[(1H-Imidazol-1-yl) methyl]-and [(3-pyridinyl) methyl] pyrroles as thromboxane synthetase inhibitors

GR Martinez, DR Hirschfeld, PJ Maloney…

文献索引：Martinez, Gregory R.; Walker, Keith A. M.; Hirschfeld, Donald R.; Maloney, Patrick J.; Yang, Diana S.; Rosenkranz, Roberto P. Journal of Medicinal Chemistry, 1989 , vol. 32, # 4 p. 890 - 897

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被引用次数: 21

摘要

Several [(1H-imidazol-1-yl) methyl]-and [(3-ppidinyl) methyl] pyrroles were prepared and evaluated in vitro as thromboxane synthetase inhibitors in human platelet aggregation studies. A number of structures, eg lOb, f, g, i (respective ICm values: 1 pM, 50 nM, 42 nM, 44 nM) showed superior in vitro inhibition of TXAz synthetase when compared to the standard dazoxiben (1). However, it was found that in vitro potency did not translate into nor ...