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

• Main Authors: Laurent R. Chiarelli (Author), Matteo Mori (Author), Giangiacomo Beretta (Author), Arianna Gelain (Author), Elena Pini (Author), Josè Camilla Sammartino (Author), Giovanni Stelitano (Author), Daniela Barlocco (Author), Luca Costantino (Author), Margherita Lapillo (Author), Giulio Poli (Author), Isabella Caligiuri (Author), Flavio Rizzolio (Author), Marco Bellinzoni (Author), Tiziano Tuccinardi (Author), Stefania Villa (Author), Fiorella Meneghetti (Author)
• Format: Book
• Published: Taylor & Francis Group, 2019-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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 Ki of 8.8 µM and...