New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents

Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro moiety, leading to the disclosure of a new lead exhibiting a strong activity against MbtI. Our best candidate 1 h displayed a K(i) of 8.8 µM an...

詳細記述

保存先:
書誌詳細
出版年:J Enzyme Inhib Med Chem
主要な著者: Chiarelli, Laurent R., Mori, Matteo, Beretta, Giangiacomo, Gelain, Arianna, Pini, Elena, Sammartino, Josè Camilla, Stelitano, Giovanni, Barlocco, Daniela, Costantino, Luca, Lapillo, Margherita, Poli, Giulio, Caligiuri, Isabella, Rizzolio, Flavio, Bellinzoni, Marco, Tuccinardi, Tiziano, Villa, Stefania, Meneghetti, Fiorella
フォーマット: Artigo
言語:Inglês
出版事項: Taylor & Francis 2019
主題:
Short Communication
オンライン･アクセス:https://ncbi.nlm.nih.gov/pmc/articles/PMC6427685/
https://ncbi.nlm.nih.gov/pubmed/30889995
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1080/14756366.2019.1589462
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