Synthesis and Biological Activity of 1-Phenylsulfonyl-4-Phenylsulfonylaminopyrrolidine Derivatives as Thromboxane A2 Receptor Antagonists Original Research Article

The synthesis and biological activity of novel 1-phenylsulfonyl-4- phenylsulfonylaminopyrrolidine analogues are described. All compounds were produced through modification of the substituent formally corresponding to the 1,3-dioxane ring system and the ω-octenol side chain of thromboxane A2 (TXA2), in reference to the structure of Daltroban. Several compounds were found to be potent TXA2 receptor antagonists. Compound 51a was the most effective inhibitor of 9,11-epoxymethano PGH2 (U-46619)-induced rat aortic strip contraction (IC50=0.48 nM).