Synthesis and biological evaluation of 2-acetamidothiophene-3-carboxamide derivatives against Leishmania donovani

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) a...

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Bibliographic Details
Published in:MedChemComm 2014, Vol.5 (2), p.142-146
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
Subjects:
Leishmania donovani
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Summary: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 vitroanti-leishmanial activities were evaluated using biological assays of not only extracellular promastigotes but also intracellular amastigotes. Compound 6a showed promising anti-amastigote activity (EC sub(50) = 6.41 mu M) against L. donovaniwithout any cytotoxicity (CC sub(50) > 50 mu M) towards human macrophages.
ISSN:2040-2503
2040-2511
DOI:10.1039/C3MD00299C