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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
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
The present invention relates to 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.
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机译:本发明涉及3-乙酰氧基-17-乙酰氨基-16-甲酰基-雄酮-5,17-二烯(4)和3-乙酰氧基2′-氯-5-雄烯基[17,16-b]的制备和生物学评价。吡啶(5)作为胃质子泵抑制剂,并与临床上使用的抗胃溃疡药物奥美拉唑进行比较。化合物(4)对胃壁细胞中组胺刺激的酸分泌表现出剂量依赖性抑制作用,其IC 50值可与西咪替丁相当。在单剂量1 g / Kg体重化合物(4)的水平下,未观察到瑞士白化病小鼠的死亡或行为异常。化合物(4)在体内对消炎痛诱导的溃疡还表现出优异的抗溃疡活性。
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