Title: Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs
Authors: Li, Dongyue ×
Zhan, Peng
Liu, Huiqing
Pannecouque, Christophe
Balzarini, Jan
De Clercq, Erik
Liu, Xinyong #
Issue Date: Apr-2013
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:21 issue:7 pages:2128-2134
Article number: 10.1016/j.bmc.2012.12.049
Abstract: In continuation of our efforts toward identification and optimization of novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), we have employed a structure-based bioisosterism strategy, with which a new series of diarylpyridazine (DAPD) derivatives were synthesized and evaluated for their anti-HIV-1 (human immunodeficiency virus type 1) activity. Most of the title compounds displayed excellent anti-HIV-1 activity at submicromolar concentrations ranging from 34nM to 5.08μM. The most promising compound 8g inhibited HIV-1 IIIB in MT-4 cells at a low EC50 value (0.034μM), which was lower than the reference drug nevirapine and delavirdine. The structure activity relationships (SARs) were discussed and rationalized by docking simulations.
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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