assay relative2019Journal 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.
AID576942Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as parasite DNA level at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection measured 180 days post dose b2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID677312Trypanosomicidal activity against Trypanosoma cruzi epimastigotes assessed as change in L-lactate metabolite excretion after 96 hrs by NMR analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1720853Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Albino Swiss mouse assessed as lysis of parasite in presence of 5 % mouse blood incubated for 24 hrs by Neubauer chamber method2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Strategies towards potent trypanocidal drugs: Application of Rh-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulation and nitroalkene reactions for the synthesis of substituted quinones and their evaluation against Trypanosoma cruzi.
AID1508561Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID287713Antitrypanosomatid activity against Trypanosoma cruzi Tulahuen 2 epimastigotes assessed as reduction of growth after 5 days2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships.
AID1070011Selectivity index, ratio of LC50 for mouse NCTC-929 cells to IC50 for epimastigote stage of Trypanosoma cruzi CL Brener2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
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.
AID1616163In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection and measured 8 da2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID337150Antitrypanosomal activity against Trypanosoma cruzi TeCL2 after 48 hrs
AID1780965Antiprotozoal activity against Trypanosoma cruzi epimastigotes assessed as decrease in parasitemia by measuring change in fluorescence intensity at >2.5 uM measured after 3 days by flourescence based analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID213640In vitro inhibitory affect against Trypanosoma cruzi; (32.7 mM Sb)2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID1381736Antitrypanosomal activity against Trypanosoma cruzi amastigote form2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1811308Trypanocidal activity against Trypanosoma cruzi MHOM/MX/1994/Ninoa assessed as inhibition of parasite growth measured after 48 hrs by MTT assay2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID1613482Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1155754Induction of NO release assessed as nitrite level2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.
AID1439206Cytotoxicity against human U2OS cells2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols.
AID728172Antitrypanosomal activity against Trypanosoma cruzi trypomastigote infected in monkey LLC-MK2 cells after 96 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID1498172Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes after 48 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID450069Cytotoxicity against BALB/c mouse splenocyte assessed as [3H]thymidine incorporation by beta-counting2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents.
AID527277Trypanocidal activity against intracellular amastigotes of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 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.
AID287514Toxicity against Vero cells after 72 hrs2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
1,4-Bis(alkylamino)benzo[g]phthalazines able to form dinuclear complexes of Cu(II) which as free ligands behave as SOD inhibitors and show efficient in vitro activity against Trypanosoma cruzi.
AID1615041Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free brain at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1140998Antitrypanosomal activity against Trypanosoma cruzi CL Brener infected in BALB/c mouse assessed as mouse survival at 192 umol/kg/day, po for 14 days administered in saline and tween 80 measured up to 60 days relative to control2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.
AID1254921Activity of histidine tagged recombinant Trypanosoma brucei brucei type 1 nitroreductase assessed as NADH oxidation at 100 uM by spectrophotometry method2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID671572Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen infected in Swiss mouse model of chagas disease assessed as decrease in parasite level in blood at 100 mg/kg, po administered 8 day after post infection qd for 20 days2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
AID768692Inhibition of Trypanosoma cruzi cruzain expressed in Escherichia coli DH5-alpha using Bz-Phe-Arg-AMC as substrate at 10 uM preincubated for 5 mins followed by substrate addition measured for 5 mins by spectrofluorimetric analysis relative to control2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates.
AID1199919Antiprotozoal activity against intracellular amastigote stage of Trypanosoma cruzi Tulahuen C4 by colorimetric assay2015Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4
Antiprotozoal activity and DNA binding of dicationic acridones.
AID378199Antitrypanosomal activity against galactosidase gene containing Trypanosoma cruzi Tulahuen C2C4 trypomastigotes in rat L6 cells after 4 days2000Journal of natural products, Nov, Volume: 63, Issue:11
Ancistroealaines A and B, two new bioactive naphthylisoquinolines, and related naphthoic acids from Ancistrocladus ealaensis.
AID1678867Selectivity index, ratio of LC50 for cytotoxicity against albino Swiss mouse peritoneal macrophages to IC50 for Antitrypanosomal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes assessed as lysis of parasite in presence of 5 % mouse2020RSC medicinal chemistry, Oct-01, Volume: 11, Issue:10
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: redox and biological implications.
AID396008Antimicrobial activity against Trypanosoma cruzi genotype 19 and genotype 32 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1496048Selectivity index, ratio of LC50 for Swiss Webster mouse cardiac cells to EC50 for bloodstream trypomastigote stage of Trypanosoma cruzi Y2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID1615090Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 post inf2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID547257Antimicrobial activity against Trypanosoma cruzi Y infected in mongrel dog assessed as survival of dog at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID753408Trypanocidal activity against Trypanosoma cruzi Y trypomastigotes infected in human HeLa cells at 37 degC after 18 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID613448Selectivity index, ratio of CC50 for african green monkey COS7 cells to IC50 for bloodstream trypomastigote form of Trypanosoma cruzi2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID1603888Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as inhibition of DNA and RNA levels at IC50 measured after 72 hrs by by acridine orange staining based flow cytometry relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1254916Antichagasic activity against amastigote forms of Trypanosoma cruzi Tulahuen C4 assessed as inhibition of growth2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1074380Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by propidium iodide/fluorescein diacetate staining-based flow cytometric analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID726609Inhibition of Toxoplasma gondii farnesyl diphosphate synthase assessed as incorporation of [4-14C]IPP measured at 37 degC2013European journal of medicinal chemistry, Feb, Volume: 60Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.
AID1432878Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigote forms harboring LacZ infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric method2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and activity of nucleoside-based antiprotozoan compounds.
AID580600Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as occurrence of subpatent parasitemia level in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 4 to 242009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
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.
AID1613538Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 16 post 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID537131Antileishmanial activity against amastigotes of Leishmania chagasi MHOM/BR/1972/LD after 24 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1074379Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for epimastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN32014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID1615015Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1854935Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth inhibition measured after 72 hrs by hemocytometer chamber based analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1456724Antiparasitic activity against Trypanosoma cruzi infected in human assessed as cure rate under acute condition2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases.
AID1603873Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum urea level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 70 post inf2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1420624Trypanocidal activity against Trypanosoma cruzi Tulahuen trypomastigotes infected in human THP1 cells assessed as growth inhibition after 48 hrs by chlorophenolred-beta-d-galactopyranoside/Nonidet P-40 reagent-based assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus.
AID576104Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Aphthous stomatitis at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID576089Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Anorexia at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1682937Cardiac toxicity in BALB/c mouse infected with blood trypomastigote form of Trypanosoma cruzi strain Y assessed as CK-MB level in plasma at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-infection and measured on 16th day2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1254024Antiparasitic activity against trypomastigote form of Trypanosoma cruzi Y strain assessed as parasite viability at 62.5 to 500 uM incubated for 24 hrs2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi.
AID1361364Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood assessed as parasite lysis at 10 ug/ml after 24 hrs by optical microscopic method relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.
AID1615124Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID537130Antileishmanial activity against promastigotes of Leishmania chagasi MHOM/BR/1972/LD after 18 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1687704Selectivity index, ratio of CC50 African green monkey Vero cells to IC50 for Trypanosoma cruzi epimastigotes2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1290516Cytotoxicity against human THP1 cells assessed as cell viability after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID1616175In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily for 5 days with 2 days interval for 3 cycles and measured up to 30 days pos2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1519009Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as adipocytes replacement in skeletal muscle by measuring number of adipocyte at 30 mg/kg/day, po administered via gavage for 30 consecutive days 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID284136Trypanocidal activity in Swiss albino mouse inoculated with Trypanosoma cruzi Y blood trypomastigotes assessed as parasitaemia reduction administered after 7th day of inoculation at 250 mg/kg, po after 4 hrs relative to control2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Synthesis and trypanocidal activity of ent-kaurane glycosides.
AID1603951Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on L-alanine excretion at IC50 after 72 hrs by H NMR method relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID710590Selectivity index, ratio of IC50 for rat L6 cells to IC50 for intracellular amastigote form of Trypanosoma cruzi Tulahuen strain C2C42012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
AID1712839Antiparasitic activity against Trypanosoma cruzi Y strain trypomastigotes assessed as reduction in parasite viability after 24 hrs by Neubauer chamber counting method2016European journal of medicinal chemistry, Oct-04, Volume: 121New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.
AID603333Antitrypanosomal activity against bloodstream trypomastigote form of Trypanosoma cruzi Y isolated from albino mouse blood after 24 hrs2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Synthesis and anti-Trypanosoma cruzi activity of β-lapachone analogues.
AID1054891Trypanocidal activity against intracellular amastigote stage of Trypanosoma cruzi CL-B5 infected in mouse NCTC-929 cells assessed as reduction of parasite load after 7 days by resazurin dye-based fluorometric analysis2013Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22
In vitro and in vivo antileishmanial and trypanocidal studies of new N-benzene- and N-naphthalenesulfonamide derivatives.
AID1498185Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615026Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1584761Trypanocidal activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Swiss mouse cardiac cells assessed as parasite death after 24 hrs by neubauer chamber based light microscopy2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1683718Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) epimastigote form assessed as parasite growth inhibition incubated for 48 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID693340Growth inhibition of epimastigote form of Trypanosoma cruzi CL-B5 at 128 uM after 72 hrs by lacZ reporter gene assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1687714Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as well-groomed fur and alert at 10 mg/kg, po treated 10 days post infection measured on day 192020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1198535Trypanocidal activity against GFP expressing Trypanosoma cruzi Y C57BL/6J mouse acute model of trypanosomal infection assessed as reduction in cardiac amastigote nests counts at 100 mg/kg/day, ip measured at 10,14 and 20 days post infection by HE staining2015European journal of medicinal chemistry, Mar-26, Volume: 93Computer-guided drug repurposing: identification of trypanocidal activity of clofazimine, benidipine and saquinavir.
AID1615078Toxicity in Balb/c mouse assessed as death at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID675025Trypanocidal activity against epimastigotes of Trypanosoma cruzi Tulahuen 2 assessed as inhibition of parasite growth after 4 days by trypan blue staining2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents.
AID396580Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Pyrimido[1,2-a]quinoxaline 6-oxide and phenazine 5,10-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi.
AID558399Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity.
AID677293Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as necrotic cells in portal tracts at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1578098Antitrypanosomal activity against Trypanosoma brucei rhodesiense2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Antiprotozoal alkaloid principles of the plant family Amaryllidaceae.
AID1196784Antichagasic activity against trypomastigote stage of Trypanosoma cruzi Brazil infected in Balb/c mouse assessed as reduction of parasite index at 15 mg/kg/day, ip measured after 10 days by luciferase reporter gene assay relative to control2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1565128Trypanocidal activity against luciferase expressing Trypanosoma cruzi Dm28c trypomastigotes isolated from infected Vero cells assessed as reduction in parasite viability after 24 hrs by luciferase-luminescence assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID577156Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as reduction in reduction in parasite induced histopathological changes in skeletal muscle at 60 mg/kg/day, po for 6 days per week until completion of 60 compound d2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
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.
AID1616188In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as reduction in parasitemia at 100 mg/kg, po administered once daily for 5 days with 2 days interval for 3 cycles in presence of cyclophosphamid2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID730419Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
AID1487118Selectivity index, ratio of CC50 for cytotoxicity against mouse J774 cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Queretaro epimastigotes2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and biological evaluation of 2-methyl-1H-benzimidazole-5-carbohydrazides derivatives as modifiers of redox homeostasis of Trypanosoma cruzi.
AID396024Antimicrobial activity against Trypanosoma cruzi Bug2148 cl1 and Trypanosoma cruzi MAS cl11 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1254441Antiparasitic activity against amastigote stage of Trypanosoma cruzi Y in BALB/c mouse macrophages assessed as decrease in number of intracellular amastigotes incubated for 6 hrs by Giemsa staining-based optical microscopic analysis2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID597236Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss albino mouse assessed as increase of mouse survival days at 50 mg/kg/day, po relative to control2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.
AID677291Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as intestinal hemorrhage at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1272502Trypanocidal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes at 25 uM after 5 days2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity.
AID1603815Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 assessed as survival in presence of Sprague-Dawley rat liver S9 fraction metabolic activation by SOS/umu assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1238022Selectivity index, ratio of EC50 for BALB/c mouse peritoneal macrophages to EC50 for Leishmania amazonensis MPRO/BR/1972/M1841-LV-79 amastigotes2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1615022Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603755Antitrypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 1 epimastigotes measured after 72 hrs by Neubauer hemocytometer2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1518994Toxicity in C3H/HeNk mouse infected with Trypanosoma cruzi K98 bloodstream form assessed as decrease in body weight at 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection measured at 150 days post infectio2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1773690Cytotoxicity against mouse C2C12 cells2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
Structure-Based Optimization of Quinazolines as Cruzain and
AID1686732Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigote forms infected in African green monkey Vero cells incubated for 72 hrs by Giemsa staining based micrscopy2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1422890Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c trypomastigotes infected in African green monkey Vero cells2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID1695264Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability
AID1638042Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 amastigotes infected in African green monkey Vero cells2019European journal of medicinal chemistry, Mar-01, Volume: 165Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity.
AID1613480Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1498245Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in stomach tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days star2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1507198Selectivity index, ratio of IC50 for mouse NCTC-929 cells to IC50 for Trypanosoma cruzi clone CL B5 epimastigotes2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID1565131Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for luciferase expressing Trypanosoma cruzi Dm28c trypomastigotes isolated from infected Vero cells2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1202576Selectivity index, ratio of IC50 for human LL24 cells to IC50 for Trypanosoma cruzi Y epimastigote forms2015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1518993Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as reduction in parasite burden in cardiac muscle at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1584763Cytotoxicity against Swiss mouse embryonic cardiomyocytes assessed as reduction in cell viability after 24 hrs by prestoblue-staining based colorimetry2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID601812Trypanocidal activity against Trypanosoma cruzi Y epimastigotes after 72 hrs by MTT assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Absolute configuration and selective trypanocidal activity of gaudichaudianic acid enantiomers.
AID1683694Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in BALB/c mouse assessed as reactivation parasitaemia at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured up to 2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1615088Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 127 p2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1383435Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Swiss Webster mouse assessed as reduction in parasitemia at 100 mg/kg, po administered daily on day 5 to 9 post infection relative to control2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1439205Antitrypanosomal activity against Trypanosoma cruzi Y amastigote forms infected in human U2OS cells after 96 hrs by Draq5 staining-based high content analysis2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols.
AID576096Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Gastrointestinal disorders at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1686757Antitrypanosomal activity against Trypanosoma cruzi Arequipa trypomastigotes infected in BALB/c mouse assessed as reduction in mouse mortality measured during acute phase (days 0 to 40 post infection) at 50 to 100 mg/kg, po dosed on alternating days (7 to2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1403403Trypanocidal activity against Trypanosoma cruzi Dm28c trypomastigotes infected in monkey LLC-MK2 cells after 24 hrs by luminescent assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID344433Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.1 mM after 24 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID337147Antitrypanosomal activity against Trypanosoma cruzi Y after 48 hrs
AID1615048Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free adipose tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infect2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1616183Cytotoxicity against mouse L929 cells assessed as reduction in cell viability2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1615018Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID373283Antitrypanosomal activity against Trypanosoma cruzi bloodstream trypomastigote infected in BALB/c mouse assessed as antibodies at 50 mg/kg, po after 30 days by colorimetric method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In vitro and in vivo antitrypanosomatid activity of 5-nitroindazoles.
AID1480891Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes measured after 4 to 5 days by neubauer chamber method2017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID1687777Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in African green monkey Vero cells assessed as increase in parasite lysis measured after 24 hrs by Neubauer chamber method2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID1498209Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 p2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1290518Selectivity index, ratio of CC50 for human THP1 cells to IC50 for Trypanosoma cruzi Tulahuen2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID547510Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Y assessed as production of antibody IgG at 12 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID382236Trypanocidal activity against Trypanosoma cruzi Y blood stream trypomastigotes after 24 hrs2008Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9
Synthesis and anti-Trypanosoma cruzi activity of derivatives from nor-lapachones and lapachones.
