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...

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書目詳細資料
發表在:J Enzyme Inhib Med Chem
Main Authors: 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
格式: Artigo
語言:Inglês
出版: Taylor & Francis 2019
主題:
Short Communication
在線閱讀: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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