Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis of the Optically Active trans-Isomers of Diltiazem and Their Cardiovascular Effects and Ca-Antagonistic Activity
Takashi TANAKA, Hirozumi INOUE, Tadamasa DATE, Kimio OKAMURA, Keiichi AOE, Mikio TAKEDA, Hiroshi KUGITA, Sakae MURATA, Takashi YAMAGUCHI, Kohei KIKKAWA, Shigeyo NAKAJIMA, Taku NAGAO
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Keywords: diltiazem, diltiazem (+)-trans isomer, diltiazem (-)-trans isomer, absolute stereochemistry, cardiovasculer effect, Ca-channel blocking activity
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1992 Volume 40 Issue 6 Pages 1476-1480

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Abstract

Optically active trans-isomers of diltiazem were synthesized and their cardiovascular effects were evaluated in anesthetized dogs and in isolated guinea pig hearts.Both (+)-2 (2R, 3S) and (-)-2 (2S, 3R) were much less active than diltiazem (1, 2D, 3S) with short duration of action. No substantial enantiomeric difference in activity was seen between them. Their Ca-antagonistic activities on Ca2+-induced contractions in K+ -depolarized canine basilar arteries were also examined.Absolute stereochemistry of (+)-2 was determined to be 2R, 3S by X-ray crystallographic analysis.

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© The Pharmaceutical Society of Japan
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