Synthesis, Structure Elucidation and H+/K+-ATPase Inhibitory Activity of Bisabolangelone Reduction Derivatives

Nine bisabolangelone reduction derivatives were synthesized and separated as potential anti-ulcer agent. Their structures were characterized by 2D NMR, IR, ESI-MS, elemental analysis and single-crystal X-ray diffraction analysis. Preliminarily H+/K+-ATPase activity evaluation indicated that all the target compounds had a certain inhibitory effect, and compounds II and IV exhibited the better inhibitory activity against H+/K+-ATPase than bisabolangelone and the commercial omeprazole with the IC50 of 23.21 and 65.32 μmol/L, respectively. The initial structure-activity analysis suggested that the presence of carbonyl group in six-membered ring and double bond in side-chain seemed to be necessary to the activity.