Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of …

…, BG Utterback, VL Wyss, JA Jakubowski

Index: Takeuchi, Kumiko; Kohn, Todd J.; True, Timothy A.; Mais, Dale E.; Wikel, James H.; Utterback, Barbara G.; Wyss, Virginia L.; Jakubowski, Joseph A. Journal of Medicinal Chemistry, 1998 , vol. 41, # 27 p. 5362 - 5374

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Citation Number: 11

Abstract

A novel series of oxazolecarboxamide-substituted ω-phenyl-ω-(3-pyridyl) alkenoic acid derivatives was discovered as potent dual-acting agents to block the TXA2 receptor and to inhibit the thromboxane synthase (TRA/TSI). Synthesis, structure-activity relationship (SAR), and in vitro and in vivo pharmacology of this series of compounds are described. Modification of the series revolved around the oxazole moiety to increase the ...