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Title: Synthesis and antiviral evaluation of 3'-substituted thymidine analogs derived from 3'-amino-3'-deoxythymidine
Authors: Pannecouque, Christophe ×
Busson, Roger
Balzarini, Jan
Claes, Paul
De Clercq, Erik
Herdewijn, Piet #
Issue Date: May-1995
Publisher: Pergamon-elsevier science ltd
Series Title: Tetrahedron vol:51 issue:18 pages:5369-5380
Abstract: Based on the structure-activity relationship for antiviral activity, a series of 3'-deoxy-3'-N-functionalized thymidine analogues derived from 3'-amino-3'-deoxythymidine was synthesized. These compounds were evaluated for their antiviral activity. Three of the prepared molecules namely 3'-(1,2,4-triazol-1-yl)carbimidoylamino-3'-deoxythymidine 6, 3'-(3-amino-1-methyl-1,2,4-triazol-5-yl)amino-3'-deoxythymidine 8b and 3'-N-cyano-O-phenylisourea-3'-deoxythymidine 7 show moderate but selective in vitro activity against HIV-1 and HIV-2. These data demonstrate that some steric bulk in the 3'-position is compatible with anti-HIV activity.
URI: 
ISSN: 0040-4020
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Laboratory of Virology and Chemotherapy (Rega Institute)
Formal and Computational Linguistics (ComForT), Leuven
Centre for Industrial Management / Traffic & Infrastructure
Cell Metabolism
× corresponding author
# (joint) last author

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