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

被引：20

作者：

Nagendar, Pendem ^{[1
]}

Gillespie, J. Robert ^{[2
]}

Herbst, Zackary M. ^{[2
]}

Ranade, Ranae M. ^{[2
]}

Molasky, Nora M. R. ^{[2
]}

Faghih, Omeed ^{[2
]}

Turner, Rachael M. ^{[2
]}

Gelb, Michael H. ^{[1
]}

Buckner, Frederick S. ^{[2
]}

机构：

[1] Univ Washington, Dept Chem, Seattle, WA 98195 USA

[2] Univ Washington, Dept Med, Seattle, WA 98109 USA

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2019年 / 10卷 / 01期

基金：

美国国家卫生研究院;

关键词：

Trypanosomiasis; Chagas disease; imidazopyridine; triazolopyrimidine; drug discovery; POSACONAZOLE;

D O I：

10.1021/acsmedchemlett.8b00498

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：105 / 110

页数：11

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