Synthesis and platelet-activating factor (PAF)-antagonistic activities of trisubstituted piperazine derivatives.

Abstract:

:2- or 3-Substituted 1-(2,3-dimethoxy-6,7-dihydro-5H-benzocyclohepten-8- ylcarbonyl)-4-(3,4,5-trimethoxybenzoyl)- and 4-(3,4,5-trimethoxybenzyl)piperazines (2a-s, 3a, b) were prepared and evaluated for antagonistic activities against platelet-activating factor (PAF)-induced platelet aggregation and blood pressure reduction. The 2-methoxymethyl derivative (2f) showed the most potent activities in this series. The enantiomers (R)-(+)-2f and (S)-(-)-2f were synthesized from carbobenzoxy-O-benzyl-L- and D-serine in several steps. In the binding experiment, (S)-(-)-2f showed thirty times greater affinity than the R isomer for the PAF receptor.

authors

Fukushi H,Mabuchi H,Terashita Z,Nishikawa K,Sugihara H

doi

10.1248/cpb.42.551

subject

Has Abstract

pub_date

1994-03-01 00:00:00

pages

551-9

issue

3

eissn

0009-2363

issn

1347-5223

journal_volume

42

pub_type

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