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

摘要

src="http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/amclct/2017/amclct.2017.8.issue-8/acsmedchemlett.7b00045/20170804/images/medium/ml-2017-00045m_0012.gif">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.