On July 15, 2018, Chiarelli, Laurent R.; Mori, Matteo; Barlocco, Daniela; Beretta, Giangiacomo; Gelain, Arianna; Pini, Elena; Porcino, Marianna; Mori, Giorgia; Stelitano, Giovanni; Costantino, Luca; Lapillo, Margherita; Bonanni, Davide; Poli, Giulio; Tuccinardi, Tiziano; Villa, Stefania; Meneghetti, Fiorella published an article.Reference of 2-Chloro-4-nitrobenzoic acid The title of the article was Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents. And the article contained the following:
The virtual screening, synthesis, and biol. evaluation of new furan derivatives targeting Mycobacterium tuberculosis salicylate synthase (MbtI) was reported. A receptor-based virtual screening procedure was applied to screen the enamine database, identifying two compounds, I [R1 = Ph, 4-O2NC6H5, 4-F3CC6H5; R2 = H, Me] and II, endowed with a good enzyme inhibitory activity. Considering the most active compound I as starting point for the development of novel MbtI inhibitors, new derivatives based on the furan scaffold were prepared Among the SAR performed on this class, compound I [R1 = 4-O2NC6H5, R2 = H] emerged as the most potent MbtI inhibitor reported to date (Ki = 5.3 μM). Moreover, compound I [R1 = 4-O2NC6H5, R2 = H] showed a promising antimycobacterial activity (MIC99 = 156 μM), which is conceivably related to mycobactin biosynthesis inhibition. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Reference of 2-Chloro-4-nitrobenzoic acid
The Article related to arylfuranyl carboxylate preparation tuberculostatic sar mol docking, antimycobacterial drugs, drug design, iron, siderophores, tuberculosis, virtual screening, Heterocyclic Compounds (One Hetero Atom): Furans and other aspects.Reference of 2-Chloro-4-nitrobenzoic acid
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Chlorides – an overview | ScienceDirect Topics