New synthetic 1H-1,2,3-triazole derivatives of 3-O-acetyl-?-boswellic acid and 3-O-acetyl-11-keto-?-boswellic acid from Boswellia sacra inhibit carbonic anhydrase II in vitro

Boswellic acids are genus specific to Boswellia; they the principal biologically active compounds holding exceptionally potent anti-inflammatory activity. A series of new 1H-1,2,3-triazole tethered 3-O-acetyl-?-boswellic acid (ABA, 1) and 3-O-acetyl-11-keto-?-boswellic (AKBA, 2) derivatives (10a-d 11a-d) were synthesized their carbonic anhydrase II (CA II) inhibitory activity was evaluated in vitro. The structures all confirmed by 1H-, 13C-NMR, HR-MS spectral data (10b, 10c 11b, 11c). displayed a moderate significant inhibition against CA with IC50 values 13.2–60.1 ?M. All reported for first time potential. After preliminary screening, kinetic studies most inhibitors (5 10b) carried out investigate mode determine constants Ki. Both found be non-competitive Ki 10.40 ± 0.013 14.25 0.017 µM, respectively. Molecular docking revealed that well accommodated allosteric site II. current study has demonstrated usefulness incorporating moiety into boswellic skeleton.