Studies on agents with vasodilator and beta-blocking activities. III. Synthesis and activity of optical isomers of TZC-1370.
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 beta-blocking activity than the (R)-isomer, while their hypotensive activities were equipotent with that of the racemic compound, TZC-1370.
Research Division, Teikoku Hormone Manufacturing Co., Ltd., Kanagawa, Japan.
T
T
Seki
T
T
Takezaki
R
R
Ohuchi
M
M
Saitoh
T
T
Ishimori
K
K
Yasuda
D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology*
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D011724:Pyridazines; C097463:TZC 1370; D014665:Vasodilator Agents