Journal of Medicinal Chemistry p. 647 - 652 (1985)
Update date:2022-08-02
Topics:
Pascal, Jean-Claude
Beranger, Serge
Pinhas, Henri
Poizot, Alain
Desiles, Jean-Pierre
A series of 3,4-dihydro-1,3-dimethyl-7-<3-(4-substituted-piperazin-1-yl)-substituted-alkyl>-1H-purine-2,6-diones and 3,7-dihydro-3,7-dimethyl-1-<3-<4-substituted-piperazin-1-yl)-substituted-alkyl>-1H-purine-2,6-diones was synthesized and evaluated for antihistaminic activity.Some of them displayed good inhibition of both histamine-induced bronchospasm in the anesthetized guinea pig at 10 μ/kg by the intravenous route and of passive cutaneous anaphylaxis in the rat at 10 mg/kg by the oral route.Comparison of the two most active compounds revealed a higher antihistaminic activity with the compounds containing a (phenylthio)propyl group (1 and 2) as compared with that containing a phenoxy group.Compound 2
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