AID776295Antimicrobial activity against Trypanosoma cruzi RA amastigotes infected in African green monkey Vero cells assessed as growth inhibition at 1 ug/ml after 72 hrs by Giemsa staining-based light microscopy2013European journal of medicinal chemistry, Nov, Volume: 69Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi.
AID317066Antiparasitic activity against Trypanosoma cruzi epimastigotes after 72 hrs2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings.
AID1459245Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as maximal parasite density at 1 to 15 uM supplemented with fresh medium containing compound every 9 to 10 days measured on third week by haemocytometric method2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID1498251Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection mea2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1683672Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on ALP level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1851973Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells assessed as inhibition of parasite growth incubated for 48 hrs by Hoechst 3348 staining based analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1244469Trypanocidal activity against intracellular amastigotes of Trypanosoma cruzi Tulahuen infected in human U937 cells assessed as reduction of viability of intracellular amastigotes by measuring beta-galactosidase activity at 20 ug/ml after 72 hrs by spectro2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids.
AID1633353Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes assessed as reduction in epimastigotes number after 48 hrs by resazurin dye based spectrophotometric method
AID576086Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Hyperpigmentation at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID323757Antiparasitic activity against Trypanosoma cruzi Y epimastigote2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
AID669302Selectivity ratio of CC50 for monkey LLC-MK2 cells to IC50 for Trypanosoma cruzi Y amastigotes2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID1287595Antiparasitic activity against nifurtimox-sensitive amastigote stage of Trypanosoma cruzi tulahuen CL2 infected in human MRC5 cells2016European journal of medicinal chemistry, May-04, Volume: 113In vitro screening of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives as antiprotozoal agents and docking studies on Trypanosoma cruzi CYP51.
AID1496047Cytotoxicity against Swiss Webster mouse cardiomyocyte assessed as reduction in cell viability after 24 hrs by PrestoBlue assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID1633354Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as reduction in epimastigotes resazurin dye based spectrophotometric method assay
AID1294229Antichagasic activity against Trypanosoma cruzi Y strain epimastigotes in mouse cardiomyocytes assessed as growth inhibition after 48 hrs by resazurin assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1278152Selectivity index, ratio of CC50 for mouse NCTC-292 cells to IC50 for Trypanosoma cruzi Y trypomastigotes2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.
AID1613477Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID753409Trypanocidal activity against Trypanosoma cruzi Y trypomastigotes infected in human HeLa cells at 4 degC after 18 hrs by hemocytometric analysis2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID1498317Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1156610Antiparasitic activity against chloroquine-resistant Plasmodium falciparum K1 after 3 days by [3H]-hypoxanthine incorporation assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID1615060Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection mea2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1074923Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in African green monkey Vero cells assessed as reduction in number of trypomastigotes at IC25 treated for 12 hrs followed by compound-washout measured after 10 days by micros2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1191152Antitrypanosomal activity against epimastigote stage of Trypanosoma cruzi Y after 96 hrs by hemocytometry2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents.
AID302069Reduction of Trypanosoma cruzi Y amastigotes infection in Vero cells at 25 uM after 48 hrs2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides.
AID726226Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 32 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID155965Cytotoxicity against peritoneal macrophages of female CD1 mice culturing amastigote stages of Leishmania donovani; no data2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID576087Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Erythema nodosum at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1603880Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum aspartate aminotransferase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID666684Cytotoxicity against mouse J774 cells after 18 hrs by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.
AID1420626Selectivity index, ratio of CC50 for human THP1 cells to G150 for Trypanosoma cruzi Tulahuen trypomastigotes2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus.
AID1603823Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free oesophagus in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1682934Hepatotoxicity in BALB/c mouse infected with blood trypomastigote form of Trypanosoma cruzi strain Y assessed as AST level in plasma at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post-infection and measured on 16th day pos2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID263378Antitrypanosomal activity against Trypanosoma cruzi epimastigotes at 1 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID728167Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in monkey LLC-MK2 cells after 48 to 72 hrs by beta-galactosidase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID1480893Selectivity index, ratio of highest non-cytotoxic concentration for mouse J774A.1 cells to CC50 for bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells2017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID1244585Antiparasitic activity against trypomastigotes of Trypanosoma cruzi Y assessed as induction of parasite death at 5 uM after 24 hrs using propidium iodide staining after 24 hrs by flow cytometry analysis2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID694793Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction of parasite level in blood at 100 mg/kg, po administered after 5 days of postinfection qd for 5 days2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice.
AID564081Antitrypanosomal activity against Trypanosoma cruzi 958 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1608335Anti-parasitic activity against trypomastigotes form of Trypanosoma cruzi after 24 hrs2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis of quinones with highlighted biological applications: A critical update on the strategies towards bioactive compounds with emphasis on lapachones.
AID596807Cytotoxicity against african green monkey Vero cells assessed as cell viability after 72 hrs by FACS analysis2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID644366Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes infected in rat L6 myoblasts after 96 hrs by CPRG/Nonidet-based spectrophotometry2012Bioorganic & 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.
AID1613548Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID313539Antitrypanosomal activity against Trypanosoma cruzi Tulahuen epimastigotes after 72 hrs2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Leishmanicidal and trypanocidal activities of 2-aminocyclohexanol and 1,2-cyclohexanediamine derivatives.
AID671576Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen infected immunosuppressed Swiss mouse assessed as level of parasite in blood at 100 mg/kg, po administered 8 day after post infection qd for 20 days measured after 3 cycles of2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1687707Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as reduction in parasitemia at 10 mg/kg, po treated 10 days post infection for 7 consecutive days by Neubauer chamber counting method relative to control2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1400238Selectivity index, ratio of CC50 for human THP1 cells to GI50 for Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Synthesis and SAR of new isoxazole-triazole bis-heterocyclic compounds as analogues of natural lignans with antiparasitic activity.
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.
AID1613526Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 127 p2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1706426Antitrypanosomal activity against bloodstream trypomastigotes form of Trypanosoma cruzi CL Brener infected in BALB/c mouse assessed as reduction in parasitemia at 100 mg/kg, po qd administered for 5 days starting from day 114 post infection followed by cy2020European journal of medicinal chemistry, Dec-01, Volume: 207Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
AID1154402Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y infected in BALB/c mouse peritoneal macrophages assessed as inhibition of host cell invasion at 10 uM after 2 hrs by hematoxylin/eosin staining-based optical microscopic analysi2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
AID247798Trypanocidal activity against amastigote forms of Y strain of Trypanosoma cruzi2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
AID1683674Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on ALT/GPT level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID373281Toxicity in BALB/c mouse assessed as survival fraction at 50 mg/kg, po after 9 weeks2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In vitro and in vivo antitrypanosomatid activity of 5-nitroindazoles.
AID564747Toxicity in male Swiss-Webster mouse assessed as weight loss at cumulative dose of 200 mg/kg, ip measured after 48 hrs2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID669382Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi after 72 hrs by MTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
AID1070012Cytotoxicity against mouse NCTC-929 cells after 48 hrs by resazurin staining-based fluorescence assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1687778Antitrypanosomal activity against Trypanosoma cruzi Y axenic amastigotes infected in African green monkey Vero cells after 24 hrs by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID1496044Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse L929 cells after 96 hrs by beta galactosidase reporter assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID575890Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of polyneuritis on 4th week of treatment2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1612899Antimicrobial activity against Trypanosoma cruzi Y infected in human U2OS cells after 96 hrs by HCS assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Discovery of new potent hits against intracellular Trypanosoma cruzi by QSAR-based virtual screening.
AID1678866Cytotoxicity against albino Swiss mouse peritoneal macrophages assessed as reduction in cell viability incubated for 24 hrs by Presto blue assay2020RSC medicinal chemistry, Oct-01, Volume: 11, Issue:10
Synthesis of quinone imine and sulphur-containing compounds with antitumor and trypanocidal activities: redox and biological implications.
AID1569975Selectivity index, ratio of maximum non-toxic concentration for Balb/c mouse splenocyte to IC50 for bloodstream form of Trypanosoma cruzi trypomastigotes2019European journal of medicinal chemistry, Oct-15, Volume: 1802-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity.
AID1687701Antitrypanosomal activity against bloodstream Trypanosoma cruzi trypomastigotes measured after 24 hrs by Neubauer chamber method2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1498177Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID576079Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Dermatological disorder at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID564757Antitrypanosomal activity against Trypanosoma cruzi Y bloodstream forms infected in Swiss-Webster mouse assessed as survival of mouse at 100 mg/kg/day, ip administered 8 days postinfection measured on day 1202010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1615047Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free stomach at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection fol2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID677311Trypanosomicidal activity against Trypanosoma cruzi epimastigotes assessed as change in succinate metabolite excretion after 96 hrs by NMR analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1498205Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection meas2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1403394Therapeutic index, ratio of CC50 for African green monkey Vero cells to IC50 for infected Swiss Webster mouse derived bloodstream form of Trypanosoma cruzi Y2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1624251Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 3 days by resazurin dye-based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1683681Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on total bilirubin level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatme2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1687705Selectivity index, ratio of CC50 African green monkey Vero cells to IC50 for Trypanosoma cruzi trypomastigotes2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1633361Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c trypomastigotes infected in African green monkey Vero cells
AID1669164Antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in rat H9C2 cells after 72 hrs by Hoechst 33342 staining based fluorescence microscopy2020ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from
AID1615095Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1070013Cytotoxicity against mouse NCTC-929 cells at 256 uM after 48 hrs by resazurin staining-based fluorescence assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1603882Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum alanine aminotransferase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting fr2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID677212Trypanosomicidal activity against Trypanosoma cruzi infected in Vero cells assessed as reduction in rate of infection after 10 days by Giemsa staining method2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID536029Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y assessed as viability at 40 uM after 7 days by trypan blue exclusion assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID710878Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 11 days2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID1686740Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Arequipa trypomastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID576098Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Nausea at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1613532Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1603838Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum aspartate aminotransferase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID576080Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Urticaria at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID707776Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/VO/2008/SN3 blood trypomastigotes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1074381Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as parasite growth inhibition after 72 hrs by Giemsa staining-based microscopic analysis2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID575886Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of arthralgias2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1615027Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypomastigotes derived from infected Balb/c mouse2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1498188Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypamastigotes derived from infected Balb/c albino mouse2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1508574Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Balb/c mouse macrophages assessed as reduction in number of intracellular amastigotes at 0.5 uM measured after 3 days by hoeschst staining based confocal2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1739883Antitrypanosomal activity against Trypanosoma cruzi (MHOM/CH/00/Tulahuen C2, lacZ) amastigotes infected in HFF-1 cells assessed as reduction in parasite growth at 300 uM incubated for 120 hrs by CPRG/Igepal substrate based photometric method relative to c2020European journal of medicinal chemistry, Sep-01, Volume: 201Discovery of highly potent and selective antiparasitic new oxadiazole and hydroxy-oxindole small molecule hybrids.
AID1753504Toxicity in Swiss webster mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as animal survival at 100 mg/kg, po qd for 5 days treatment started at 6 days post-infection and measured at 34 days post-infection2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID1507199Antitrypanosomal activity against Trypanosoma cruzi clone CL B5 amastigotes harboring lacZ infected in mouse NCTC-929 cells after 7 days by beta-galactosidase reporter gene assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID1165090Antiparasitic activity against trypomastigote forms of Trypanosoma cruzi Tulahuen C2C4 infected in rat L6 cells assessed as inhibition of growth after 96 hrs by inverted microscopy2014European journal of medicinal chemistry, Nov-24, Volume: 87Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
AID392023Toxicity against Trypanosoma cruzi Colombiana infected Swiss mouse assessed as mouse survival at 120 mg/kg/day, po after 25 days2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1603835Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum uric acid level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 post i2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1543107Selectivity index, ratio of CC50 for cytotoxicity in mouse NCTC-929 cells to EC50 for Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in LLC-MK2-ATCC CCL7 cells2019Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12
Structure-activity relationship study of antitrypanosomal chalcone derivatives using multivariate analysis.
AID1740563Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID1498180Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypamastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1503433Selectivity index, ratio of LC50 for cytotoxicity in human U937 cells to EC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen intracellular amastigotes transfected with beta-galactosidase infected in human U937 cells2017European journal of medicinal chemistry, Dec-01, Volume: 141Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities.
AID1518996Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as change in QRS morphology at 30 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measured 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1254025Antiparasitic activity against amastigote form of Trypanosoma cruzi Y strain infected in bone marrow macrophage cells assessed as amastigote viability incubated for 4 days by rapid panoptic stain based microscopy method2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi.
AID1603739Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 assessed as umu gene induction in absence of Sprague-Dawley rat liver S9 fraction metabolic activation by SOS/umu assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1603767Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa; DTU 5 amastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1375932Parasiticidal activity against amastigote stage of Trypanosoma cruzi Tulahuen infected in mouse brain fibroblast assessed as time duration of effect at 9.6 microM preincubated for 5 days followed by another 10 days incubation with fresh compound2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
NMR Biochemical Assay for Oxidosqualene Cyclase: Evaluation of Inhibitor Activities on Trypanosoma cruzi and Human Enzymes.
AID343557Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Tulahuen 22008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle.
AID1228663Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y assessed as inhibition of cell viability after 24 hrs by MTT assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Anti-parasitic Guanidine and Pyrimidine Alkaloids from the Marine Sponge Monanchora arbuscula.
AID1615119Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID252103In vivo percent inhibition of compound at a dose of 45 mg/kg, p.o., for 5 doses in rodent model with Trypanosoma brucei brucei STIB 795 strain [ND = not determined]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.
AID564734Antitrypanosomal activity against Trypanosoma cruzi MS1523 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1603827Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free muscle in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID392018Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected Swiss mouse assessed as prevention of liver congestion at 200 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1615057Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection mea2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID597246Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss albino mouse assessed as reduction of microbial antibody level at 50 mg/kg/day, po by Wilconxon test2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.
AID1683687Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on urea level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
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.
AID563559Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss-Webster mouse assessed as decrease in parasite-induced weight loss at 100 mg/kg/day, ip administered 5 days post-infection for 10 consecutive days measured on day 1202010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID564767Hepatotoxicity in Swiss-Webster mouse assessed as increased GPT level at 100 mg/kg/day, ip administered 21 days postinfection measured on day 1202010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1603766Trypanocidal activity against Trypanosoma cruzi trypomastigote form infected in African green monkey Vero cells assessed as ratio of infected cells at 25 uM measured after 72 hrs by Giemsa staining based assay relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1811312Selectivity index, ratio of CC50 for mouse J774.2 cells to IC50 for Trypanosoma cruzi ITRI/MX/2018/TH2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID677205Trypanosomicidal activity against Trypanosoma cruzi SN3 epimastigote after 72 hrs by hemocytometric analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1851974Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells assessed as reduction in parasite growth at Emax concentration incubated for 48 hrs by Hoechst 3348 staining based analysis2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1603743Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasitemia reactivation in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting from2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID548280Antimicrobial activity against Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1536892Antitrypanosomal activity against beta-galactosidase expressing nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as reduction in parasite burden after 168 hrs by CPRG and Nonidet based spectrophotometric analys2019Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4
Synthesis and antimicrobial activities of N
AID726227Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 64 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1697062Selectivity index, ratio of CC50 for mouse peritoneal macrophages to IC50 for Trypanosoma cruzi amastigotes infected in BALB/c mouse peritoneal macrophages2020Journal of natural products, 09-25, Volume: 83, Issue:9
Production of Highly Active Antiparasitic Compounds from the Controlled Halogenation of the
AID1403389Cytotoxicity activity against Swiss Webster mouse primary hepatocytes assessed as reduction in cell viability after 72 hrs by cell-titer-glo assay2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID576835Antitrypanosomal activity against trypomastigote of Trypanosoma cruzi infected in BALB/c mouse assessed as increase of host survival at 1 mg/kg, ip for 5 days administered 7 days after infection2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1615050Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free brain at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID344438Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss mouse assessed as decrease in parasitemia at 385 umol/kg, po after 15 consecutive days2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID580668Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as reactivation of parasite in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1329380Selectivity index, ratio of CC50 for mouse NCTC-929 cells to IC50 for Leishmania infantum MHOM/BR/1972/LD amastigote forms infected in BALB/c mouse macrophages2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID753407Trypanocidal activity against Trypanosoma cruzi H510 trypomastigotes infected in human HeLa cells at 37 degC after 18 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID1615044Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free lungs at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1070015Antimicrobial activity against epimastigote stage of Trypanosoma cruzi CL Brener assessed as growth inhibition at 256 uM after 72 hrs by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID1603816Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 assessed as survival in absence of Sprague-Dawley rat liver S9 fraction metabolic activation by SOS/umu assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID714975Antitrypanosomal activity against bloodstream trypomastigote form of Trypanosoma cruzi NINOA isolated from infected mouse at the peak of parasitemia assessed as reduction in parasite motility at 5 to 50 ug/ml after 24 hrs2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Identification of benzoylisoquinolines as potential anti-Chagas agents.
