Chemical and Pharmaceutical Bulletin p. 84 - 96 (1998)
Update date:2022-08-05
Topics:
Seki, Toshimi
Kanada, Arihiro
Nakao, Tomio
Shiraiwa, Masahumi
Asano, Hajime
Miyazawa, Katuhiko
Ishimori, Tsutomu
Minami, Nobuyoshi
Shibata, Kenyu
Yasuda, Kikuo
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 the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).
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(1998)