Title: Design, synthesis, and SAR of naphthyl-substituted diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Authors: Liang, Yong-Hong ×
Feng, Xiao-Qing
Zeng, Zhao-Sen
Chen, Fen-Er
Balzarini, Jan
Pannecouque, Christophe
De Clercq, Erik #
Issue Date: Sep-2009
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Series Title: ChemMedChem vol:4 issue:9 pages:1537-1545
Abstract: A series of 38 2-naphthyl-substituted diarylpyrimidine (DAPY) analogues, characterized by various substitution patterns on the pyrimidine and naphthalene rings, was synthesized in a straightforward fashion by means of parallel synthesis and evaluated as inhibitors of the HIV-1 wild-type and double mutant (K103N+Y181C) strains. Most of the compounds displayed strong activity against wild-type HIV-1. The most active compound, with a cyano group at position C6 on the naphthalene ring, exhibited activity against wild-type HIV-1 with an EC(50) value of 0.002 muM and against the double mutant strain with an EC(50) value of 0.24 muM; the selectivity index (SI) against wild-type is >180 000, the highest SI value among DAPY analogues. The structure-activity relationship (SAR) of the newly synthesized DAPYs is presented herein.
ISSN: 1860-7179
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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