Synthesis and anti-HIV activity of C4-modified pyrimidine nucleosides

Authors
Wallis, MP Mahmood, N Fraser, W
Citation
Mp. Wallis et al., Synthesis and anti-HIV activity of C4-modified pyrimidine nucleosides, FARMACO, 54(1-2), 1999, pp. 83-89
Citations number
20
Categorie Soggetti
Pharmacology & Toxicology
Journal title
FARMACO
ISSN journal
0014827X → ACNP
Volume
54
Issue
1-2
Year of publication
1999
Pages
83 - 89
Database
ISI
SICI code
0014-827X(199901/02)54:1-2<83:SAAAOC>2.0.ZU;2-P
Abstract
One-pot syntheses provided a series of triazole- and pentafluorophenyloxy-s ubstituted pyrimidine nucleosides. Most of the compounds in the series disp layed anti-HIV activities but none as potent as AZT 2. 1-(beta-D-Erythro-pe ntofuranosyl)-4-pentafluorophenyloxy-2(1H)-pyrimidinone 14 was the most pot ent and the most selective compound;in the series with EC50 = 1.6 mu M. (C) 1999 Elsevier Science S.A. All rights reserved.