ArticleAntimicrobial agents and chemotherapy2015
Identification of a new amide-containing thiazole as a drug candidate for treatment of Chagas' disease.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 46 citations in OpenAlex.
- Recent Progress in Thiazole, Thiosemicarbazone, and Semicarbazone Derivatives as Antiparasitic Agents Against Trypanosomatids andMolecules (Basel, Switzerland) · 2025Review
- Thiazole, Isatin and Phthalimide Derivatives TestedCurrent medicinal chemistry · 2024Review
- Preclinical Studies and Drug Combination of Low-Cost Molecules for Chagas Disease.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Identification of 2-(4-N,N-Dimethylaminophenyl)-5-methyl-1-phenethyl-1H-benzimidazole targeting HIV-1 CA capsid protein and inhibiting HIV-1 replication in cellulo.BMC pharmacology & toxicology · 2022Article
- Preclinical Studies in Anti-Pharmaceuticals (Basel, Switzerland) · 2021Article
- An Overview on the Therapeutics of Neglected Infectious Diseases-Leishmaniasis and Chagas Diseases.Frontiers in chemistry · 2021Review
- Review on Experimental Treatment Strategies AgainstJournal of experimental pharmacology · 2021Review
- Novel and selective inactivators of Triosephosphate isomerase with anti-trematode activity.Scientific reports · 2020Article
- Computational studies of 2-(4-oxo-3-phenylthiazolidin-2-ylidene)malononitrile.BMC chemistry · 2019Article
- A Nature-Inspired Design Yields a New Class of Steroids Against Trypanosomatids.Molecules (Basel, Switzerland) · 2019Article
- Article
- Novel and SelectiveVeterinary sciences · 2018Article
- Looking for combination of benznidazole and Trypanosoma cruzi-triosephosphate isomerase inhibitors for Chagas disease treatment.Memorias do Instituto Oswaldo Cruz · 2018Article
- Multi-Anti-Parasitic Activity of Arylidene Ketones and Thiazolidene Hydrazines against Trypanosoma cruzi and Leishmania spp.Molecules (Basel, Switzerland) · 2017Article
- 3-H-[1,2]Dithiole as a New Anti-Trypanosoma cruzi Chemotype: Biological and Mechanism of Action Studies.Molecules (Basel, Switzerland) · 2015Article
Corrections and comments
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Authors and funding
15 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Although the parasitic infection Chagas' disease was described over 100 years ago, even now there are not suitable drugs. The available drugs nifurtimox and benznidazole have limited efficacies and tolerances, with proven mutagenic effects. Attempting to find appropriate drugs to deal with this problem, here we report on the development and pharmacological characterization of new amide-containing thiazoles. In the present study, we evaluated the in vitro and in vivo effects of new candidates against Trypanosoma cruzi, the etiological agent of Chagas' disease. The lead amide-containing thiazole derivative had potent in vitro activity, an absence of both in vitro mutagenic and in vivo clastogenic effects, and excellent in vitro selectivity and in vivo tolerance. The compound suppressed parasitemia in mice, modifying the anti-T. cruzi antibodies like the reference drug, benznidazole, and displayed the lowest mortality among the tested drugs. The present evidence suggests that this compound is a promising anti-T. cruzi agent surpassing the lead optimization stage in drug development and leading to a candidate for preclinical study.
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