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Eur J Med Chem ; 43(12): 2717-23, 2008 Dec.
Article in English | MEDLINE | ID: mdl-18339456

ABSTRACT

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 K(2)CO(3) 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.


Subject(s)
Brugia malayi/drug effects , Filaricides/chemical synthesis , Filaricides/pharmacology , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Alkylation , Animals , Dose-Response Relationship, Drug , Filaricides/chemistry , Models, Molecular , Molecular Structure , Parasitic Sensitivity Tests , Stereoisomerism
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