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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Short Communication
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427685/
https://www.ncbi.nlm.nih.gov/pubmed/30889995
http://dx.doi.org/10.1080/14756366.2019.1589462

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6427685/
https://www.ncbi.nlm.nih.gov/pubmed/30889995
http://dx.doi.org/10.1080/14756366.2019.1589462

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