Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries,ACS Medicinal Chemistry Letters

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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.

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