A simultaneous method for the prepration of a mixture of 3- acetoxy-17-acetamdo-16-formyl-androst-5, 17-diene and 3-acetoxy-2'-chloro-5-androsteno[17, 16-B]p

摘要

The present invention relates to preparation and biological evaluation of 3-acetoxy-17- acetamido-16-formyl-an-drost-5,17-diene (4) and 3-acetoxy2'-chloro-5-androsteno [17,16- 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 IC50value comparable to cimetidine. No mortality or behavioral abnormality of Swiss albino mice was observed under single-dose level of 1g/Kg body weight of compound (4). Compound (4) further exhibited excellent anti ulcer activityin vivoagainst indomethacin induced ulcer.