Synthesis and biological evaluation of 2-acetamidothiophene-3-carboxamide derivatives against Leishmania donovaniElectronic supplementary information (ESI) available: Experimental details in biology and chemistry, melting point and NMR spectra of all new compounds. See DOI: 10.1039/c3md00299c

• Main Authors: Oh, Sangmi, Kwon, Bosung, Kong, Sunju, Yang, Gyongseon, Lee, Nakyung, Han, Dawoon, Goo, Junghyun, Siqueira-Neto, Jair L, Freitas-Junior, Lucio H, Liuzzi, Michel, Lee, Jinhwa, Song, Rita
• Format: Article
• Language: English
• ISSN: 2040-2503; 2040-2511
• DOI: 10.1039/c3md00299c

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 (EC 50 = 6.41 μM) against L. donovani without any cytotoxicity (CC 50 > 50 μM) towards human macrophages. Synthesis and biological evaluation of compound 6a resulted in promising anti-amastigote activity (EC 50 = 6.41 μM) against L. donovani without any cytotoxicity (CC 50 > 50 μM) toward human macrophages.