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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Detalhes bibliográficos
Publicado no: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
Formato: Artigo
Idioma:Inglês
Publicado em: Taylor & Francis 2019
Assuntos:
Short Communication
Acesso em linha: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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