Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines.

Abstract

A series of tricyclic carboxylic acids having 6-amino-pyrimidine-2,4(1H,3H)-dione with piperazino or homopiperazino moiety linked by propylene, were synthesized and evaluated for their affinity toward human histamine H(1) receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice… (More)
DOI: 10.1016/j.bmc.2011.03.003

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