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Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.

ABSTRACT: Better therapeutics are greatly needed to treat patients infected with trypanosomatid parasites such as Trypanosoma cruzi or Trypanosoma brucei. This report describes 28 new imidazopyridines and triazolopyrimidines with potent and selective antitrypanosomal activity. Drug-like properties were demonstrated in a number of in vitro assays. In vivo efficacy was observed for 19 and 20 in acute mouse models of T. cruzi infection. Compounds 19 and 20 represent potential leads for new anti-Chagas disease drugs.

SUBMITTER: Nagendar P

PROVIDER: S-EPMC6331164 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.

Nagendar Pendem P Gillespie J Robert JR Herbst Zackary M ZM Ranade Ranae M RM Molasky Nora M R NMR Faghih Omeed O Turner Rachael M RM Gelb Michael H MH Buckner Frederick S FS

ACS medicinal chemistry letters 20181204 1

Better therapeutics are greatly needed to treat patients infected with trypanosomatid parasites such as Trypanosoma cruzi or Trypanosoma brucei. This report describes 28 new imidazopyridines and triazolopyrimidines with potent and selective antitrypanosomal activity. Drug-like properties were demonstrated in a number of in vitro assays. In vivo efficacy was observed for 19 and 20 in acute mouse models of T. cruzi infection. Compounds 19 and 20 rep ...[more]

PMID: 30655955

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