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Oh, S.,Kwon, B.,Kong, S.,Yang, G.,Lee, N.,Han, D.,Goo, J.,Siqueira-Neto, J.,Freitas-Junior, L.,Liuzzi, M. TEH ROYAL SOCIETY OF CHEMISTRY 2014 MedChemComm Vol.5 No.2
A high-throughput (HTS) and high-content screening (HCS) campaign of a commercial library identified 2-acetamidothophen-3-carboxamide as a novel scaffold for developing new anti-leishmanial agents. A series of chemical modifications were performed to study the structure-activity relationship (SAR) and in vitro anti-leishmanial activities were evaluated using biological assays of not only extracellular promastigotes but also intracellular amastigotes. Compound 6a showed promising anti-amastigote activity (EC50 = 6.41 mu M) against L. donovani without any cytotoxicity (CC50 > 50 mu M) towards human macrophages.