AID1686745Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi NS3 amastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1613478Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes derived from infected Balb/c albino mouse2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1613496Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free bone marrow at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID337141Antitrypanosomal activity against Trypanosoma cruzi C8 CL1 after 48 hrs
AID693344Growth inhibition of epimastigote form of Trypanosoma cruzi CL-B5 at 64 uM after 72 hrs by lacZ reporter gene assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1613471Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypomastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1615020Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypomastigotes derived from infected Balb/c mouse after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1383423Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigote forms infected in mouse L929 cells assessed as reduction in parasite load after 96 hrs by beta-galactosidase reporter gene assay2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1613527Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID396581Antitrypanosomal activity against Trypanosoma cruzi CL Brener epimastigotes2008European journal of medicinal chemistry, Aug, Volume: 43, Issue:8
Pyrimido[1,2-a]quinoxaline 6-oxide and phenazine 5,10-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi.
AID1454628Antitrypanosomal activity against bioluminescent PpyRE9h expressing Trypanosoma cruzi Tulahuen tryptomastigotes infected subcutaneously in BALB/c mouse assessed as suppression of Trypanosoma cruzi infection at 100 mg/kg, po qd administered for 5 days meas2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
New Class of Antitrypanosomal Agents Based on Imidazopyridines.
AID576101Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Heartburn at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID324607Effect on oxygen uptake per mg of protein in Trypanosoma cruzi Tulahuen epimastigotes relative to control2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Trypanosoma cruzi: activities of lapachol and alpha- and beta-lapachone derivatives against epimastigote and trypomastigote forms.
AID324608Effect on oxygen redox cycling in Trypanosoma cruzi Tulahuen assessed as oxygen consumption per mg of protein relative to control2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Trypanosoma cruzi: activities of lapachol and alpha- and beta-lapachone derivatives against epimastigote and trypomastigote forms.
AID1517431Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi CL Brener infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID1613570Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1507435Antitrypanosomal activity against bloodstream forms of Trypanosoma cruzi Y isolated from parasite infected Albino Swiss mouse assessed as induction of parasite lysis incubated for 24 hrs by Neubauer chamber based cell counting method2017European journal of medicinal chemistry, Aug-18, Volume: 136Rhodium-catalyzed C-H bond activation for the synthesis of quinonoid compounds: Significant Anti-Trypanosoma cruzi activities and electrochemical studies of functionalized quinones.
AID1615039Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free adipose tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infect2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1351071Antitrypanosomal activity Trypanosoma cruzi Bug 2149 cl10 Tc5 epimastigotes measured after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID1244578Antitrypanosomal activity against amastigote and trypomastigote forms of Trypanosoma cruzi Tulahuen expressing beta-galactosidase gene infected in mouse L-929 cells assessed as inhibition of parasite growth after 7 days by colorimetric betagalactosidase a2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1277886Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse C3H cells after 72 hrs by microplate reader analysis2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Semisynthesis of new aphidicolin derivatives with high activity against Trypanosoma cruzi.
AID1264450Selectivity index, ratio of IC50 for rat L6 cells to IC50 for epimastigote stage of Trypanosoma cruzi MHOM/ES/2203/BCN5902015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1587053Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells assessed as relapse time at 25 times EC50 supplemented with fresh medium containing compound every 4 days for 16 days followed by compound washout and mea2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID404373Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C2C42008Journal 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.
AID707782Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 intracellular amastigotes infected in african green monkey Vero cells incubated for 72 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID564733Antitrypanosomal activity against Trypanosoma cruzi 960 epimastigotes after 24 hrs by light microscopy2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1615051Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free oesophagus at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1498193Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 up to 0.5 mg/ml by SOS/umu assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615129Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1174782Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for intracellular amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN32015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1849823Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in Swiss Webster mouse assessed as reduction in viable parasite in blood incubated for 24 hrs by Neubauer counting chamber based light microscopic analysis2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
AID1140922Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes assessed as growth inhibition after 5 days2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.
AID287513Inhibition of Trypanosoma cruzi Maracay epimastigotes after 72 hrs2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
1,4-Bis(alkylamino)benzo[g]phthalazines able to form dinuclear complexes of Cu(II) which as free ligands behave as SOD inhibitors and show efficient in vitro activity against Trypanosoma cruzi.
AID1615036Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in parasitaemia level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection meas2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1154400Cytotoxicity against BALB/c mouse peritoneal macrophages after 72 hrs by AlamarBlue assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
AID1613572Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1683712Antitrypanosomal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen (DTU VI) amastigote form infected in Vero cells assessed as parasite growth inhibition incubated for 72 hrs by Giemsa-staining based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1275380Antitrypanosomal activity against epimastigote stage of Trypanosoma cruzi Dm28c after 72 hrs by resazurin dye based microplate reader analysis2016European journal of medicinal chemistry, Feb-15, Volume: 109New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease.
AID1383431Cytotoxicity against Swiss Webster mouse cardiac cells assessed as reduction in cell viability after 24 hrs by light microscopic analysis2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1361012Antiparasitic activity against trypomastigote form of Trypanosoma cruzi assessed as parasite lysis after 24 hrs by Pizzi-Brener method2018European journal of medicinal chemistry, Jul-15, Volume: 155Symmetrical and unsymmetrical substituted 2,5-diarylidene cyclohexanones as anti-parasitic compounds.
AID1879401Antitrypanosomal activity against Trypanosoma cruzi Y strain infected in acute CD Swiss Webster mouse model assessed as reduction in parasitemia at 100 mg/kg, po qd for 5 consecutive days by light microscopy relative to control2022European journal of medicinal chemistry, Mar-05, Volume: 231N
AID547277Antitrypanosomal activity against Trypanosoma cruzi Y infected in mongrel dog assessed as reduction in INFgamma production in right atrium at 12 mg/kg, po BID after 180 days by semiquantitative RT-PCR2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1498235Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in spleen tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days start2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID656217Cytotoxicity against african green monkey Vero cells at 6.25 uM after 3 days2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Phosphonium lipocations as antiparasitic agents.
AID1498298Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 post2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1074921Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in BALB/c mouse assessed as reduction in parasitemia at 1 mg/kg/day, ip treated from day 5 to day 10 post-infection measured on day 30 post-infection relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1074373Trypanocidal activity against metacyclic trypomastigote stage of Trypanosoma cruzi infected in BALB/c albino mouse acute chagas disease model assessed as reduction of parasite burden at 25 mg/kg, ip administered on day 7 to 12 post-infection measured on d2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID576107Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of degree 1 esophagopathy at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1070008Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 8 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID344424Antitrypanosomal activity against bloodstream trypomastigote of Trypanosoma cruzi Y assessed as number of motile forms after 1 hr by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1486932Antiprotozoal activity against Giardia intestinalis IMSS:0696:1 (genotype A) trophozoites incubated for 48 hrs2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID1277885Cytotoxicity against mouse C3H cells after 72 hrs by MTS assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Semisynthesis of new aphidicolin derivatives with high activity against Trypanosoma cruzi.
AID548283Selectivity ratio of EC50 for Trypanosoma brucei NfxR1 to EC50 for Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID3375Effective concentration required to inhibit the growth of murine 3T3 fibroblasts2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.
AID706518Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 axenic amastigotes infected in african green monkey Vero cells incubated for 72 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1638040Cytotoxicity against African green monkey Vero cells after 72 hrs by propidium iodide/fluorescein diacetate staining based flow cytometry2019European journal of medicinal chemistry, Mar-01, Volume: 165Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity.
AID396017Antimicrobial activity against Trypanosoma cruzi genotype 20 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1686730Antitrypanosomal activity against Trypanosoma cruzi Arequipa trypomastigote froms infected in mouse blood incubated for 24 hrs by Neubauer chamber based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1603818Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free bone marrow in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID580599Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD4+ T-lymphocyte knockout C57BL/6 mouse assessed as occurrence of subpatent parasitemia level in mouse at 20 mg/kg/day, po administered twice daily for 20 consecutive days measured 4 to 242009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1055166Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as hepatic destruction in portal space at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light micros2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID707777Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/VO/2008/SN3 intracellular amastigotes2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID580595Antitrypanosomal activity against Trypanosoma cruzi Y infected in B-lymphocyte knockout C57BL/6 mouse assessed as cure rate in mouse at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 60 days post infection2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1278147Antiparasitic activity against trypomastigote stage of Trypanosoma cruzi Y assessed as parasite viability after 24 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
Gibbilimbol analogues as antiparasitic agents--Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum.
AID1615089Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603826Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free muscle in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 82019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID344430Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 0.1 mM after 4 hrs by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1432289Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Mar-10, Volume: 128Design and synthesis of a new series of 3,5-disubstituted isoxazoles active against Trypanosoma cruzi and Leishmania amazonensis.
AID1603952Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on D-lactate excretion at IC50 after 72 hrs by H NMR method relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
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.
AID1555445Cytotoxicity against mouse NCTC-929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi.
AID1074375Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as reduction of trypomastigote number per mililiter of culture medium at IC25 preincubated for 12 hrs followed by compound washout measured every 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID1420625Trypanocidal activity against Trypanosoma cruzi Tulahuen trypomastigotes infected in human THP1 cells at 20 uM after 48 hrs by chlorophenolred-beta-d-galactopyranoside/Nonidet P-40 reagent-based assay2018Bioorganic & medicinal chemistry letters, 11-01, Volume: 28, Issue:20
Synthesis and biological evaluation of isoxazolyl-sulfonamides: A non-cytotoxic scaffold active against Trypanosoma cruzi, Leishmania amazonensis and Herpes Simplex Virus.
AID1498181Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615054Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free muscle at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection foll2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603848Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum creatine kinase muscle to brain ratio level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID337151Antitrypanosomal activity against Trypanosoma cruzi 31R16CL1 after 48 hrs
AID677288Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as delocalized hepatic destruction at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID766418Selectivity index, ratio of LC50 for mouse NCTC-929 cells to IC50 for amastigotes of Trypanosoma cruzi CL Brener2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1400235Growth inhibition of Trypanosoma cruzi Tulahuen amastigote forms infected in human THP1 cells at 20 uM after 72 hrs by beta-galactosidase reporter gene assay relative to control2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
Synthesis and SAR of new isoxazole-triazole bis-heterocyclic compounds as analogues of natural lignans with antiparasitic activity.
AID753406Trypanocidal activity against Trypanosoma cruzi strain CL trypomastigotes infected in human HeLa cells at 37 degC after 18 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID564766Hepatotoxicity in Swiss-Webster mouse assessed as effect on GPT level at 50 mg/kg/day, ip administered 21 days postinfection measured on day 1202010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1638038Anti-trypanosomal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 epimastigotes after 72 hrs by Neubauer hemocytometric method2019European journal of medicinal chemistry, Mar-01, Volume: 165Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity.
AID1503429Cytotoxicity in human U937 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Triclosan-caffeic acid hybrids: Synthesis, leishmanicidal, trypanocidal and cytotoxic activities.
AID1294225Antichagasic activity against Trypanosoma cruzi CL-B5 intracellular amastigotes in mouse L929 cells assessed as growth inhibition after 7 days by beta galactosidase reporter gene assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Antichagasic and trichomonacidal activity of 1-substituted 2-benzyl-5-nitroindazolin-3-ones and 3-alkoxy-2-benzyl-5-nitro-2H-indazoles.
AID1470751Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID373279Antitrypanosomal activity against Trypanosoma cruzi bloodstream trypomastigote infected in BALB/c mouse assessed as parasitemia at 50 mg/kg, po after 60 days by colorimetric method2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
In vitro and in vivo antitrypanosomatid activity of 5-nitroindazoles.
AID1486933Antiprotozoal activity against Trichomonas vaginalis GT3 trophozoites incubated for 48 hrs2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID1697061Antiparasitic activity against intracellular Trypanosoma cruzi amastigotes infected in mouse peritoneal macrophage measured after 72 hrs2020Journal of natural products, 09-25, Volume: 83, Issue:9
Production of Highly Active Antiparasitic Compounds from the Controlled Halogenation of the
AID449387Inhibition of Mitochondrial dehydrogenase in Trypanosoma cruzi Y epimastigotes at 20 uM after 30 to 240 mins by MTT dye reduction assay in relative to control2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Second generation of 2H-benzimidazole 1,3-dioxide derivatives as anti-trypanosomatid agents: synthesis, biological evaluation, and mode of action studies.
AID1480898Induction of apoptosis in bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells assessed as necrotic cells at 25 uM measured after 24 hrs by Annexin-V-FITC/propidium iodide staining based flow cytometric method (Rvb = 0.2017European journal of medicinal chemistry, Apr-21, Volume: 130Desing and synthesis of potent anti-Trypanosoma cruzi agents new thiazoles derivatives which induce apoptotic parasite death.
AID547248Toxicity in mongrel dog infected with Trypanosoma cruzi Y assessed as weight loss at 7 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 6 months2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1065866Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes after 5 days by resazurin dye-based assay2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Design, synthesis, and evaluation of hydroxamic acid derivatives as promising agents for the management of Chagas disease.
AID1584733Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell viability after 3 days resazurin-based fluorimetric assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID337146Antitrypanosomal activity against Trypanosoma cruzi CL after 48 hrs
AID1780973Trypanocidal activity against Trypanosoma cruzi CL-Luc-Neon amastigotes infected in BSR cells assessed as inhibition of parasite growth at 20 times IC50 incubated for 20 days measured after 30 days of compound wash out by epifluorescence microscopy analys2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID753035Selectivity index, ratio of IC50 for human fibroblasts to GI50 for epimastigote stage of Trypanosoma cruzi Y2013European journal of medicinal chemistry, Jun, Volume: 64Ligand-based design, synthesis, and experimental evaluation of novel benzofuroxan derivatives as anti-Trypanosoma cruzi agents.
AID1496045Cytotoxicity against mouse L929 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID1615092Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603858Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum alkaline phosphatase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days and measured on d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1683683Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on AST/GOT level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1565133Trypanocidal activity against intracellular amastigote stage of Trypanosoma cruzi Y strain infected in Swiss webster cardiac cells assessed as reduction in parasite viability after 24 hrs by Celltiter-Glo assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1638041Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 epimastigotes2019European journal of medicinal chemistry, Mar-01, Volume: 165Design, synthesis and molecular docking studies of novel N-arylsulfonyl-benzimidazoles with anti Trypanosoma cruzi activity.
AID1074932Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) epimastigotes after 72 hrs by Neubauer chamber counting analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1603837Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum creatine kinase muscle to brain ratio level in acute phase at 20 mg/kg/day, po administered for 5 consecutive day2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1614006Antiprotozoal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes infected in rat L6 cells after 96 hrs by inverted microscopic 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.
AID1686733Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigote froms infected in mouse blood incubated for 24 hrs by Neubauer chamber based assay2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID249626Percentage delyse against amastigote forms of Y strain of Trypanosoma cruzi at 32 uM2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
AID1613468Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID396016Antimicrobial activity against Trypanosoma cruzi 1 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1399456Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigote forms infected in rat H9c2 cells assessed as reduction in amastigote number per cell after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.
AID1592303Antitrypanosomal activity against Trypanosoma cruzi MHOM/MX/1994/INC5 epimastigotes assessed as growth inhibition measured after 24 hrs by MTT assay
AID1065867Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as growth inhibition at 32 uM after 5 days by Neubauer chamber counting analysis relative to control2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Design, synthesis, and evaluation of hydroxamic acid derivatives as promising agents for the management of Chagas disease.
