Synthesis and in vitro pharmacology of 7-oxabicyclo [2.2. 1] heptane analogs of thromboxane A2/PGH2

PW Sprague, JE Heikes, JZ Gougoutas…

Index: Sprague; Heikes; Gougoutas; Malley; Harris; Greenberg Journal of Medicinal Chemistry, 1985 , vol. 28, # 11 p. 1580 - 1590

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Citation Number: 32

Abstract

A series of chemically stable TXA2/PGH2 analogues modeled after the structure of the natural products was prepared in search of useful inhibitors of TXA2/PGH2-mediated pathophysiology. Each of the 16 isomers implied in structure 1 was prepared in chiral form and evaluated for activity in vitro in platelets and smooth muscle. Depending on relative side chain and carbinol stereochemistry, TXA2/PGH2 agonist and antagonist and, surprisingly, ...