Synthesis and structure-activity relationships of acyclic. omega. chain conjugated diene analogs of enisoprost

…, RL Shone, WE Perkins, AF Gasiecki…

Index: Collins, P. W.; Shone, R. L.; Perkins, W. E.; Gasiecki, A. F.; Kalish, V. J.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 4 p. 694 - 704

Full Text: HTML

Citation Number: 6

Abstract

A series of acyclic w chain conjugated diene analogues of enisoprost were synthesized and evaluated for gastric antisecretory and diatrheagenic activities in comparison to enisoprost and a previously identified cyclic dienyl analogue. Several novel approaches to the cuprate reagents involved in the synthesis of the series are described. From this SAR study, it appears that both the conjugated diene and the overall space filling characteristics of the ...