AID1615025Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 epimastigotes2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1860609Antitrypanosomal activity against Trypanosoma cruzi infected in Vero cells assessed as relapse day after washout at 50 times EC50 for 8 days followed by washout by microscopic analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.
AID1686725Antitrypanosomal activity against Trypanosoma cruzi infected in African green monkey Vero cells assessed as reduction in infection rate measured up to 10 days by Giemsa staining based hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1686735Antitrypanosomal activity against Trypanosoma cruzi SN3 amastigote forms infected in African green monkey Vero cells incubated for 72 hrs by Giemsa staining based micrscopy2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID598284Antileishmanial activity against Leishmania mexicana MHOM/MX/ISETGS promastigotes after 72 hrs by neubauer chamber2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
AID1361011Antiparasitic activity against epimastigote form of Trypanosoma cruzi Y assessed as parasite growth inhibition after 96 hrs by Neubauer hemocytometer2018European journal of medicinal chemistry, Jul-15, Volume: 155Symmetrical and unsymmetrical substituted 2,5-diarylidene cyclohexanones as anti-parasitic compounds.
AID1498236Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in stomach tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days star2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID575884Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of dermatitis with cutaneous eruptions on day 7 to 102010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID728165Antitrypanosomal activity against Trypanosoma cruzi Y infected in monkey LLC-MK2 cells after 48 to 72 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID1381717Cytotoxicity against human A549 cells after 48 hrs by CellTiter-Glo assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1613472Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes after 48 to 72 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1616181Antitrypanosomal activity against Trypanosoma cruzi Y amastigotes infected in Swiss mouse primary cardiac cells replenished for every 48 hrs for 168 hrs by geimsa staining based assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID677210Selectivity index, ratio of IC50 for Vero cells to IC50 for Trypanosoma cruzi anexic amastigote2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID706519Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 epimastigotes infected in african green monkey Vero cells incubated for 72 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1498343Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on d2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID396015Antimicrobial activity against Trypanosoma cruzi 1 and Trypanosoma cruzi dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID392021Antitrypanosomal activity against Trypanosoma cruzi Colombiana infected Swiss mouse assessed as prevention of skeletal muscle inflammatory infiltrates at 120 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID576105Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Hearing impairment at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1603745Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as reduction in serum Ig-G level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1155759Cytotoxicity against human HepG2 cells after 24 hrs by XTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.
AID1507190Growth inhibition of Trypanosoma cruzi clone CL B5 amastigotes harboring lacZ derived from infected mouse NCTC-929 cells at 25 uM after 7 days by beta-galactosidase reporter gene assay relative to control2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID1615086Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 p2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603740Genotoxicity in Salmonella typhimurium TA1535 harboring pSK1002 assessed as umu gene induction in presence of Sprague-Dawley rat liver S9 fraction metabolic activation by SOS/umu assay2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID214326In Vitro inhibition concentration against Trypomastigote form of Trypanosoma cruzi2000Journal 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.
AID1779354Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 strain amastigotes infected in rat L6 cells measured after 96 hrs by inverted microscopy analysis2021European journal of medicinal chemistry, Oct-05, Volume: 221Synthesis, in vitro antiprotozoal activity, molecular docking and molecular dynamics studies of some new monocationic guanidinobenzimidazoles.
AID1254435Antiparasitic activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y assessed as parasite viability after 24 hrs by Neubauer chamber analysis2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1605625Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 trypomastigotes infected in rat L6 cells incubated for 96 hrs by photometric method based assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Discovery and Optimization of a Compound Series Active against
AID576095Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Paresthesia at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498261Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as decrease in urea level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 162018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1381727Cytotoxicity against human 786-O cells assessed as decrease in mitochondrial viability after 6 hrs by CMXRos staining based assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1456550Cytotoxicity against human U937 cells after 72 hrs by MTT assay
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.
AID576940Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as parasite DNA level at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection measured 30 days post dose by2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1156605Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahen LacZ/C4 amastigotes2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID1454607Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells after 6 days by beta galactosidase reporter asay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
New Class of Antitrypanosomal Agents Based on Imidazopyridines.
AID1740562Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes infected in African green monkey Vero cells incubated for 120 hrs measured on day 6 cells followed by trypomastigotes release by haemocytometer-based light microscopy2020European journal of medicinal chemistry, Sep-15, Volume: 2028-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi.
AID213787Inhibitory concentration against Epimastigotes (Tulahuen strain) of Trypanosoma cruzi2001Bioorganic & medicinal chemistry letters, Oct-22, Volume: 11, Issue:20
Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds.
AID1517430Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi 92.80 cl2 infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID1154398Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y assessed as living parasites level after 24 hrs by Neubauer chamber analysis2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
AID748436Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C2C4 amastigotes infected in rat L6 cells after 96 hrs by photometric analysis2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.
AID1854934Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth inhibition measured after 48 hrs by hemocytometer chamber based analysis2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1587074Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in Balb/c mouse assessed as reduction in infection at 100 mg/kg, po administered once daily for 5 days starting from day 7 post-infection measured on day 13, 17 and 242019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.
AID768695Mutagenicity in Swiss albino mouse at 100 mg/kg after 30 hrs by micronucleus test2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates.
AID1202578Selectivity index, ratio of IC50 for human LL24 cells to IC50 for Trypanosoma cruzi Bug 2149 cl102015European journal of medicinal chemistry, , Volume: 96Designing and exploring active N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients.
AID1518995Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as change in QRS morphology at 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measured 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID287714Antitrypanosomatid activity against Trypanosoma cruzi CL Brener epimastigotes assessed as reduction of growth after 5 days2007Bioorganic & medicinal chemistry, Apr-01, Volume: 15, Issue:7
Second generation of 5-ethenylbenzofuroxan derivatives as inhibitors of Trypanosoma cruzi growth: synthesis, biological evaluation, and structure-activity relationships.
AID1616169In vivo antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss mouse assessed as mouse survival at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection and measured daily up to 402019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID327492Antitrypanosomal activity against Trypanosoma cruzi Y infected in human LLC-MK2 cells after 24 hrs by MTT assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Antiparasitic, antineuroinflammatory, and cytotoxic polyketides from the marine sponge Plakortis angulospiculatus collected in Brazil.
AID1432600Selectivity index, ratio of CC50 for mouse L929 cells to IC50 for Trypanosoma cruzi Tulahuen trypomastigote forms infected in mouse L929 cells2017Bioorganic & medicinal chemistry, 03-15, Volume: 25, Issue:6
Synthesis and biological evaluation of potential inhibitors of the cysteine proteases cruzain and rhodesain designed by molecular simplification.
AID1498182Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 trypamastigotes derived from infected Balb/c albino mouse after 24 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1383441Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Swiss Webster mouse assessed as reduction in parasitemia at 100 mg/kg, po administered daily measured at day 8 post infection2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID613447Cytotoxicity against african green monkey COS7 cells after 24 hrs by MTT assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID382468Therapeutic index, ratio of IC50 for rat L6 cells to IC50 for Plasmodium falciparum K12008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Synthesis and antiprotozoal activities of simplified analogs of naphthylisoquinoline alkaloids.
AID728164Antitrypanosomal activity against Trypanosoma cruzi trypomastigote infected in mouse NIH/3T3 cells at 9.5 uM incubated for 3 days post infection by DAPI-staining based immunofluorescence assay2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Antitrypanosomal lead discovery: identification of a ligand-efficient inhibitor of Trypanosoma cruzi CYP51 and parasite growth.
AID1381691Antitrypanosomal activity against Trypanosoma brucei Lister 427 bloodstream form after 72 hrs by SYBR Green assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1074372Trypanocidal activity against metacyclic trypomastigote stage of Trypanosoma cruzi infected in BALB/c albino mouse acute chagas disease model assessed as inhibition of parasitemia at 25 mg/kg, ip administered on day 7 to 12 post-infection measured every 22014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID362866Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 at 25 uM after 5 days2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
4-nitroacetophenone-derived thiosemicarbazones and their copper(II) complexes with significant in vitro anti-trypanosomal activity.
AID1070004Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 0.5 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID282995Antiparasitic activity against Trypanosoma cruzi MHOM/CL/00/Tulahuan-LacZ intracellular amastigotes2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate.
AID263383Antitrypanosomal activity against Trypanosoma cruzi amastigotes at 10 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID575887Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of lymphadenopathy2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498252Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection mea2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1254922Activity of histidine tagged recombinant Trypanosoma cruzi type 1 nitroreductase assessed as NADH oxidation at 100 uM by spectrophotometry method2015European journal of medicinal chemistry, Oct-20, Volume: 1033-Nitrotriazole-based piperazides as potent antitrypanosomal agents.
AID1498229Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in bone marrow tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days 2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1055188Trypanocidal activity against extracellular epimastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 after 72 hrs by Neubauer hemocytometric analysis2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID766415Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 1 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1244580Selectivity index, ratio of CC50 for mouse L929 cells to IC50 for amastigote and trypomastigote forms of Trypanosoma cruzi Tulahuen2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1124788Antimicrobial activity against epimastigote stage of Trypanosoma cruzi Y after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID1613528Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 post inf2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1683695Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in BALB/c mouse assessed as reactivation parasitaemia at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured up to 142020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1196804Activity of his-tagged recombinant Trypanosoma cruzi type-1 nitroreductase assessed as oxidized NADH level per mg of protein after 5 mins by absorption spectrum analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1683699Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in Vero cells assessed as parasite growth inhibition at 50 uM incubated for 72 hrs by Giemsa-staining based assay relative to control2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1683685Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on CK-MB level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1555444Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BALB/c mouse peritoneal macrophages assessed as decrease in parasitic load with in the cell incubated for 48 hrs by Giemsa staining based light microscopy2019European journal of medicinal chemistry, Aug-15, Volume: 176Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi.
AID707767Toxicity in Trypanosoma cruzi IRHOD/VO/2008/SN3 metacyclic forms infected BALB/c mouse model of acute Chagas disease assessed as mortality incidence at 5 mg/kg/day, ip administered for 5 consecutive days starting on day 7 post infection until day 12 post 2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1486937Antiprotozoal activity against Trypanosoma cruzi MHOM/MX/1994/Ninoa incubated for 72 hrs by Neubauer chamber based cell counting method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID1518969Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as reduction in cardiac tissue inflammation at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post i2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1555446Selectivity index, ratio of CC50 for mouse NCTC-929 cells to IC50 for Trypanosoma cruzi amastigotes infected in BA;B/c mouse peritoneal macrophages2019European journal of medicinal chemistry, Aug-15, Volume: 176Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi.
AID764119Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
5-Nitro-2-furfuriliden derivatives as potential anti-Trypanosoma cruzi agents: design, synthesis, bioactivity evaluation, cytotoxicity and exploratory data analysis.
AID337142Antitrypanosomal activity against Trypanosoma cruzi A98CL5 after 48 hrs
AID249625Percentage delyse against amastigote forms of Y strain of Trypanosoma cruzi at 8 uM2005Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2
Trypanocidal activity of (-)-cubebin derivatives against free amastigote forms of Trypanosoma cruzi.
AID669380Antileishmanial activity against Leishmania amazonensis MPRO/BR/1972/M1841-LV-79 after 72 hrs by MTT assay2012Journal of natural products, May-25, Volume: 75, Issue:5
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
AID323759Antiparasitic activity against Trypanosoma cruzi Y amastigotes2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
AID1501883Cytotoxicity against mouse NCTC-929 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID1459251Trypanocidal activity against Trypanosoma cruzi RA tripamastigote bloodstream forms infected in Balb/c mouse assessed as reduction in parasitaemia at 100 mg/kg, po administered on day 9 post infection for 5 consecutive days measured on day 35 post infecti2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID439873Antimicrobial activity against Trypanosoma cruzi Tulahuen C2C4 amastigote forms infected in rat L6 cells2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
AID1518992Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as reduction in parasite burden in skeletal muscle at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID449369Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes assessed as inhibition of parasite growth after 5 days2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Second generation of 2H-benzimidazole 1,3-dioxide derivatives as anti-trypanosomatid agents: synthesis, biological evaluation, and mode of action studies.
AID1202550Antimicrobial activity against bloodstream trypomastigote stage of Trypanosoma cruzi INC-5 after 24 hrs by Brener method2015European journal of medicinal chemistry, , Volume: 96Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
AID1773692Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 bloodstream forms measured after 72 hrs by SYBR green dye based assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
Structure-Based Optimization of Quinazolines as Cruzain and
AID1613509Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in splenomegaly at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured o2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1196799Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells assessed as parasite growth inhibition after 96 hrs by colorimetric analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID766427Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 4 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1501893Toxicity in BALB/c mouse infected with Trypanosoma cruzi Y assessed as mortality at 100 mg/kg/day, po administered for 10 consecutive days starting on day 5 post infection measured during compound dosing2017European journal of medicinal chemistry, Oct-20, Volume: 139Efficacy of a series of alpha-pyrone derivatives against Leishmania (L.) infantum and Trypanosoma cruzi.
AID1405635Antitrypanosomal activity against luciferase-expressing Trypanosoma cruzi CL Brener infected in Balb/c mouse assessed as reduction in parasitemia at 50 mg/kg, ip bid for 4 days by bioluminescence assay relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents.
AID1603945Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as change in RNA level at IC50 measured after 72 hrs by acridine orange staining based flow cytometry relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1498170Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes after 48 hrs by resazurin dye based assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1811313Antitrypanosomal activity against Trypanosoma cruzi MHOM/MX/1994/Ninoa infected in animal assessed as reduction in viable parasite in blood measured after 24 hrs by neubauer chamber assay2021Bioorganic & medicinal chemistry, 10-15, Volume: 48In vitro, ex vivo and in vivo short-term screening of DHEA nitrate derivatives activity over Trypanosoma cruzi Ninoa and TH strains from Oaxaca State, México.
AID1329381Selectivity index, ratio of CC50 for mouse NCTC-929 cells to IC50 for Trypanosoma cruzi Y trypomastigote form infected in monkey LLC-MK2 cells2016Journal of natural products, 09-23, Volume: 79, Issue:9
Analogues of Marine Guanidine Alkaloids Are in Vitro Effective against Trypanosoma cruzi and Selectively Eliminate Leishmania (L.) infantum Intracellular Amastigotes.
AID1254444Antiparasitic activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in BALB/c mouse assessed as increase in survival rate by measuring mortality at 100 mg/kg, po qd administered for 5 days measured until 30 days2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1055171Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as granuloma with lymphocytic infiltrate at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light micr2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1613552Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1753511Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in Swiss mouse peritoneal macrophages assessed as inhibition of parasite growth measured after 7 days by spectrophotometric analysis2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID575888Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of polyneuropathy on 4th week of treatment2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID725217Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 amastigotes after 96 hrs2013Bioorganic & 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.
AID1244462Cytotoxicity against human U937 cells assessed as cell viability after 72 hrs by MTT assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis, leishmanicidal, trypanocidal and cytotoxic activity of quinoline-hydrazone hybrids.
AID547249Toxicity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as weight loss at 12 mg/kg, po BID for 90 days started 12 to 22 days postinfection measured after 6 months2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1184289Cytotoxicity against human U2OS cells infected with intracellular Trypanosoma cruzi2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a]benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi.
AID1202549Antimicrobial activity against bloodstream trypomastigote stage of Trypanosoma cruzi NINOA after 24 hrs by Brener method2015European journal of medicinal chemistry, , Volume: 96Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
AID445550Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 epimastigotes assessed as parasite growth inhibition after 5 days2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Anti-trypanosomatid benzofuroxans and deoxygenated analogues: synthesis using polymer-supported triphenylphosphine, biological evaluation and mechanism of action studies.
AID401526Antitrypanosomal activity against Trypanosoma cruzi2004Journal of natural products, May, Volume: 67, Issue:5
Ancistrotanzanine C and related 5,1'- and 7,3'-coupled naphthylisoquinoline alkaloids from Ancistrocladus tanzaniensis.
AID343556Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Tulahuen 2 at 25 uM relative to control2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle.
AID1177592Antiparasitic activity against Trypanosoma cruzi Tulahuen C42014Journal of natural products, Aug-22, Volume: 77, Issue:8
Xenortide Biosynthesis by Entomopathogenic Xenorhabdus nematophila.
