通过使用基于混合物的文库鉴定抗利什曼原虫化合物的活性系列
Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries.
作者信息
Giulianotti Marc A, Vesely Brian A, Azhari Ala, Souza Ashley, LaVoi Travis, Houghten Richard A, Kyle Dennis E, Leahy James W
机构信息
Department of Chemistry, University of South Florida, CHE 205, 4202 East Fowler Avenue, Tampa, Florida 33620, United States.
Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie, Florida 34987, United States.
出版信息
ACS Med Chem Lett. 2017 Jul 10;8(8):802-807. doi: 10.1021/acsmedchemlett.7b00045. eCollection 2017 Aug 10.
Abstract
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 (IC < 500 nM) and selective compounds within this series as well as potent and selective monoguanidines.
摘要
在一项涵盖包含超过600万种化合物的基于混合物的文库的筛选活动中，一系列双环胍被确定为最有前景的先导化合物。先导化合物优化导致在该系列中鉴定出强效（IC<500 nM）且具有选择性的化合物以及强效且具有选择性的单胍。
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