Studies on Agents with Vasodilator and β-Blocking Activities. III. Synthesis and Activity of Optical Isomers of TZC-1370

Toshimi SEKI; Takayuki TAKEZAKI; Rikio OHUCHI; Morinobu SAITOH; Tsutomu ISHIMORI; Kikuo YASUDA

doi:10.1248/cpb.43.1719

Toshimi SEKI, Takayuki TAKEZAKI, Rikio OHUCHI, Morinobu SAITOH, Tsutomu ISHIMORI, Kikuo YASUDA

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Keywords: phenoxypropanolamine, optical isomer, antihypertensive agent, hydrazinopyridazine, β-blocking activity, hypotensive activity

JOURNAL FREE ACCESS

1995 Volume 43 Issue 10 Pages 1719-1723

DOI https://doi.org/10.1248/cpb.43.1719

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Abstract

Optical isomers of TZC-1370 (1) were prepared from (R)- and (S)-1-(2-chlorophenoxy)-2, 3-epoxypropane. When given intravenously to anesthetized rats, the (S)-isomer was about 40 times more potent in terms of β-blocking activity than the (R)-isomer, while their hypotensive activities were equipotent with that of the racemic compound, TZC-1370.

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