AID1228665Cytotoxicity against rhesus monkey LLC-MK2 cells assessed as inhibition of cell viability after 48 hrs by MTT assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Anti-parasitic Guanidine and Pyrimidine Alkaloids from the Marine Sponge Monanchora arbuscula.
AID1584732Antiparasitic activity against Trypanosoma cruzi Tulahuen CL2 intracellular amastigotes expressing beta-galactosidase infected in human MRC5 SV2 cells after 7 days by chlorophenol red beta-D-galactopyranoside-based spectrophotometric analysis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID1586958Antitrypanosomal activity against Trypanosoma cruzi MHOM/BR/78/Silvio cloneX10/7A epimastigotes measured after 4 days by resazurin dye based fluorescence assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Nongenotoxic 3-Nitroimidazo[1,2-
AID1281433Induction of apoptosis in trypamostigote form of Trypanosoma cruzi Y assessed as necrotic cells at 25 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry relative to untreated control2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID1498305Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID497467Trypanocidal activity against trypomastigote form of Trypanosoma cruzi Tulahuen infected in rat L6 cells after 96 hrs2010Journal of natural products, Aug-27, Volume: 73, Issue:8
Antiprotozoal steroidal saponins from the marine sponge Pandaros acanthifolium.
AID1156604Antiparasitic activity against Trypanosoma cruzi Tulahen LacZ/C4 amastigotes after 4 days by beta-galactosidase reporter gene assay2014European journal of medicinal chemistry, Aug-18, Volume: 83Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.
AID1498190Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells assessed as infected cells at 50 uM after 72 hrs by Giemsa-staining based microscopic assay relative to control2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1174780Cytotoxicity against african green monkey Vero cells after 72 hrs2015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID1613537Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infect2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1403407Therapeutic index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c intracellular amastigotes infected in African green monkey Vero cells2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1851975Cytotoxicity against mouse 3T3 cells2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1860608Antitrypanosomal activity against Trypanosoma cruzi infected in Vero cells assessed as relapse day after washout at 12.5 times EC50 for 8 days followed by washout by microscopic analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.
AID1613475Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 to 72 hrs by resazurin dye based assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1245580Antiparasitic activity against amastigote stage of Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells assessed as parasite growth inhibition after 96 hrs by beta-galactosidase reporter gene assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID744593Antiprotozoal activity against trypomastigote form of Trypanosoma cruzi Colombian infected in BALB/c mouse assessed as decrease in parasitemia at 100 mg/kg, po administered for 1 week followed by weekly administration measured after 8 months2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
New antiprotozoal agents: their synthesis and biological evaluations.
AID1615058Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection mea2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID537136Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1615059Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post in2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
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.
AID1603830Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as parasite-free stomach in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID596811Antitrypanosomal activity against blood trypomastigote forms of Trypanosoma cruzi infected in BALB/c mouse assessed as mouse survival rate at 1 mg/kg, ip administered 7 days postinfection once daily for 5 days2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID1070007Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 4 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID595452Antiparasitic activity against intracellular amastigotes of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometrically2011Journal of natural products, Apr-25, Volume: 74, Issue:4
Didemnidines A and B, indole spermidine alkaloids from the New Zealand ascidian Didemnum sp.
AID299531Inhibition of Trypanosoma cruzi2007Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
Synthesis and in vitro protozoocidal activity of diazabicyclic benzotropolone derivatives.
AID1683668Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as reduction in weight at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured up to 145 days post infection2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1615121Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID580661Antitrypanosomal activity against Trypanosoma cruzi Y infected in CD8+ T-lymphocyte knockout C57BL/6 mouse assessed as occurrence of low level of circulating parasites at 100 mg/kg/day, po administered once daily for 20 consecutive days measured 15 days p2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Absence of CD4+ T lymphocytes, CD8+ T lymphocytes, or B lymphocytes has different effects on the efficacy of posaconazole and benznidazole in treatment of experimental acute Trypanosoma cruzi infection.
AID1498231Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in esophagus tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days st2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID396589Antitrypanosomal activity against Trypanosoma cruzi CL-B5 amastigotes infected in mouse NCTC-929 fibroblast after 7 days by colorimetric method2008European journal of medicinal chemistry, Sep, Volume: 43, Issue:9
Activity of a hydroxybibenzyl bryophyte constituent against Leishmania spp. and Trypanosoma cruzi: in silico, in vitro and in vivo activity studies.
AID392005Antitrypanosomal activity against Trypanosoma cruzi Colombiana infected Swiss mouse assessed as reduction in circulating trypomastigotes antibody level at 120 mg/kg/day, po after 44 days postinfection2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1074925Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) infected in African green monkey Vero cells assessed as reduction in number of amastigotes at IC25 treated for 12 hrs followed by compound-washout measured after 10 days by microscopi2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID382467Antiplasmodial activity against Plasmodium falciparum K1 infected human erythrocytes after 48 hrs as [3H]hypoxanthine uptake2008European journal of medicinal chemistry, Jan, Volume: 43, Issue:1
Synthesis and antiprotozoal activities of simplified analogs of naphthylisoquinoline alkaloids.
AID1687780Selectivity index, ratio of GI50 for mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay to IC50 for antitrypanosomal activity against Trypanosoma cruzi Y axenic amastigotes infected in African green monkey Ver2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID1074929Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by propidium iodide staining-based flow cytometric analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID155967Cytotoxicity against peritoneal macrophages of female CD1 mice culturing amastigote stages of Trypanosoma cruzi; no data2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID613446Trypanocidal activity against intracellular amastigotes form of Trypanosoma cruzi expressing beta-galactosidase infected in mouse J774 cells on day 72011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID344425Cytotoxicity against chinese hamster V79 cells2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1498239Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in brain tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starti2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1462695Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 intracellular amastigotes infected in rat L6 cells assessed as growth inhibition at 4.8 ug/ml after 96 hrs by CPRG/Nonidet reagent based photometric 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.
AID1498360Induction of mitochondrial membrane potential disruption in Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as inhibition of DNA replication and RNA synthesis at IC25 after 72 hrs by acridine orange staining based flow cytometry relat2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1616127Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based assay2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID766422Cytotoxicity against mouse NCTC-929 cells after 48 hrs by resazurin based fluorescence assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID575891Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of thrombopenic purpura after 2nd week of treatment2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1459247Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as effect on parasite viability at 1 to 15 uM supplemented with fresh medium containing compound every 9 to 10 days measured on third week by maximal parasite density2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID537133Antileishmanial activity against promastigotes of Leishmania major MHOM/1L/80/Fredlin after 18 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID677209Selectivity index, ratio of IC50 for Vero cells to IC50 for Trypanosoma cruzi epimastigote2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1245590Prodrug conversion assessed as Trypanosoma cruzi recombinant type-1 nitroreductase-mediated drug metabolism by measuring NADH oxidation after 5 mins by spectrophotometric analysis2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID547276Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Y assessed as production of antibody IgG2 at 7 mg/kg, po BID for 90 days measured after 6 months by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1603764Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 6 trypomastigote forms infected in BALB/c albino mouse measured after 10 mins by Neubauer chamber method2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
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]
AID213667In vitro growth inhibition of amastigotes of Trypanosoma cruzi2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
Toxic effects of natural piperine and its derivatives on epimastigotes and amastigotes of Trypanosoma cruzi.
AID1238021Anti-leishmanial activity against Leishmania amazonensis MPRO/BR/1972/M1841-LV-79 amastigotes infected in BALB/c mouse peritoneal macrophages assessed as reduction in the infection index incubated for 24 hrs by Giemsa staining method2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1351075Selectivity index, ratio of CC50 for cytotoxicity against human U2OS cells to IC50 for Trypanosoma cruzi Y Tc2 amastigotes infected in human U2OS cells2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID1163253Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID576108Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of dolichocolon at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498176Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1254020Antiparasitic activity against trypomastigote form of Trypanosoma cruzi Tulahuen-lacZ infected in LLC-MK2 ATCC cells assessed as parasite viability incubated for 4 days at 37 degC by chlorophenol beta-D-galactopyranose substrate based trypanocidal assay2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi.
AID1849827Antitrypanosomal activity against bloodstream form of Trypanosoma cruzi Y trypomastigotes infected in albino mouse assessed as reduction in viable parasite in blood by Neubauer counting chamber method2021European journal of medicinal chemistry, Jan-15, Volume: 210A comprehensive review on β-lapachone: Mechanisms, structural modifications, and therapeutic potentials.
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.
AID548109Antiparasitic activity against Trypanosoma cruzi T2 epimastigotes assessed as growth inhibition2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
AID672967Cytotoxicity against african green monkey Vero cells after 72 hrs by spectrophotometric analysis2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
AID1055186Trypanocidal activity against extracellular trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 after 24 hrs by Neubauer hemocytometric analysis2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1682939Antitrypanosomal activity against blood trypomastigote form of Trypanosoma cruzi strain Y infected in BALB/c mouse assessed as reduction in parasite DNA load in host heart at 25 mg/kg, po administered via gavage daily for 15 days starting from 2 days post2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1498187Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID710861Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in mouse peritoneal macrophages assessed as reduction of intracellular parasite level at 10 uM after 4 days2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID1498340Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as increase in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID285210Effect on survival in Trypanosoma cruzi Y infected C57BL/6 mouse Chagas disease model assessed as mean survival time at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1496049Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Swiss Webster mouse cardiac cells after 24 hrs2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID1498240Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in esophagus tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days st2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID396006Antimicrobial activity against Trypanosoma cruzi infected in BALB/c mouse assessed as parasitemia remaining by PCR method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID576837Antitrypanosomal activity against trypomastigote of Trypanosoma cruzi infected in BALB/c mouse assessed as reduction of anti-Trypanosoma cruzi antibody level at 1 mg/kg, ip qd for 5 days measured after 120 days postinfection by ELISA2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
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.
AID1615122Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1780969Selectivity index, ratio of cytotoxicity against golden hamster BSR cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi trypomastigotes2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID439776Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Neglected tropical diseases: multi-target-directed ligands in the search for novel lead candidates against Trypanosoma and Leishmania.
AID1196810Binding affinity to recombinant full-length Trypanosoma cruzi CYP51 by UV-spectrophotometric analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID613444Trypanocidal activity against epimastigote form of Trypanosoma cruzi assessed as [3H]thymidine uptake after 72 hrs by liquid scintillation counter2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives.
AID1321006Cytotoxicity against human U2OS cells infected with amastigote stage of Trypanosoma cruzi Y assessed as decrease in number of cells after 96 hrs by Draq5 staining-based high content screening assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.
AID1498228Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in adipose tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days star2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID766421Cytotoxicity against mouse NCTC-929 cells at 256 uM after 48 hrs by resazurin based fluorescence assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID344439Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss mouse assessed as survivality at 385 umol/kg, po for 1 day after 15 days2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1456723Antiparasitic activity against Trypanosoma cruzi infected in human assessed as cure rate under chronic condition2017Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
Nitroimidazoles: Molecular Fireworks That Combat a Broad Spectrum of Infectious Diseases.
AID1191151Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y infected in monkey LLC-MK2 cells after 24 hrs by Pizzi-Brener method2015European journal of medicinal chemistry, Jan-27, Volume: 90Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents.
AID1687703Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1682944Antitrypanosomal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen strain infected in monkey LLC-MK2 cells assessed as reduction in parasite viability incubated for 72 hrs by beta-galactosidase reporter gene assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1238025Anti-leishmanial activity against Leishmania infantum MHOM/BR/72 amastigotes infected in BALB/c mouse peritoneal macrophages assessed as reduction in the infection index incubated for 24 hrs by Giemsa staining method2015Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
AID1633359Antitrypanosomal activity against Trypanosoma cruzi Dm28c intracellular amastigotes infected in African green monkey Vero cells incubated for 24 hrs by luciferase-luminescence based assay
AID547280Antitrypanosomal activity against Trypanosoma cruzi Y infected in mongrel dog assessed as reduction in IL10 production in right atrium at 7 mg/kg, po BID after 180 days by semiquantitative RT-PCR2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID576947Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as reduction in blood parasite load at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses administered 5 days post infection2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1686731Antitrypanosomal activity against Trypanosoma cruzi Tulahuen epimastigote forms incubated for 72 hrs by hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1498230Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in brain tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starti2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615013Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1683692Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) amastigote form infected in BALB/c mouse assessed as parasite free organ tissue ratio at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID547251Antimicrobial activity against Trypanosoma cruzi Y infected in mongrel dog assessed as suppression of microbial proliferation at 12 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1375934Parasiticidal activity against amastigote stage of Trypanosoma cruzi Tulahuen infected in mouse brain fibroblast assessed as time duration of effect at 19.2 microM preincubated for 5 days followed by another 10 days incubation with fresh compound2018Journal of medicinal chemistry, 06-14, Volume: 61, Issue:11
NMR Biochemical Assay for Oxidosqualene Cyclase: Evaluation of Inhibitor Activities on Trypanosoma cruzi and Human Enzymes.
AID344437Antitrypanosomal activity against Trypanosoma cruzi Y infected in Swiss mouse assessed as survivality at 100 nmol/kg, ip after 15 consecutive days2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1613525Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 81 po2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1498179Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID548284Selectivity ratio of EC50 for Trypanosoma brucei NfxR2 to EC50 for Trypanosoma brucei2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1367742Antitrypanosomal activity against tdTomato red labeled trypomastigote stage of Trypanosoma cruzi infected in gamma-irradiated African green monkey Vero cells after 3 days by fluorescence assay2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Selenium-containing analogues of WC-9 are extremely potent inhibitors of Trypanosoma cruzi proliferation.
AID677290Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as lymphocytic infiltrations in portal tracts at 5 mg/kg, ip after 120 days postinfection Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1290514Antiprotozoan activity against intracellular amastigote stage of Trypanosoma cruzi Tulahuen infected in human THP1 cells assessed as reduction in parasite viability after 48 hrs by microplate based assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Individual and combined antiparasitic effect of six plant metabolites against Leishmania amazonensis and Trypanosoma cruzi.
AID414763Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as parasite growth at 20 ug/ml after 24 hrs2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
Molecular modeling studies and in vitro bioactivity evaluation of a set of novel 5-nitro-heterocyclic derivatives as anti-T. cruzi agents.
AID1198737Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Tulahuen infected in human U937 cells assessed as parasite growth inhibition at 20 ug/mL after 72 hrs by beta-galactosidase reporter gene assay relative to control2015European journal of medicinal chemistry, Mar-26, Volume: 93An efficient synthesis of new caffeine-based chalcones, pyrazolines and pyrazolo[3,4-b][1,4]diazepines as potential antimalarial, antitrypanosomal and antileishmanial agents.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID317067Toxicity in african green monkey Vero cells after 72 hrs2008Journal of medicinal chemistry, Mar-27, Volume: 51, Issue:6
Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings.
AID1608322Selectivity index, ratio of CC50 for monkey LLC-MK2 cells to IC50 for Trypanosoma cruzi Y strain bloodstream trypomastigotes2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis of quinones with highlighted biological applications: A critical update on the strategies towards bioactive compounds with emphasis on lapachones.
AID547255Antimicrobial activity against Trypanosoma cruzi Y infected in mongrel dog assessed as survival of dog at 12 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1498241Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in heart tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days starti2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID576829Cytotoxicity against african green monkey Vero cells after 72 hrs by trypan blue assay2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID677206Trypanosomicidal activity against Trypanosoma cruzi SN3 anexic amastigote after 48 hrs by hemocytometric analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1496046Selectivity index, ratio of LC50 for mouse L929 cells to EC50 for Trypanosoma cruzi Tulahuen amastigotes2018Bioorganic & medicinal chemistry letters, 06-15, Volume: 28, Issue:11
Identification and preliminary structure-activity relationship studies of novel pyridyl sulfonamides as potential Chagas disease therapeutic agents.
