Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity

被引：11

作者：

Singh, Kamaljit ^{[1
]}

Singh, Kawaljit ^{[1
]}

Balzarini, Jan ^{[2
]}

机构：

[1] Guru Nanak Dev Univ, UGC, Ctr Adv Study 1, Dept Chem, Amritsar 143005, Punjab, India

[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 67卷

关键词：

Interferon inducers; Antiviral; Pyrimidinone; Cytotoxicity; Regioselectivity; Lithiation; INTERFERON INDUCERS; AGENTS; STIMULATION; RHINOVIRUS; TILORONE;

D O I：

10.1016/j.ejmech.2013.06.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-amino-5-bromo-4(3H)-pyrimidinone derivatives bearing different substituents at the C-6 position were synthesized using a highly regioselective lithiation substitution protocol, and the effect of structural variation at the C-6 position on their antiviral activity in cell culture was evaluated. Although some of the derivatives were found to be active against various virus strains, they were effective only close to their toxicity threshold. (C) 2013 Elsevier Masson SAS. All rights reserved.

引用

页码：428 / 433

页数：6

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