Title: Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors
Authors: Chen, Xuwang ×
Zhan, Peng
Liu, Xin
Cheng, Ziheng
Meng, Caicai
Shao, Siyuan
Pannecouque, Christophe
De Clercq, Erik
Liu, Xinyong #
Issue Date: Jun-2012
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:20 issue:12 pages:3856-3864
Abstract: A novel series of piperidine-linked amino-triazine derivatives were designed, synthesized and evaluated for in vitro anti-HIV activity as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. Screening results indicated that most compounds showed excellent activity against wild-type HIV-1 with EC(50) values in low nanomolar concentration range (especially compound 6b3, EC(50)=4.61nM, SI=5945) and high activity against K103N/Y181C resistant mutant strain of HIV-1 with EC(50) values in low micromolar concentration range. In addition, preliminary structure-activity relationship and molecular modeling of these new analogs were detailed in this manuscript.
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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