A. Abdel-Hafez, Hosny A H Elsherief, M. Jo
Nov 1, 2002
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0
Influential Citations
10
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Quality indicators
Journal
Arzneimittelforschung
Abstract
Summary In a one pot procedure, 18 compounds of 7-(substituted phenyl)-2-substituted-6,7-dihydro-4H-[1,2,4]triazolo[1,5-a] pyrimidin-5-one derivatives (16–33) have been synthesized. 3(5)-Amino-5(3)-substi-tuted-1,2,4-triazole derivatives (7–12) were used as synthones which were cyclo-condensed by fusion with substituted methyl cinnamate esters (13–15) to afford the target compounds (16–33). In an effort to develop new non-nucleoside antiviral agents, compounds 16–33 were evaluated for their anti-HIV-1 and anti- HSV-1 activities. Complete inhibition of the proliferation of HIV-1 viruses was achieved by compounds 22, 23 and 24 at concentrations of 25, 25 and 50 µg/ml, respectively. 7-Phenyl-2-(n-pentyl)-6,7-dihy-dro-4H-[1,2,4]triazolo[1,5-a]pyrimidin-5-one (19) exhibited potential activity against HSV-I with 88 % reduction in the viral plaques. The suggested marked specificity of this class of compounds as anti-HIV-1 and HSV-1 agents is discussed.