Synthesis of new C -dimethylated chalcones as potent antitubercular agents

AbstractA new class ofC-dimethylated-chalcones (9a–q) were synthesized by using 2-hydroxy-3,5-dimethyl-4,6-dimethoxy acetophenone as a key intermediate. The compounds were screened for anti-tubercular activity againstMycobacterium tuberculosis strain (H37Rv) by Microplate Alamar Blue assay (MABA) method at a concentration of 100 –0.8 µg/mL. The chalcones,9a,9b,9c,9k,9o, and9p were found to have higher antitubercular activity than the standard drugs, while the remaining compounds showed moderate activity. The antitubercular activity of the chalcones,9b (MIC90 = 3.98 µM) and9o (MIC90 = 3.84 µM) was found to be more than two-fold more active than the standard drugs, streptomycin (MIC90 = 10.75 µM) and ciprofloxacin (MIC90 = 9.43 µM), while their antitubercular activity was found to be more than six-fold more active than pyrazinamide (MIC90 = 25.38 µM). Further, the molecular docking studies employingMycobacterium tuberculosis protein tyrosine phosphatase (MtbPtp) was carried out to observe docking scores.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research