Title: N(1),N(3)-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
Authors: Novikov, Mikhail S ×
Valuev-Elliston, Vladimir T
Babkov, Denis A
Paramonova, Maria P
Ivanov, Alexander V
Gavryushov, Sergey A
Khandazhinskaya, Anastasia L
Kochetkov, Sergey N
Pannecouque, Christophe
Andrei, Graciela
Snoeck, Robert
Balzarini, Jan
Seley-Radtke, Katherine L #
Issue Date: Mar-2013
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:21 issue:5 pages:1150-8
Article number: 10.1016/j.bmc.2012.12.027
Abstract: A series of phenyloxyethyl and cinnamyl derivatives of substituted uracils were synthesized and found to exhibit potent activity against HIV-RT and HIV replication in cell culture. In general, the cinnamyl derivatives proved superior to the phenyloxyethyl derivatives, however 1-[2-(4-methylphenoxy)ethyl]-3-(3,5-dimethylbenzyl)uracil (19) exhibited the highest activity (EC(50)=0.27μM) thus confirming that the 3-benzyluracil fragment in the NNRTI structure can be regarded as a functional analogue of the benzophenone pharmacophore typically found in NNRTIs.
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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