Synthesis and biological evaluation of coumarin clubbed thiazines scaffolds as antimicrobial and antioxidant

AbstractA new series of 4-methyl-6-nitro-2-oxo-2H-chroman-7yl-2-(4-(4-fluorophenyl)-6-phenyl-2H-1,3-thiazin-2-yl-amino)acetates5a–j were synthesized from 6-nitro-4-methyl coumarinyl chloroacetate (5) and 2-amino thiazines (IIIa–j). The structure of the final compounds was adequately confirmed via spectroscopic techniques (IR,1H NMR,13C NMR, Mass) and characterization of physical properties. Final compounds were screened for their antimicrobial, antitubercular, and antioxidant activities. Compounds5c and5h found to have antibacterial potency againstE. coli with MIC values 50  µg/mL compared to standard drugs. Compound5d demonstrated better antifungal potency (MIC  = 200 µg/mL) againstC. albicans when compared with griseofulvin. Compounds5b and5h found to be encouraging antitubercular (MIC  = 62.5 µg/mL with 98–99% inhibition) againstM. tuberculosis H37Rv. The newly synthesized5h and5b were appeared to have high radical scavenging efficacies as 33.99  ± 0.301 and 35.35 ± 0.470 μg/mL ± SD of IC50 values, respectively, in DPPH and ABTS bioassay.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research