Thromboxane A₂ Receptor Antagonists. II. : Synthesis and Pharmacological Activity of 6, 6-Dimethylbicyclo[3.1.1]heptane Derivatives with the Benzenesulfonylamino Group

Abstract

Various stereoisomers based on the α- and ω-side chain ring junctions of 6, 6-dimethylbicyclo[3.1.1]heptane were synthesized. Their sodium salts 12, 18, 20, 30 and 37 were examined in vitro for their inhibitory activity toward aggregation of rabbit platelet-rich plasma and rat washed platelets. Their potency was very high and the partial agonist effect was small. The differences of the side chain ring junctions did not affect the activity very much. Homologication in the ω-side chain (as in 47) decreased the activity.