Synthesis of thromboxane receptor antagonists with bicyclo[3.1.0]hexane ring systems

Susumu Kamata, Nobuhiro Haga, Tatsuo Tsuri, Kiyohisa Uchida, Hisato KAKUSHI, Hitoshi Arita, Kohji Hanasaki

Journal of Medicinal Chemistry · 1990 · 22 citations · 0 references

Concepts

Abstract

Thromboxane A2 receptor antagonists 11a, 15a, 26a, 30a, 34a, 36a, 46a, 52a, 61a, 72a, and 82a, which contain 6-oxabicyclo[3.1.0]hexane, 6-thiabicyclo[3.1.0]hexane, bicyclo[3.1.0]hexane, or 6,6-dimethylbicyclo[3.1.0]hexane ring systems with heptenoic and (phenylsulfonyl)amino side chains, and their corresponding sodium salts and methyl esters were synthesized. This study then examined the inhibitory effects of their sodium salts for the platelet aggregation induced by arachidonic acid with rabbit platelet-rich plasma and platelet aggregation induced by collagen with rat washed platelets.