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Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries
Journal article   Peer reviewed

Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries

Marc A Giulianotti, Brian A Vesely, Ala Azhari, Ashley Souza, Travis LaVoi, Richard A Houghten, Dennis E Kyle and James W Leahy
ACS medicinal chemistry letters, Vol.8(8), pp.802-807
10/08/2017
DOI: https://doi.org/10.1021/acsmedchemlett.7b00045
PMCID: PMC5554901
PMID: 28835792

Abstract

screening mixture-based libraries Leishmaniasis lead optimization
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.

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