419546-08-0Relevant academic research and scientific papers
Synthesis and biological evaluation of 2-acetamidothiophene-3-carboxamide derivatives against Leishmania donovani
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
, p. 142 - 146 (2014/03/21)
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 μM) against L. donovani without any cytotoxicity (CC50 > 50 μM) towards human macrophages.
