Synthesis and gastric antisecretory properties of 4, 5 unsaturated derivatives of 15-deoxy-16-hydroxy-16-methylprostaglandin E1

…, R Pappo, AF Gasiecki, RG Bianchi…

Index: Collins; Dajani; Pappo; Gasiecki; Bianchi; Woods Journal of Medicinal Chemistry, 1983 , vol. 26, # 6 p. 786 - 790

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Citation Number: 29

Abstract

The synthesis and gastric antisecretory activities of the A4his, A4s6-trans, and 4, 5- acetylenic analogues of 15-deoxy-16-hydroxy-16-methyl prostaglandin El methyl ester are described. The key step in the preparation of these compounds involved the stereospecific conjugate addition of a cuprate reagent to the appropriate cyclopentenones. Although the trans and acetylenic derivatives were weak inhibitors of gastric acid secretion, the cis ...