Title: Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs
Authors: Gu, Shuang-Xi ×
He, Qiu-Qin
Yang, Shi-Qiong
Ma, Xiao-Dong
Chen, Fen-Er
De Clercq, Erik
Balzarini, Jan
Pannecouque, Christophe #
Issue Date: Sep-2011
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:19 issue:17 pages:5117-5124
Abstract: A series of 26 diarylpyrimidines, characterized by the hydroxymethyl linker between the left wing benzene ring and the central pyrimidine, were synthesized and evaluated for in vitro anti-HIV activity. Most of the compounds exhibited moderate to excellent activities against wild-type HIV-1. Among them, compound 10i, bearing a chlorine atom at the C-2 position of left benzene ring, was the best congener and showed potent activity against wild-type HIV-1 with an EC(50) value of 0.009μM, along with moderate activities against the double RT mutant (K103N+Y181C) HIV-1(III(B)) and HIV-2(ROD) with an EC(50) value of 6.2 and 6.0μM, respectively. The preliminary structure-activity relationship (SAR) of this new series of compounds was also investigated.
ISSN: 0968-0896
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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