Bioorganic and Medicinal Chemistry Letters p. 1947 - 1950 (2002)
Update date:2022-08-04
Topics:
Kimura, Makoto
Masuda, Tomoko
Yamada, Koji
Kubota, Nobuo
Kawakatsu, Nobuyuki
Mitani, Masaki
Kishii, Kenichi
Inazu, Masato
Namiki, Takayuki
Two types of novel diphenylalkyl piperazine derivatives containing the thio or aminopropanol moiety substituted by phenyl or benzyl group were synthesized, and evaluated for their calcium antagonistic and antioxidative activities. These compounds showed apparent inhibitions against KCl-induced contractions in isolated rat aorta. Among them, phenylamino compound 9 and benzylamino compound 13 also possessed potent inhibitory activities against auto-oxidative lipid peroxidations in canine brain homogenates. Two representative compounds 3a and 9 were evaluated for their inhibitory activities against KCl-induced contractions in isolated canine arteries (basilar, coronary, mesenteric, and renal). Both compounds showed the most potent inhibitions to basilar artery.
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