SYNTHESIS AND ANTIVIRAL ACTIVITY OF ACYCLIC NUCLEOSIDE ANALOGS OF 6-METHYLURACIL AND 4-ALKYLAMINO-6-METHYL-2(1H)-PYRIMIDINONES

Authors
Citation
S. Bhat, SYNTHESIS AND ANTIVIRAL ACTIVITY OF ACYCLIC NUCLEOSIDE ANALOGS OF 6-METHYLURACIL AND 4-ALKYLAMINO-6-METHYL-2(1H)-PYRIMIDINONES, Collection of Czechoslovak Chemical Communications, 59(3), 1994, pp. 683-690
Citations number
17
Categorie Soggetti
Chemistry
ISSN journal
00100765
Volume
59
Issue
3
Year of publication
1994
Pages
683 - 690
Database
ISI
SICI code
0010-0765(1994)59:3<683:SAAAOA>2.0.ZU;2-W
Abstract
Reaction of 2,4-Dimethoxy-6-methylpyrimidine (I) with allyl bromide or benzyl bromide afforded 1-substituted 4-methoxy-6-methyl-2(1H)-pyrimi dinone intermediates III, X. Oxidation of the compound III afforded ra cemic cis diol VI. O-Demethylation and nucleophilic displacement of th e intermediates III, VI and X gave 1-substituted 6-methyluracils IV, V II, IX and I-substituted 4-alkylamino-6-methyl-2(1H)-pyrimidinones V, VIII, XII in good yields. The compounds II - XII were evaluated agains t Ranikhet disease virus (RDV); compounds Vb, VII, X, XIIb - XIId show ed 100, 43, 44, 75, 72 and 100% inhibition, respectively.