Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives

Synthesis and initial in vitro evaluation of a novel series of phenyl oxazole derivatives are described. An SAR study of the novel dual-acting TRA/TSI agent has revealed that the lipophilicity of the oxazole amide substituents greatly influences the TRA activity but not the TSI. The chain length of...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-08, Vol.8 (15), p.1943-1948
Hauptverfasser:	Takeuchi, Kumiko, Kohn, Todd J, Mais, Dale E, True, Timothy A, Wyss, Virginia L, Jakubowski, Joseph A
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Medical sciences Pharmacology. Drug treatments Receptors, Thromboxane - antagonists & inhibitors Structure-Activity Relationship Thromboxane-A Synthase - antagonists & inhibitors
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