某些2-(1H-苯并咪唑-2-基氨基)嘧啶-4(3H)-酮及其相关衍生物的合成与体外抗HIV活性

Synthesis and in vitro anti-HIV activity of certain 2-(1H-benzimidazol-2-ylamino)pyrimidin-4(3H)-ones and related derivatives.

作者信息

Kappe T

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, AR Egypt.

出版信息

Arch Pharm (Weinheim). 1997 Mar;330(3):59-62. doi: 10.1002/ardp.19973300304.

DOI:10.1002/ardp.19973300304

PMID:9167448

Abstract

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.

摘要

为了持续开发新型非核苷类人类免疫缺陷病毒抑制剂，通过2-胍基-1H-苯并咪唑与乙氧基亚甲基丙二酸二乙酯、取代丙二酸二乙酯、一些β-酮酯和2-乙酰基丁内酯的环缩合反应，合成了一系列取代的2-(1H-苯并咪唑-2-基氨基)嘧啶-4(3H)-酮及相关衍生物。从这些系列化合物中，证实2-(1H-苯并咪唑-2-基氨基)-6-羟基-5-苯基嘧啶-4(3H)-酮（5f，NSC 666286）具有中等的体外抗HIV活性。