US8513226: Simultaneous method for the preparation of a mixture of 3-acetoxy-17-acetamido-16-formyl-androst-5,17-diene and 3-acetoxy-2'-chloro-5-androsteno[17,16-b]pyridine
The invention relates to the preparation and biological evaluation of 3-acetoxy-17-acetamido-16-formyl-androst-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 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.
Patent No:
US8513226
Application No:
12/935877
Filing Date:
30-09-2010
Issue Date:
20-08-2013
Applicant:
CSIR-North East Institute of Science and Technology (CSIR-NEIST), Jorhat
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