Synthesis and biological activity of 1-phenylsulfonyl-4-phenylsulfonylaminopyrrolidine derivatives as thromboxane a(2) receptor antagonists |
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Authors: | Marusawa Hiroshi Setoi Hiroyuki Sawada Akihiko Kuroda Akio Seki Jiro Motoyama Yukio Tanaka Hirokazu |
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Affiliation: | Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd. 5-2-3 Tokodai, Tsukuba-shi, 300--2698, Ibaraki, Japan. |
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Abstract: | 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 omega-octenol side chain of thromboxane A(2) (TXA(2)), in reference to the structure of Daltroban. Several compounds were found to be potent TXA(2) receptor antagonists. Compound 51a was the most effective inhibitor of 9,11-epoxymethano PGH(2) (U-46619)-induced rat aortic strip contraction (IC(50)=0.48 nM). |
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