AID285214Antimicrobial activity against Trypanosoma cruzi Y infected IFN-gamma knock out C57BL/6 mouse Chagas disease model assessed as percent of cured mouse at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID547264Antimicrobial activity against Trypanosoma cruzi Berenice-78 infected in mongrel dog assessed as parasite level in blood of dog at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 30 days by PCR analysis2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1603762Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3;DTU 1 isolated from parasite infected BALB/c Albino mouse cardiac cells after 24 hrs by Neubauer chamber based cell counting method2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID596808Selectivity index, ratio of IC50 for african green monkey Vero cells to IC50 for epimastigote form of Trypanosoma cruzi2011Journal of natural products, Apr-25, Volume: 74, Issue:4
In vitro and in vivo trypanocidal activity of flavonoids from Delphinium staphisagria against Chagas disease.
AID726232Inhibition of Trypanosoma cruzi CL Brener recombinant alpha-carbonic anhydrase expressed in insect Sf9 cell Baculovirus system by stopped flow CO2 hydration assay2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID766425Antiparasitic activity against amastigotes of Trypanosoma cruzi CL Brener expressing Escherichia coli lacZ gene infected in mouse NCTC-929 cells assessed as parasite growth inhibition at 16 uM after 7 days by colorimetric assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase.
AID1613540Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 127 post2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1312163Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Y measured after 24 hrs using propidium iodide by neubauer chamber method2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi.
AID1584770Antiparasitic activity against Trypanosoma cruzi Y strain bloodstream trypomastigotes infected in Swiss Webster mouse at 100 mg/kg, po sid via gavage administered for 5 consecutive days starting from day 5 post infection followed by cyclophosphamide-induc2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel 7-Aryl 7-Deazapurine 3'-Deoxy-ribofuranosyl Nucleosides with Potent Activity against Trypanosoma cruzi.
AID214501The compound was evaluated for its in vitro inhibitory affect against trypanothione reductase; No data2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID626321Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahuen C2C4 trypomastigotes2011Bioorganic & 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).
AID1244586Antiparasitic activity against trypomastigotes of Trypanosoma cruzi Y assessed as induction of parasite death at 25 uM after 24 hrs using propidium iodide staining after 24 hrs by flow cytometry analysis2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID333757Antitrypanosomal activity against Trypanosoma cruzi2004Journal 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.
AID677307Trypanosomicidal activity against Trypanosoma cruzi epimastigotes assessed as inhibition of acetate metabolite excretion after 96 hrs by NMR analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
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.
AID1487116Antitrypanosomal activity against Trypanosoma cruzi Queretaro epimastigotes assessed as reduction in parasite viability incubated for 24 hrs by Neubauer hematocytometery2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis and biological evaluation of 2-methyl-1H-benzimidazole-5-carbohydrazides derivatives as modifiers of redox homeostasis of Trypanosoma cruzi.
AID597239Antitrypanosomal activity against Trypanosoma cruzi CL Brener clone infected in BALB/c mouse assessed as increase of mouse survival days at 50 mg/kg/day, po relative to control2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.
AID343558Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi CL Brener2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
New trypanocidal hybrid compounds from the association of hydrazone moieties and benzofuroxan heterocycle.
AID1281416Selectivity index, ratio of MNTD90 for cytotoxicity against BALB/c mouse splenocytes to IC50 for trypamostigote form of Trypanosoma cruzi Y infected in African green monkey Vero cells2016European journal of medicinal chemistry, Mar-23, Volume: 111Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi.
AID1155760Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for Trypanosoma cruzi Tulahuen C2C42014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.
AID537139Cytotoxicity in BALB/c mouse erythrocytes assessed as hemolysis at 50 uM after 3 hrs2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1615017Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypomastigotes derived from infected Balb/c mouse after 72 hrs by resazurin dye based assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1164932Induction of apoptosis in human monocytes assessed as early apoptotic cells using Annexin V/propidium iodide by flow cytometry (Rvb = 2.18 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID1683716Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) blood stream trypomastigote form assessed as parasite growth inhibition incubated for 24 hrs by resazurin dye based assay2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1198739Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Tulahuen infected in human U937 cells assessed as parasite growth inhibition after 72 hrs by beta-galactosidase reporter gene assay2015European journal of medicinal chemistry, Mar-26, Volume: 93An efficient synthesis of new caffeine-based chalcones, pyrazolines and pyrazolo[3,4-b][1,4]diazepines as potential antimalarial, antitrypanosomal and antileishmanial agents.
AID1603834Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum urea level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 post infect2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID536030Toxicity in Swiss mouse assessed as mortality at 100 mg/kg, ip after 72 hrs2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID1064593Antiparasitic activity against trypomastigote form of Trypanosoma cruzi Y infected in LLCMK2 cells assessed as parasite lysis after 24 hrs by Pizzi-Brener method2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents.
AID303380Antitrypanosomal activity against Trypanosoma cruzi Y2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.
AID1613470Trypanocidal activity against Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1498184Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes derived from infected Balb/c albino mouse2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1592304Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability measured after 20 hrs by MTT assay
AID677309Trypanosomicidal activity against Trypanosoma cruzi epimastigotes assessed as change in L-alanine metabolite excretion after 96 hrs by NMR analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1608332Anti-parasitic activity against amastigote form of Trypanosoma cruzi after 24 hrs2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis of quinones with highlighted biological applications: A critical update on the strategies towards bioactive compounds with emphasis on lapachones.
AID1615053Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free lungs at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post infection follo2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID272980Antitrypanosomal activity against Trypanosoma cruzi trypomastigotes in CD1 mouse macrophage2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
Evaluation of azasterols as anti-parasitics.
AID1351077Antitrypanosomal activity against Trypanosoma cruzi Y Tc2 amastigotes infected in human U2OS cells at 1.56 uM after 72 hrs by Draq5 staining based HCS analysis2018European journal of medicinal chemistry, Jan-20, Volume: 144Investigating the structure-activity relationships of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against Trypanosoma cruzi to design novel active compounds.
AID597234Antitrypanosomal activity against Trypanosoma cruzi CL Brener clone infected in Swiss albino mouse assessed as increase of mouse survival days at 50 mg/kg/day, po relative to control2011Journal of medicinal chemistry, May-26, Volume: 54, Issue:10
3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.
AID1470753Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood assessed as parasite lysis at 50 ug/ml after 24 hrs by optical microscopic method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID677289Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as blood vessels with thickened walls at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID344429Antiproliferative activity against Trypanosoma cruzi Y epimastigotes assessed as number of motile forms at 1 mM after 1 hr by hemocytometer2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
AID1459242Trypanocidal activity against Trypanosoma cruzi TCC epimastigotes assessed as parasite duplication time at 15 uM measured after 9 to 10 days (Rvb = 2 day)2017European journal of medicinal chemistry, Jan-05, Volume: 125Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.
AID1686737Cytotoxicity in African green monkey Vero cells incubated for 72 hrs2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID285207Mortality rate in Trypanosoma cruzi Y infected wild type C57BL/6 mouse Chagas disease model at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1615093Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603947Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as reduction in serum Ig-G level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1074906Antitrypanosomal activity against Trypanosoma cruzi (IRHOD/CO/2008/SN3) epimastigotes assessed as plasma membrane with scalloped appearance with undulations and discontinuities at IC25 after 96 hrs by transmission electron microscopic analysis2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1868700Selectivity index, ratio of CC50 for cytotoxicity against human MRC5 cells to EC50 for Trypanosoma cruzi Tulahuen CL2 amastigotes expressing beta galactosidase infected in human MRC5 cells2022European journal of medicinal chemistry, Jul-05, Volume: 237Exploration of 6-methyl-7-(Hetero)Aryl-7-Deazapurine ribonucleosides as antileishmanial agents.
AID1244579Cytotoxicity against mouse L929 cells assessed as cell viability after 96 hrs by alamarBlue assay2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1603850Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as increase in serum lactate dehydrogenase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1639039Cytotoxicity against African green monkey Vero cells after 72 hrs by Alamar Blue assay2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Further insights of selenium-containing analogues of WC-9 against Trypanosoma cruzi.
AID672965Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes assessed as cell death at 50 uM after 72 hrs by propidium iodide staining-based flow cytometric analysis2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
AID1687783Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID1264448Trypanocidal activity against epimastigote stage of Trypanosoma cruzi MHOM/ES/2203/BCN590 after 72 hrs by cell counting analysis2015European journal of medicinal chemistry, Nov-13, Volume: 105Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.
AID1498196Toxicity in Balb/c mouse assessed as death at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID263379Unspecific cytotoxicity against murine J774 macrophages at 100 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID1067348Antimicrobial activity against promastigote stage of Leishmania amazonensis IFLA/BR/67/PH-8 clinical isolate after 72 hrs by Neubauer chamber analysis2014Bioorganic & medicinal chemistry, Mar-01, Volume: 22, Issue:5
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.
AID1615019Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID396013Antimicrobial activity against Trypanosoma cruzi and Trypanosoma cruzi 2 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID576106Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of cardiac disorders at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1164934Induction of apoptosis in human monocytes assessed as necrotic cells using Annexin V/propidium iodide by flow cytometry (Rvb = 0.02 %)2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID693345Growth inhibition of mouse J774 cells at 64 uM after 24 hrs by resazurin reduction assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and chemometric analysis of indazole derivatives. 1,2-Disubstituted 5-nitroindazolinones, new prototypes of antichagasic drug.
AID1613481Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi IRHOD/CO/2008/SN3 DTU 1 trypomastigotes derived from infected Balb/c albino mouse2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1055169Hepatotoxicity in BALB/c mouse infected with bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 assessed as vessels with thickened walls at 5 mg/kg/day, ip administered for 5 days measured 150 days post-infection by light microscopic a2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1615073Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as change in mitochondrial membrane potential at IC25 after 72 hrs by Rho123 staining based flow cytometry relative to control2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID672966Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes after 72 hrs by Neubauer counter-based microscopic analysis2012Bioorganic & medicinal chemistry, Aug-15, Volume: 20, Issue:16
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
AID762752Selectivity index, ratio of C57BL/6 mouse spleen cells to trypomastigotes forms of Trypanosoma cruzi Tulahuen infected in monkey LLC-MK2 cells2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Molecular design, synthesis and biological evaluation of 1,4-dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity.
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]
AID1613545Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measur2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1422887Antitrypanosomal activity against Trypanosoma cruzi Dm28c amastigotes infected in African green monkey Vero cells after 48 hrs by CPRG/Nonidet reagent based beta-galactosidase reporter gene assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID337139Antitrypanosomal activity against Trypanosoma cruzi 13379 CL6 after 48 hrs
AID1624262Selectivity index, ratio of EC50 for human MRC5 cells to EC50 for nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 harboring beta-galactosidase2019European journal of medicinal chemistry, Feb-15, Volume: 164Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity.
AID1498183Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID762753Trypanocidal activity against trypomastigotes forms of Trypanosoma cruzi Tulahuen infected in monkey LLC-MK2 cells after 24 hrs by beta-galactosidase reporter assay2013Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
Molecular design, synthesis and biological evaluation of 1,4-dihydro-4-oxoquinoline ribonucleosides as TcGAPDH inhibitors with trypanocidal activity.
AID1683670Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as reduction in survival at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured up to 145 days post infection2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID548282Antimicrobial activity against Trypanosoma brucei NfxR22010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis.
AID1498189Trypanocidal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 amastigotes infected in African green monkey Vero cells assessed as reduction in infected cells after 72 hrs by Giemsa-staining based microscopic assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID341600Antiplasmodial activity against Plasmodium falciparum NF542007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1613473Trypanocidal activity against Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells after 72 hrs by Giemsa-staining based microscopic assay2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID100286In vitro inhibitory affect against Leishmania donovani; No data2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Synthesis and evaluation of 9,9-dimethylxanthene tricyclics against trypanothione reductase, Trypanosoma brucei, Trypanosoma cruzi and Leishmania donovani.
AID1383433Selectivity index, ratio of LC50 for Swiss Webster mouse cardiac cells by light microscopic analysis to EC50 for bloodstream trypomastigote stage of Trypanosoma cruzi Y measured after 24 hrs2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1124789Safety index, ratio of IC50 for human HepG2 cells to IC50 for epimastigote stage of Trypanosoma cruzi Y2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi.
AID547254Antimicrobial activity against Trypanosoma cruzi Berenice-78 infected in mongrel dog assessed as suppression of microbial proliferation at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 1 day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1866580Inhibition of Trypanosoma cruzi G6PD2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation.
AID1614011Selectivity index, ratio of CC50 for rat L6 cels to IC50 for Trypanosoma brucei Tulahuen C2C4 amastigotes2019Journal 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.
AID1565129Trypanocidal activity against intracellular amastigote stage of luciferase expressing Trypanosoma cruzi Dm28c infected in Vero cells assessed as reduction in parasite viability after 72 hrs in presence of luciferin by Giemsa staining based optical microsc2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1603824Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasite-free heart in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1462694Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 intracellular amastigotes infected in rat L6 cells assessed as growth inhibition at 0.8 ug/ml after 96 hrs by CPRG/Nonidet reagent based photometric 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.
AID341606Antimicrobial activity against Babesia divergens 1903B2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
AID1518998Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as effect on RR interval at 30 to 75 mg/kg/day, po administered via gavage for 30 consecutive days starting from 90 days post infection and measur2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1517424Antitrypanosomal activity against intracellular amastigote stage of Trypanosoma cruzi Silvio X10/1 infected in human U2OS cells measured after 96 hrs by DRAQ5 dye based microscopic analysis2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.
AID577157Antimicrobial activity against Trypanosoma cruzi Tulahuen infected in Swiss mouse assessed as reduction in reduction in parasite induced histopathological changes in liver at 60 mg/kg/day, po for 6 days per week until completion of 60 compound doses admin2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Hydroxymethylnitrofurazone is active in a murine model of Chagas' disease.
AID1074920Toxicity in BALB/c mouse assessed as survival at 1 mg/kg/day, ip relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74New perspectives on the synthesis and antichagasic activity of 3-alkoxy-1-alkyl-5-nitroindazoles.
AID1403409Cytotoxicity against Swiss Webster mouse cardiomyocytes after 72 hrs2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID1547543Trypanosomacidal activity against Trypanosoma cruzi strain Y trypomastigotes assessed as reduction in number of infected cells at faster rate at 20 uM measured for 24 to 96 hrs by Hoechst 33342 staining based fluorescence imaging assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Discovery of Potent
AID677305Antitrypanosomal activity against Trypanosoma cruzi infected in BALB/c mouse assessed as reduction in anti-organism antibody at 1 mg/kg, ip dosed for 5 days measured on day 40 to 120 post infection2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID666682Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C2C4 intracellular amastigotes infected in rat L6 cells after 4 days by photometry2012European journal of medicinal chemistry, Aug, Volume: 54Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.
AID1128397Antitrypanosomal activity against amastigote stage of lacZ expressing Trypanosoma cruzi Tulahuen after 72 hrs2014Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6
Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents.
AID378742Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in Swiss albino mouse assessed as reduction in parasitaemia at 500 mg/kg, po after 6 hrs1999Journal of natural products, Feb, Volume: 62, Issue:2
Biological activities of 7-epiclusianone.
AID656214Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 2 infected in african green monkey Vero cells expressing red fluorescent protein after 3 days by fluorescence analysis2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Phosphonium lipocations as antiparasitic agents.
AID396022Antimicrobial activity against Trypanosoma cruzi genotype 39 and genotype 32 dually infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1683684Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on LDH level at 20 mg/kg, po administered for 5 days starting at 9 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1686734Antitrypanosomal activity against Trypanosoma cruzi SN3 epimastigote forms incubated for 72 hrs by hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1569972Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes after 5 days by Neubauer chamber method2019European journal of medicinal chemistry, Oct-15, Volume: 1802-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity.
AID1603953Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 epimastigote assessed as effect on ethanol excretion at IC50 after 72 hrs by H NMR method relative to control2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1381693Antitrypanosomal activity against Trypanosoma cruzi amastigote form infected in human U2OS cells assessed as parasite growth inhibition after 72 hrs2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1613519Induction of mitochondrial membrane potential disruption Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as inhibition of DNA and RNA levels at IC25 after 72 hrs by acridine orange staining based flow cytometry relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID1381725Inhibition of recombinant full-length human aurora B kinase expressed in baculovirus system using MBP as substrate incubated for 45 mins by ADP-glo kinase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1361365Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood assessed as parasite lysis after 24 hrs by optical microscopic method2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis, molecular docking and biological evaluation of novel phthaloyl derivatives of 3-amino-3-aryl propionic acids as inhibitors of Trypanosoma cruzi trans-sialidase.
