Studies on Agents with Vasodilator and. BETA.-Blocking Activities. V. Synthesis and Pharmacological Activity of the Optical Isomers of TZC-5665.

…, A Kanada, T Nakao, M SHIRAIWA, H ASANO…

文献索引：Seki, Toshimi; Kanada, Arihiro; Nakao, Tomio; Shiraiwa, Masahumi; Asano, Hajime; Miyazawa, Katuhiko; Ishimori, Tsutomu; Minami, Nobuyoshi; Shibata, Kenyu; Yasuda, Kikuo Chemical and Pharmaceutical Bulletin, 1998 , vol. 46, # 1 p. 84 - 96

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被引用次数: 5

摘要

Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among ...