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...

Täydet tiedot

Tallennettuna:
Bibliografiset tiedot
Julkaisussa:J Enzyme Inhib Med Chem
Päätekijät: 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
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: Taylor & Francis 2019
Aiheet:
Short Communication
Linkit: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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