AID1240905Selectivity index, ratio of IC50 for rat L6 cells to IC50 for trypomastigote forms of Trypanosoma cruzi Tulahuen C42015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.
AID536028Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y assessed as viability at 40 uM after 15 hrs by trypan blue exclusion assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID392022Antitrypanosomal activity against Trypanosoma cruzi Colombiana infected Swiss mouse assessed as prevention of liver congestion at 120 mg/kg/day, po2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
AID1615112Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1379739Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigotes expressing beta-galactosidase gene incubated for 4 days by beta-galactosidase mediated CPRG substrate hydrolysis assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Synthesis and 2D-QSAR studies of neolignan-based diaryl-tetrahydrofuran and -furan analogues with remarkable activity against Trypanosoma cruzi and assessment of the trypanothione reductase activity.
AID537135Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID1055184Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for extracellular epimastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN32013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1422885Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes infected in African green monkey Vero cells after 72 hrs by CPRG/Nonidet reagent based beta-galactosidase reporter gene assay2018ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10
Discovery of a Biologically Active Bromodomain Inhibitor by Target-Directed Dynamic Combinatorial Chemistry.
AID726224Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 8 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1686744Selectivity index, ratio of IC50 for cytotoxicity in African green monkey Vero cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi NS3 epimastigote forms2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID563555Toxicity in CH3/He(H-2k) mouse assessed as effect on creatine kinase level at 100 mg/kg/day, po2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1498288Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes assessed as change in ratio of creatine kinase in muscle to brain at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infect2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID547263Antimicrobial activity against Trypanosoma cruzi Y infected in mongrel dog assessed as parasite level in blood of dog at 7 mg/kg, po BID started 12 to 22 days postinfection measured after 30 days by PCR analysis2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1615029Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 amastigotes infected in African green monkey Vero cells2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID251290In vivo activity at a dose of 45 mg/kg, p.o., for 5 doses in in rodent model with Trypanosoma brucei brucei STIB 795 strain, measured as survival days (control 13 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.
AID1603772Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen;DTU 6 trypomastigote forms2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1055177Trypanocidal activity against bloodstream trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in BALB/c mouse assessed as reduction of anti-parasitic Ig-G level in serum at 5 mg/kg/day, ip administered for 5 days measured over 40 to 120 da2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1065109Trypanocidal activity against Trypanosoma cruzi CA-I/72 infected in BESM cells assessed as parasite re-emergence at 6.6 uM treated for 20 days measured after 37 days2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.
AID302065Cytotoxicity against Vero cells by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides.
AID396012Antimicrobial activity against Trypanosoma cruzi 2 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1470754Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi NINOA infected in NIH mouse blood after 24 hrs by optical microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID1507196Antitrypanosomal activity against Trypanosoma cruzi clone CL B5 epimastigotes at 25 uM after 72 hrs by beta-galactosidase reporter gene assay2017European journal of medicinal chemistry, Aug-18, Volume: 136Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.
AID548113Inhibition of Trypanosoma cruzi triosephosphate isomerase at 400 uM after 2 hrs2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
AID1653741Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 trypomastigotes infected in rat L6 cells assessed as parasite growth inhibition measured after 96 hrs by inverted microscopy analysis2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID630656Antitrypanosomal activity against epimastigote form of Trypanosoma cruzi Y after 5 days by spectrophotometer analysis2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Synthesis, molecular modeling and preliminary biological evaluation of a set of 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazole as potential antibacterial, anti-Trypanosoma cruzi and antifungal agents.
AID1525223Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in peritoneal macrophages (unknown origin) measured after 48 hrs by resazurin dye based assay2019Journal of natural products, 05-24, Volume: 82, Issue:5
Antitrypanosomal Activity of Acetogenins Isolated from the Seeds of Porcelia macrocarpa Is Associated with Alterations in Both Plasma Membrane Electric Potential and Mitochondrial Membrane Potential.
AID1615035Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as reduction in parasitaemia level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection meas2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1603854Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as change in serum alanine aminotransferase level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1633360Cytotoxicity against African green monkey Vero cells 72 hrs by CellTiter-Glo assay
AID1615028Selectivity index, ratio of IC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi TINF/CH/1956/Tulahuen DTU 6 epimastigotes2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID263377Antitrypanosomal activity against Trypanosoma cruzi epimastigotes at 10 ug/ml2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
New ligand-based approach for the discovery of antitrypanosomal compounds.
AID669297Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes after 96 hrs by neubauer chamber2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
Terpenes from Copaifera demonstrated in vitro antiparasitic and synergic activity.
AID1683678Toxicity in BALB/c mouse infected with Trypanosomal Trypanosoma cruzi MHOM/Pe/2011/Arequipa(DTU V) assessed as effect on uric acid level at 20 mg/kg, po administered for 5 days starting at 100 days post infection and measured after 2 days post treatment2020Journal of natural products, 12-24, Volume: 83, Issue:12
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.
AID1687790Selectivity index, ratio of GI50 for human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by WST1 assay to IC50 for antitrypanosomal activity against Trypanosoma cruzi Y axenic amastigotes infected in African green monkey Vero c2020European journal of medicinal chemistry, Jan-15, Volume: 186Novel nitroimidazole derivatives evaluated for their trypanocidal, cytotoxic, and genotoxic activities.
AID1519010Antitrypanosomal activity against Trypanosoma cruzi K98 bloodstream form infected in C3H/HeNk mouse assessed as adipocytes replacement in skeletal muscle by measuring number of adipocyte at 75 mg/kg/day, po administered via gavage for 30 consecutive days 2019European journal of medicinal chemistry, 12-15, Volume: 184Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease.
AID1615085Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum urea level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 16 po2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1254443Antiparasitic activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in BALB/c mouse assessed as reduction of parasitemia at 100 mg/kg, po qd administered for 5 days measured on day 12 post infection relative to vehicle-treated 2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1603744Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote infected in BALB/c mouse assessed as parasitemia reactivation in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1616171Toxicity in Swiss Webster mouse infected with Trypanosoma cruzi Y trypomastigotes assessed as appearance of clinical symptoms at 100 mg/kg, po administered once daily via gavage for 5 days starting from 5 days post-infection and measured daily up to 40 da2019Journal of medicinal chemistry, 10-10, Volume: 62, Issue:19
Discovery of Pyrrolo[2,3-
AID1687715Anti-chagasic activity against Trypanosoma cruzi trypomastigotes infected in C3H mouse assessed as active behaviour at 10 mg/kg, po treated 10 days post infection measured on day 192020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID1486934Antiprotozoal activity against Leishmania amazonensis IFLA/BR/67/PH-8 incubated for 72 hrs by Neubauer chamber based cell counting method2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
AID337130Antitrypanosomal activity against Trypanosoma cruzi Tulahuen after 48 hrs
AID1174798Antiparasitic activity against trypomastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in BALB/c mouse acute chagas disease model assessed as parasitemia reactivation at 5 mg/kg, ip after 60 days immunosuppressed with cyclophosphamide monohydr2015European journal of medicinal chemistry, Jan-07, Volume: 89Prospects of an alternative treatment against Trypanosoma cruzi based on abietic acid derivatives show promising results in Balb/c mouse model.
AID575180Antimicrobial activity against Trypanosoma cruzi infected in rat L6E9 myoblasts assessed as inhibition of [3H]uracil incorporation by giemsa staining2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Chemical validation of phosphodiesterase C as a chemotherapeutic target in Trypanosoma cruzi, the etiological agent of Chagas' disease.
AID1439207Antitrypanosomal activity against Trypanosoma cruzi Y amastigote forms infected in human U2OS cells after 96 hrs by Draq5 staining-based high content analysis relative to control2017European journal of medicinal chemistry, Mar-10, Volume: 128Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols.
AID1565134Cytotoxicity against mouse cardiomyocytes infected with intracellular amastigote stage of Trypanosoma cruzi Y strain assessed as reduction in cardiomyocyte viability after 72 hrs by Celltiter-Glo assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1613529Nephrotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum uric acid level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID213635Effective concentration required to inhibit the growth of mammalian stage of Trypanosoma cruzi grown in murine 3T3 fibroblasts2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.
AID536024Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y assessed as viability at 40 uM after 11 days by trypan blue exclusion assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID1498237Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in parasitaemia reactivation in adipose tissue at 20 mg/kg, po pretreated once daily for 5 consecutive days star2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1603865Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum lactate dehydrogenase level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive days starting fro2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1613558Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in ratio of serum ALT to GPT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID621152Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 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.
AID303378Antitrypanosomal activity against Trypanosoma cruzi Tulahuen 22007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
In vivo anti-Chagas vinylthio-, vinylsulfinyl-, and vinylsulfonylbenzofuroxan derivatives.
AID576100Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Abdominal bloating at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1403393Therapeutic index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Y trypomastigotes infected in monkey LLC-MK2 cells2018European journal of medicinal chemistry, Jan-20, Volume: 144Efficacy of 2-hydroxy-3-phenylsulfanylmethyl-[1,4]-naphthoquinone derivatives against different Trypanosoma cruzi discrete type units: Identification of a promising hit compound.
AID707781Antitrypanosomal activity against Trypanosoma cruzi IRHOD/VO/2008/SN3 isolated from mouse blood trypomastigotes incubated for 24 hrs2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Phthalazine derivatives containing imidazole rings behave as Fe-SOD inhibitors and show remarkable anti-T. cruzi activity in immunodeficient-mouse mode of infection.
AID1254447Toxicity in BALB/c mouse infected with bloodstream trypomastigote stage of Trypanosoma cruzi Y assessed as body weight loss at 100 mg/kg, po qd administered for 5 days2015Bioorganic & medicinal chemistry, Dec-01, Volume: 23, Issue:23
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.
AID1687702Antitrypanosomal activity against bloodstream Trypanosoma cruzi amastigotes expressing beta-galactosidase infected in african green monkey VERO cells incubated for 5 days measured by microplate reader assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Hit-to-lead optimization of novel 2-alkylaminomethylquinoline derivatives as anti-chagas agents.
AID576085Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Dyshidrosis at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1498255Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypamastigotes infected in Balb/c mouse assessed as reduction in Ig-G level in serum at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 75 post in2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi.
AID1615104Cardiotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as decrease in serum LDH level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measured on day 127 po2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID710864Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in mouse peritoneal macrophages assessed as reduction of intracellular parasite level after 4 days2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
AID1184293Antitrypanosomal activity against intracellular Trypanosoma cruzi infected in human U2OS cells assessed as reduction in parasite count at 12.5 uM after 48 hrs by confocal microscopy2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a]benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi.
AID1780964Selectivity index, ratio of IC50 for cytotoxicity against golden hamster BSR cells to IC50 for antiprotozoal activity against Trypanosoma cruzi epimastigotes2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1508560Cytotoxicity against mouse J774 cells assessed as reduction in cell viability after 72 hrs by alamar blue assay2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1615110Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in ratio of serum AST to GOT level at 20 mg/kg, po once daily for 5 consecutive days starting from day 75 post infection measur2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1164939Activation of human platelets assessed as CD62P expression at 3.9 ug/ml by flow cytometry relative to control2014European journal of medicinal chemistry, Nov-24, Volume: 87In vitro antiparasitic activity of new thiosemicarbazones in strains of Trypanosoma cruzi.
AID694953Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y after 5 days2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice.
AID563560Cardiotoxicity in CH3/He(H-2k) mouse assessed as effect on heart rate level at 100 mg/kg/day, po2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.
AID1603845Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum urea level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting from day 8 post infect2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID311644Antiparasitic activity against Trypanosoma cruzi2007Journal of natural products, Oct, Volume: 70, Issue:10
Antiprotozoal polyacetylenes from the Tanzanian medicinal plant Cussonia zimmermannii.
AID1508583Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y infected in Balb/c mouse assessed as protection against mouse mortality at 100 mg/kg, po qd administered for 5 consecutive days starting from day 5 post infection me2017European journal of medicinal chemistry, Dec-01, Volume: 141Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi.
AID1615126Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as change in alkaline phosphatase level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on d2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1541165Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 amastigotes infected in rat L6 cells assessed as growth inhibition after 96 by photometric analysis
AID265555Antitrypanosomatid activity against Trypanosoma cruzi Tulahuen 2 epimastigote form2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
2H-benzimidazole 1,3-dioxide derivatives: a new family of water-soluble anti-trypanosomatid agents.
AID1713352Trypanocidal activity against Trypanosoma cruzi Tulahuen C4 amastigotes intra-peritoneally infected in BALB/C mouse assessed as reduction in spleen trypomastigotes treated day 4 postinfection for 20 days2016European journal of medicinal chemistry, Nov-10, Volume: 123Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.
AID547269Immunostimulatory activity in mongrel dog infected with Trypanosoma cruzi Berenice-78 assessed as production of antibody IgG at 12 mg/kg, po BID for 90 days measured up to 30 days by ELISA2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
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.
AID1383427Selectivity index, ratio of LC50 for mouse L929 cells by light microscopic analysis to EC50 for Trypanosoma cruzi Tulahuen trypomastigote forms2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID677287Toxicity in BALB/c mouse liver infected with Trypanosoma cruzi assessed as granulomas with limphocitic infiltration at 5 mg/kg, ip after 120 days postinfection by Histopathological analysis2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID1070010Antimicrobial activity against amastigote stage of Trypanosoma cruzi CL Brener infected in mouse NCTC-929 cells assessed as growth inhibition at 32 uM after 7 days by beta-galactosidase reporter gene assay2014Bioorganic & medicinal chemistry letters, Feb-15, Volume: 24, Issue:4
In vitro phenotypic screening of 7-chloro-4-amino(oxy)quinoline derivatives as putative anti-Trypanosoma cruzi agents.
AID726608Antiparasitic activity against Toxoplasma gondii tachyzoite expressing red fluorescence protein assessed as growth inhibition by fluorescence plate reader2013European journal of medicinal chemistry, Feb, Volume: 60Design, synthesis and biological evaluation of sulfur-containing 1,1-bisphosphonic acids as antiparasitic agents.
AID536026Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y assessed as viability after 24 hrs by trypan blue exclusion assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID1383430Antitrypanosomal activity against bloodstream trypomastigote stage of Trypanosoma cruzi Y measured after 24 hrs by light microscopic analysis2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID1415704Antitrypanosomal activity against Trypanosoma cruzi strain CL Brener epimastigotes measured after 72 hrs by Neubauer chamber based cell counting method2017MedChemComm, May-01, Volume: 8, Issue:5
Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.
AID1456554Antitrypanosomal activity against Trypanosoma cruzi Tulahuen intracellular amastigote harboring LacZ infected in human U937 cells after 72 hrs by CPRG/Nonidet reagent based spectrophotometric method
AID576833Antitrypanosomal activity against Trypanosoma cruzi infected in african green monkey Vero cells assessed as reduction of trypomastigote number per infected cell at IC25 after 10 days relative to control2011Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
In vivo trypanosomicidal activity of imidazole- or pyrazole-based benzo[g]phthalazine derivatives against acute and chronic phases of Chagas disease.
AID1780966Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BSR cells assessed as inhibition of replication of intracellular amastigotes incubated for 72 hrs by fluorescence based analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1555442Antitrypanosomal activity against Trypanosoma cruzi strain Y trypomastigotes maintained in Rhesus monkey LLC-MK1 cells assessed as decrease in trypomastigotes cell viability incubated for 24 hrs by resazurin dye based colorimetric assay2019European journal of medicinal chemistry, Aug-15, Volume: 176Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi.
AID1399457Cytotoxicity against rat H9c2 cells infected with Trypanosoma cruzi Tulahuen amastigote forms assessed as reduction in cell number after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.
AID536809Antitrypanosomal activity against clone C4 Trypanosoma cruzi Tulahuen expressing LacZ2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
QSAR guided synthesis of simplified antiplasmodial analogs of naphthylisoquinoline alkaloids.
AID1072681Cytotoxicity against BALB/c mouse splenocytes assessed as cell viability after 24 hrs by [3H]thymidine incorporation assay2014European journal of medicinal chemistry, Mar-21, Volume: 75Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death.
