Title: Arylazolyl(azinyl)thioacetanilides. Part 10: Design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors
Authors: Li, Xiao ×
Zhan, Peng
Liu, Hong
Li, Dongyue
Wang, Liu
Chen, Xuwang
Liu, Huiqing
Pannecouque, Christophe
Balzarini, Jan
Clercq, Erik De
Liu, Xinyong #
Issue Date: Sep-2012
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:20 issue:18 pages:5527-5536
Article number: 10.1016/j.bmc.2012.07.026
Abstract: In continuation of our efforts toward the discovery of potent HIV-1 NNRTIs with novel structures, we have employed a scaffold hopping strategy to explore the chemically diversed space of bioactive compounds. The original arylazolylthioacetanilide platform was replaced with different imidazopyridinyl- thioacetanilide scaffolds to yield the optimal pharmacophore moieties in order to generate novel NNRTIs with desirable potency. Some of the new compounds proved able to inhibit HIV-1 replication in the low micromolar range. In particular, compound 5b16 displayed the most potent anti-HIV-1 activity (EC(50)=0.21±0.06μM), inhibiting HIV-1 IIIB replication in MT-4 cells more effectively than dideoxycytidine (EC(50)=1.4±0.1μM) and similarly with nevirapine (EC(50)=0.20±0.10μM). Preliminary structure-activity relationship (SAR) of the newly synthesized congeners is discussed, and molecular modeling study is performed to rationalize the SAR conclusions.
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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