Synthesis and antigastric ulcer activity of novel 5-isoproyl-3,8-dimethylazulene derivatives

5-Isoproyl-3,8-dimethylazulene derivatives were synthesized and evaluated for antigastric ulcer activity in vivo. Some of them possess the best activity against gastric ulcer with ulcer index values lower than the drug reference (omeprazole). The structure–activity relationship (SAR) shows that the lipophilic flat structure contributes to quite potent antigastric ulcer activity.

N-[4-(2-Thienylmethyleneamino)phenyl]-5-isopropyl-3,8-dimethylazulene-1-sulfonamide (6c). Molecular formula: C26H26N2O2S2.Figure optionsDownload as PowerPoint slide