AID1244576Antiparasitic activity against trypomastigotes of Trypanosoma cruzi Y assessed as reduction of parasite count after 24 hrs2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1682942Selectivity index, ratio of CC50 for monkey LLC-MK2 cells to IC50 for antitrypanosomal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen strain infected in monkey LLC-MK2 cells2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.
AID1470752Trypanocidal activity against trypomastigote stage of Trypanosoma cruzi INC-5 infected in NIH mouse blood after 24 hrs by optical microscopic method2017European journal of medicinal chemistry, May-26, Volume: 132An in vitro and in vivo evaluation of new potential trans-sialidase inhibitors of Trypanosoma cruzi predicted by a computational drug repositioning method.
AID576092Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Articular involvement at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID1603836Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum lactate dehydrogenase level in acute phase at 20 mg/kg/day,po administered for 5 consecutive days starting from d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1381720Inhibition of human microsomal CYP1A2 expressed in baculovirus infected BTI-TN-5B1-4 cells incubated for 30 mins by luciferase assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
AID1613518Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 epimastigotes assessed as change in mitochondrial membrane potential at IC25 after 72 hrs by Rho123 staining based flow cytometry relative to control2019European journal of medicinal chemistry, Feb-15, Volume: 164New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases.
AID726225Antitrypanosomal activity against Trypanosoma cruzi Y epimastigotes at 16 uM incubated for 48 hrs by resazurin dye reduction based ELISA method2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Cloning, characterization, and sulfonamide and thiol inhibition studies of an α-carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
AID1633362Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Dm28c intracellular amastigotes infected in African green monkey Vero cells
AID1177051Antiprotozoan activity against Trypanosoma cruzi Tulahuen C4 amastigotes2015Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
AID1565130Selectivity index, ratio of CC50 for African green monkey Vero cells to IC50 for Trypanosoma cruzi Y strain bloodstream trypomastigotes isolated from infected Swiss webster mouse cardiac cells2019European journal of medicinal chemistry, Nov-15, Volume: 182Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.
AID1686728Antitrypanosomal activity against Trypanosoma cruzi Arequipa epimastigote forms incubated for 72 hrs by hemocytometry2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID547279Antitrypanosomal activity against Trypanosoma cruzi Y infected in mongrel dog assessed as reduction in INFgamma production in right atrium at 7 mg/kg, po BID after 180 days by semiquantitative RT-PCR2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Effects of ravuconazole treatment on parasite load and immune response in dogs experimentally infected with Trypanosoma cruzi.
AID1653748Selectivity 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 Leishmania donovani MHOM-ET-67/L82 axenic amastigotes assessed as parasite growth2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Synthesis, in-vitro antiprotozoal activity and molecular docking study of isothiocyanate derivatives.
AID621157Selectivity index, ratio of IC50 for rat L6 cells to IC50 for Trypanosoma cruzi Tulahuen C42011Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives.
AID1615042Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes infected in Balb/c mouse assessed as parasite-free oesophagus at 20 mg/kg, po pretreated once daily for 5 consecutive days starting from day 10 post infection 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1686770Antitrypanosomal activity against Trypanosoma cruzi Arequipa trypomastigotes infected in BALB/c mouse assessed as reduction in splenomegaly by measuring weight percent of spleens measured during acute phase (days 0 to 40 post infection) at 100 mg/kg, po d2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives.
AID1055180Trypanocidal activity against amastigote form of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as inhibition of amastigotes load per cell at IC25 preincubated for 12 hrs followed by compound washout measured afte2013European journal of medicinal chemistry, , Volume: 70Scorpiand-like azamacrocycles prevent the chronic establishment of Trypanosoma cruzi in a murine model.
AID1383424Antitrypanosomal activity against Trypanosoma cruzi Tulahuen trypomastigote forms infected in mouse L929 cells assessed as reduction in infection level at 10 to 12 uM after 96 hrs by beta-galactosidase reporter gene assay relative to control2018European journal of medicinal chemistry, Apr-10, Volume: 149Identification of Pyrazolo[3,4-e][1,4]thiazepin based CYP51 inhibitors as potential Chagas disease therapeutic alternative: In vitro and in vivo evaluation, binding mode prediction and SAR exploration.
AID537134Antileishmanial activity against promastigotes of Leishmania braziliensis MHO/BR/75/M2903 after 18 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Anti-leishmanial and anti-trypanosomal activities of 1,4-dihydropyridines: In vitro evaluation and structure-activity relationship study.
AID677207Trypanosomicidal activity against Trypanosoma cruzi SN3 amastigote infected in Vero cells after 72 hrs by Giemsa staining method2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
In vitro and in vivo trypanosomicidal activity of pyrazole-containing macrocyclic and macrobicyclic polyamines: their action on acute and chronic phases of Chagas disease.
AID671573Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Tulahuen infected in Swiss mouse model of chagas disease assessed as increase in host survival at 100 mg/kg, po administered 8 day after post infection qd for 20 days2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.
AID1753499Antitrypanosomal activity against Trypanosoma cruzi strain Y bloodstream trypomastigotes infected in Swiss Webster mouse assessed as reduction in parasitemia at 100 mg/kg, po qd for 5 days treatment started at 6 days post-infection and measured at 8 days 2021Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7
Revisiting Pyrazolo[3,4-
AID450068Antitrypanosomal activity against Trypanosoma cruzi trypomastigote Y strain after 24 hrs by trypan blue exclusion assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents.
AID1526367Antitrypanosomal activity against Trypanosoma cruzi amastigote stage forms infected in mouse C2C12 cells incubated for 3 days by 4',6-diamidino-2-phenylindole staining based microscopy
AID396010Antimicrobial activity against Trypanosoma cruzi 1 infected in BALB/c mouse assessed as cure rate2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Impact of dual infections on chemotherapeutic efficacy in BALB/c mice infected with major genotypes of Trypanosoma cruzi.
AID1300852Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Tulahuen C4 infected in rat L6 cells assessed as inhibition of parasite growth using CPRG/Nonidet as substrate after 96 hrs by beta-galactosidase reporter gene assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.
AID576091Toxicity in human patient infected with Trypanosoma cruzi assessed as occurrence of Fever at 5 mg/kg/day for 60 days2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Tolerance of benznidazole in treatment of Chagas' disease in adults.
AID764122Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y assessed as parasite growth inhibition after 5 days by spectrophotometric analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
5-Nitro-2-furfuriliden derivatives as potential anti-Trypanosoma cruzi agents: design, synthesis, bioactivity evaluation, cytotoxicity and exploratory data analysis.
AID1854944Induction of cell death in Trypanosoma cruzi Y epimastigotes assessed as dead cells at 125 uM incubated for 24 hrs by Annexin V/7-AAD staining based flow cytometric analysis (Rvb = 1.13 %)2022European journal of medicinal chemistry, Nov-05, Volume: 241Rational design of a trypanocidal peptide derived from Dinoponera quadriceps venom.
AID1244575Antiparasitic activity against epimastigotes of Trypanosoma cruzi Dm28c assessed as reduction of parasite count after 5 days2015European journal of medicinal chemistry, Aug-28, Volume: 101Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.
AID1851976Selectivity index, ratio of CC50 for cytotoxicity against mouse 3T3 cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in mouse 3T3 cells2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1615117Hepatotoxicity in Balb/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa DTU 5 trypomastigotes assessed as increase in total bilirubin level at 20 mg/kg, po once daily for 5 consecutive days starting from day 10 post infection measured on day 2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Synthesis and biological evaluation of new long-chain squaramides as anti-chagasic agents in the BALB/c mouse model.
AID1405621Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigote forms infected in rat L6 cells after 96 hrs by CPRG/Nonidet reagent based photometric method2018European journal of medicinal chemistry, Aug-05, Volume: 156Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents.
AID1780968Selectivity index, ratio of cytotoxicity against golden hamster BSR cells to IC50 for antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BSR cells2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of Mannich base-type derivatives containing imidazole and benzimidazole as lead compounds for drug discovery in Chagas Disease.
AID1617100Antiprotozoal activity against Trypanosoma cruzi Tulahuen C4 amastigotes infected in rat L6 cells incubated for 96 hrs by beta-galactosidase reporter gene assay2019Journal 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
AID1603943Antitrypanosomal activity against Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigotes infected in BALB/c mouse assessed as reduction in serum Ig-G level in acute phase at 20 mg/kg/day, po administered for 5 consecutive days starting 2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1196803Activity of his-tagged recombinant Trypanosoma brucei type-1 nitroreductase assessed as oxidized NADH level per mg of protein after 5 mins by absorption spectrum analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
AID1074377Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi IRHOD/CO/2008/SN3 infected in African green monkey Vero cells assessed as decrease in infection rate at IC25 preincubated for 12 hrs followed by compound washout measured every 48 hrs2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Synthesis and biological evaluation of N,N'-squaramides with high in vivo efficacy and low toxicity: toward a low-cost drug against Chagas disease.
AID753404Cytotoxicity against African green monkey Vero cells after 24 hrs by resazurin assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Aromatic glycosyl disulfide derivatives: evaluation of their inhibitory activities against Trypanosoma cruzi.
AID285213Antimicrobial activity against Trypanosoma cruzi Y infected wild type C57BL/6 mouse Chagas disease model assessed as percent of cured mouse at 100 mg/kg, po after 20 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
AID1603877Toxicity in BALB/c mouse infected with Trypanosoma cruzi MHOM/Pe/2011/Arequipa;DTU 5 bloodstream trypomastigote assessed as decrease in serum creatine kinase muscle to brain ratio level in chronic phase at 20 mg/kg/day, po administered for 5 consecutive d2019Bioorganic & medicinal chemistry, 09-01, Volume: 27, Issue:17
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.
AID1493586Cytotoxicity against human U937 cells after 72 hrs by MTT assay
AID1321007Selectivity index, ratio of CC50 for human U2OS cells infected with amastigote stage of Trypanosoma cruzi Y to EC50 for amastigote stage of Trypanosoma cruzi Y2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.
AID536027Cytotoxicity against BALB/c mouse Splenocyte assessed as non-cytotoxic concentration after 24 hrs by [3H]-thymidine incorporation assay relative to control2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,220)

TimeframeStudies, This Drug (%)All Drugs %
pre-199089 (7.30)18.7374
1990's65 (5.33)18.2507
2000's229 (18.77)29.6817
2010's652 (53.44)24.3611
2020's185 (15.16)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 61.47

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 Index61.47 (24.57)
Research Supply Index7.22 (2.92)
Research Growth Index5.10 (4.65)
Search Engine Demand Index107.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (61.47)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials51 (3.88%)5.53%
Reviews92 (7.00%)6.00%
Case Studies67 (5.10%)4.05%
Observational9 (0.68%)0.25%
Other1,095 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (20)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase 2 Proof-of-Activity Study of Oral Posaconazole in the Treatment of Asymptomatic Chronic Chagas Disease (Phase 2, Protocol No. P05267) [NCT01377480]Phase 2120 participants (Actual)Interventional2011-07-06Completed
Etiologic Treatment With Benznidazole in Adult Patients With Chronic Chagas Disease. A Randomized Double Blind Clinical Trial [NCT02386358]Phase 3910 participants (Actual)Interventional1999-03-31Completed
Cardiovascular Health Investigation and Collaboration From Countries of America to Assess the Markers and Outcomes of Chagas Disease (CHICAMOCHA-3) - EQUITY (Equivalence of Usual Interventions for Trypanosomiasis) [NCT02369978]Phase 2/Phase 3500 participants (Anticipated)Interventional2015-08-31Recruiting
A Phase 1 Pharmacokinetic Drug-Drug Interaction Study of Benznidazole and E1224 in Healthy Male Volunteers [NCT03892213]Phase 128 participants (Actual)Interventional2014-10-31Completed
A Phase I, Open-label, Study of the Absorption, Metabolism and Excretion, of [14C]-Benznidazole (BNZ) Following a Single Oral Dose in Healthy Male Subjects [NCT03739541]Phase 16 participants (Actual)Interventional2018-07-16Completed
PROTOCOL FOR PHASE II CLINICAL TRIAL, RANDOMIZED AND OPEN FOR ETIOLOGICAL TREATMENT OF CHRONIC CHAGAS DISEASE WITH POSACONAZOLE AND BENZNIDAZOLE [NCT01162967]Phase 278 participants (Actual)Interventional2010-09-30Completed
Population Pharmacokinetics Study of Benznidazole in Children With Chagas Disease [NCT00699387]37 participants (Actual)Interventional2007-04-30Completed
Phase 2 Randomized, Multicenter, Placebo-controlled, Safety and Efficacy Study to Evaluate Three Oral E1224 Dosing Regimens and Benznidazole for the Treatment of Adult Patients With Chronic Indeterminate Chagas Disease [NCT01489228]Phase 2230 participants (Anticipated)Interventional2011-06-30Recruiting
Population Pharmacokinetics Study of Benznidazole in Children With Chagas'Disease [NCT01549236]Phase 480 participants (Actual)Interventional2011-05-31Completed
Benznidazole Evaluation for Interrupting Trypanosomiasis - The BENEFIT Trial [NCT00123916]Phase 32,854 participants (Actual)Interventional2004-11-30Completed
A Phase 1 Non-Randomized Open Label Study of ICM20 [NCT05523596]Phase 124 participants (Anticipated)Interventional2022-12-20Recruiting
Phase II Clinical Trial for the Evaluation of Different Benznidazole Regimens for the Treatment of Chronic Chagas Disease in Adult Patients. Berenice Project [NCT03191162]Phase 2238 participants (Actual)Interventional2017-04-21Completed
Evolution of Serologic Biomarkers and Diastolic Function and Segmentary Contractility Determined by Echocardiography After Treatment in Chagas Diseases [NCT01755377]63 participants (Actual)Observational2012-12-31Completed
Population Pharmacokinetics in Benznidazole-treated Adults With Chronic Chagas Disease. Benznidazole Pharmacokinetics and Adverse Reactions Relationship. [NCT01755403]Phase 452 participants (Actual)Interventional2012-12-31Completed
New Chemotherapy Regimens and Biomarkers for Chagas Disease [NCT03981523]Phase 2450 participants (Anticipated)Interventional2019-12-18Active, not recruiting
Prospective, Single-arm, Multicentre Study, Using a Historical Control, to Evaluate the Efficacy/Safety and Population Pharmacokinetics of Benznidazole in Children With Chronic Indeterminate Chagas Disease [NCT04024163]Phase 3178 participants (Actual)Interventional2019-09-19Active, not recruiting
Short-course Benznidazole Treatment to Reduce Trypanosoma Cruzi Parasitic Load in Women of Reproductive Age: A Non-inferiority Randomized Controlled Trial [NCT03672487]Phase 3600 participants (Anticipated)Interventional2019-06-01Recruiting
Optimization of Sampling Procedure for PCR Technique to Assess Parasitological Response for Patients With Chronic Chagas Disease Treated With Benznidazole in Aiquile, Bolivia [NCT01678599]Phase 4220 participants (Actual)Interventional2011-04-30Completed
Phase 2 Randomized, Multicenter, Safety and Efficacy Trial to Evaluate Different Oral Benznidazole Monotherapy and Benznidazole/E1224 Combination Regimens for the Treatment of Adult Patients With Chronic Indeterminate Chagas Disease [NCT03378661]Phase 2210 participants (Actual)Interventional2016-11-30Active, not recruiting
Phase III Randomized,Multicenter Non-inferiority Study to Evaluate the Efficacy and Safety of Shorter Benznidazole Regimens Compared to the Standard Regimen to Treat Adult Patients With Chronic Chagas Disease [NCT04897516]Phase 3300 participants (Anticipated)Interventional2021-07-28Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01377480 (1) [back to overview]Percentage of Participants With a Successful Response as Measured by Qualitative Polymerase Chain Reaction

Percentage of Participants With a Successful Response as Measured by Qualitative Polymerase Chain Reaction

Blood samples were collected for qualitative polymerase chain reaction (PCR) assay for Trypanosoma cruzi deoxyribonucleic acid (DNA). Successful response was defined as a negative qualitative PCR value at the Day 180 follow up visit. (NCT01377480)
Timeframe: Day 180

InterventionPercentage of participants (Number)
Posaconazole15.6
Placebo10.0
Posaconazole + Benznidazole82.1
Benznidazole + Placebo86.7

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