Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents

被引：62

作者：

Singh, B. K. ^{[1
]}

Mishra, Mridul ^{[1
]}

Saxena, Nisha ^{[1
]}

Yadav, G. P. ^{[2
]}

Maulik, P. R. ^{[2
]}

Sahoo, M. K. ^{[3
]}

Gaur, R. L. ^{[3
]}

Murthy, P. K. ^{[3
]}

Tripathi, R. P. ^{[1
]}

机构：

[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, Mol & Struct Biol Div, Lucknow 226001, Uttar Pradesh, India

[3] Cent Drug Res Inst, Div Parasitol, Lucknow 226001, Uttar Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 12期

关键词：

Dihydropyrimidines; 1,4-Dihydropyrimidines; Antifilarial; Brugia malayi; Tetrabutyl ammonium bromide;

D O I：

10.1016/j.ejmech.2008.01.038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines (8-21) were synthesized in good yields by alkylation of 5-methyl-6-phenyl-2-thioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid ethyl esters (2-7) with different alkyl or aralkyl halides in the presence of a combination of anhydrous K2CO3 and catalytic amount of tetrabutyl ammonium bromide. The title compounds were evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro and in vivo at various concentrations. One of the compounds (18) showed promising antifilarial activity. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：2717 / 2723

页数：7

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