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

ACS Med Chem Lett. 2018 Dec 4;10(1):105-110. doi: 10.1021/acsmedchemlett.8b00498.

Pendem Nagendar ¹, J Robert Gillespie ², Zackary M Herbst ², Ranae M Ranade ², Nora M R Molasky ², Omeed Faghih ², Rachael M Turner ², Michael H Gelb ¹, Frederick S Buckner ²

Affiliations

1 Department of Chemistry, University of Washington, Seattle, Washington 98195, United States.
2 Department of Medicine, University of Washington, Seattle, Washington 98109, United States.

PMID: 30655955 DOI: 10.1021/acsmedchemlett.8b00498

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.

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