The present invention relates to preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-517-diene (4) and 3-acetoxy2'-chloro-5-androsteno[1716-b]pyridine (5) as gastric proton pump inhibitor and their comparison to that of omeprazole a clinically employed anti-gastric ulcer drug. Compound (4) exhibited dose dependent inhibition of histamine-stimulated acid secretion in gastric parietal cell with an IC50 value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1 g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activity in vivo against indomethacin induced ulcer.

暂无附图