Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.
复制标题
DOI：
10.1021/jm401178t
复制
发表时间：
2014-02-13
影响因子：
7.3
通讯作者：
Gelb MH
中科院分区：
文献类型：
--
作者：
Tatipaka HB;Gillespie JR;Chatterjee AK;Norcross NR;Hulverson MA;Ranade RM;Nagendar P;Creason SA;McQueen J;Duster NA;Nagle A;Supek F;Molteni V;Wenzler T;Brun R;Glynne R;Buckner FS;Gelb MH
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of human African trypanosomiasis, led to the identification of substituted 2-(3-aminophenyl) oxazolopyridines as a starting point for hit-to-lead medicinal chemistry. A total of 110 analogues were prepared, which led to the identification of 64, a substituted 2-(3-aminophenyl) imidazopyridine. This compound showed antiparasitic activity in vitro with an EC50 of 2 nM and displayed reasonable drug-like properties when tested in a number of in vitro assays. The compound was orally bioavailable and displayed good plasma and brain exposure in mice. Compound 64 cured mice infected with Trypanosoma brucei when dosed orally down to 2.5 mg/kg. Given its potent anti-parasitic properties and its ease of synthesis, compound 64 represents a new lead for the development of drugs to treat human African trypanosomiasis.
登录
查看更多内容
影响因子：
7.3
作者：
Dardonville, Christophe;Barrett, Michael P.;Wilson, W. David
通讯作者：
Wilson, W. David
影响因子：
9.6
作者：
Baker N;de Koning HP;Mäser P;Horn D
通讯作者：
Horn D
影响因子：
3.8
作者：
Harrill, Alison H.;DeSmet, Kristina D.;Watkins, Paul B.
通讯作者：
Watkins, Paul B.
影响因子：
5.1
作者：
FREEMAN, SJ;LLOYD, JB
通讯作者：
LLOYD, JB
DOI：
10.1073/pnas.96.8.4273
发表时间：
1999-04-13
影响因子：
11.1
作者：
Aronov, AM;Suresh, S;Gelb, MH
通讯作者：
Gelb, MH