Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis
Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis
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DOI：
10.1021/acsmedchemlett.8b00498
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发表时间：
2019-01-01
影响因子：
4.2
通讯作者：
Buckner, Frederick S.
中科院分区：
文献类型：
--
作者：
Nagendar, Pendem;Gillespie, J. Robert;Buckner, Frederick S.
非常需要更好的治疗方法来治疗感染锥虫寄生虫如克氏锥虫或布氏锥虫的患者。本文报道了28个新的咪唑并吡啶和三唑并嘧啶类化合物，它们具有强的选择性抗锥虫活性。在许多体外试验中证明了药物样特性。在T.克氏感染化合物19和20代表了新的抗恰加斯病药物的潜在先导。
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.