当前位置: X-MOL 学术ACS Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-07-13 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00045
Marc A. Giulianotti 1, 2 , Brian A. Vesely 3 , Ala Azhari 3 , Ashley Souza 3 , Travis LaVoi 2 , Richard A. Houghten 2 , Dennis E. Kyle 3 , James W. Leahy 1, 4, 5
Affiliation  

From a screening campaign that included mixture-based libraries containing more than 6 million compounds, a lead series of bis-cyclic guanidines was identified as the most promising. Lead optimization resulted in the identification of potent (IC50 < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.

中文翻译:

通过使用基于混合物的库,鉴定一系列热门的抗leishmanialial化合物

通过一项筛选活动,其中包括包含超过600万种化合物的基于混合物的文库,将双环胍的前导系列确定为最有前途的。铅的优化导致鉴定了该系列中有效的(IC 50 <500 nM)和选择性化合物,以及有效的和选择性的单胍。
更新日期:2017-07-14
down
wechat
bug