Structure-activity relationships in an imidazole-based series of thromboxane synthase inhibitors

PW Manley, NM Allanson, RFG Booth…

文献索引：Manley, Paul W.; Allanson, Nigel M.; Booth, Robert F. G.; Buckle, Philip E.; Kuzniar, Edward J.; et al. Journal of Medicinal Chemistry, 1987 , vol. 30, # 9 p. 1588 - 1595

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被引用次数: 18

摘要

Analogues of 4-[[2-(lH-imidazol-l-y1)-1-[[(4-methoxyphenyl) methoxy] methyl] ethoxy] methyl] benzoic acid (5m) were prepared and evaluated as thromboxane synthase inhibitors. A series of esters of 5m showed a parabolic relationship between lipophilicity and inhibition of TxB, generation in intact platelets, with activities up to 50 times greater than that of dazoxiben. However, on administration to rabbits the ethyl ester 5d had a short duration of ...