Ethenesulfonamide and ethanesulfonamide derivatives, a novel class of orally active endothelin-A receptor antagonists

…, M Orita, H Nakahara, J Shimaya, S Tsukamoto…

Index: Harada, Hironori; Kazami, Jun-ichi; Watanuki, Susumu; Tsuzuki, Ryuji; Sudoh, Katsumi; Fujimori, Akira; Sanagi, Masanao; Orita, Masaya; Nakahara, Hideaki; Shimaya, Jun; Tsukamoto, Shin-ichi; Tanaka, Akihiro; Yanagisawa, Isao Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 11 p. 2955 - 2968

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Citation Number: 15

Abstract

In the previous paper, we described a series of 2-phenylethenesulfonamide derivatives, a novel class of ETA-selective endothelin (ET) receptor antagonists, including the 2- methoxyethoxy derivative 2a and the 2-fluoroethoxy derivative (2b). In this paper, we wish to report further details of structure–activity relationships (SARs) of the two regions of the molecule in compound 2b, which were the alkoxy region at the 6-position of the core ...