Thieno [2, 3-d] pyrimidine-3-acetic Acids A New Class of Nonpeptide Endothelin Receptor Antagonists.

…, T SUGO, Y MASUDA, A ABE, K KUSUMOTO…

Index: Cho, Nobuo; Nara, Yoshi; Harada, Mioko; Sugo, Tsukasa; Masuda, Yasushi; Abe, Akemi; Kusumoto, Keiji; Itoh, Yasuaki; Ohtaki, Tetsuya; Watanabe, Toshifumi; Furuya, Shuichi Chemical and Pharmaceutical Bulletin, 1998 , vol. 46, # 11 p. 1724 - 1737

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Citation Number: 13

Abstract

On the basis of structural information for the cyclic hexapeptide endothelin (ET) receptor antagonist, TAK-044, a series of thieno [2, 3-d] pyrimidine-2, 4-dione derivatives bearing a carboxyl group and aromatic rings that were important for receptor binding were designed, synthesized, and evaluated for ET receptor binding affinities and inhibitory activities against ET-induce vasconstriction. Optimization of each substituent in the thieno [2, 3-d] ...