Synthesis and biological activity of 1-phenylsulfonyl-4-phenylsulfonylaminopyrrolidine derivatives as thromboxane A2 receptor antagonists

被引：27

作者：

Marusawa, H ^{[1
]}

Setoi, H ^{[1
]}

Sawada, A ^{[1
]}

Kuroda, A ^{[1
]}

Seki, J ^{[1
]}

Motoyama, Y ^{[1
]}

Tanaka, H ^{[1
]}

机构：

[1] Fujisawa Pharmaceut Co Ltd, Exploratory Res Labs, Tsukuba, Ibaraki 3002698, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 05期

关键词：

D O I：

10.1016/S0968-0896(01)00397-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 (IC50 = 0.48 nM). (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1399 / 1415

页数：17

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