Synthesis and in vitro anti-HIV activity of certain 2-(1H-benzimidazol-2-ylamino)pyrimidin-4(3H)-ones and related derivatives.
In an ongoing effort to develop novel non-nucleoside human immunodeficiency virus inhibitors, a series of substituted 2-(1H-benzimidazol-2-ylamino)pyrimidin-4(3H)-ones and related derivatives were synthesized via cyclocondensation of 2-ganidino-1H-benzimidazole with diethyl ethoxymethylenemalonate, substituted diethyl malonates, some beta-keto esters and 2-acetylbutyrolactone. From these series of compounds, 2-(1H-benzimidazol-2-ylamino)-6-hydroxy-5-phenylpyrimidin -4(3H)-ones (5f, NSC 666286) was confirmed to have a moderate in vitro anti-HIV activity.
Badawey el-S
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, AR Egypt.
Kappe
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D015107:4-Butyrolactone / Q000031:analogs & derivatives; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D006678:HIV / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure
C510630:2-acetylbutyrolactone; D019380:Anti-HIV Agents; D001562:Benzimidazoles; D015107:4-Butyrolactone