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N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2013
Mikhail S Novikov, and
Vladimir T Valuev-Elliston, and
Denis A Babkov, and
Maria P Paramonova, and
Alexander V Ivanov, and
Sergey A Gavryushov, and
Anastasia L Khandazhinskaya, and
Sergey N Kochetkov, and
Christophe Pannecouque, and
Graciela Andrei, and
Robert Snoeck, and
Jan Balzarini, and
Katherine L Seley-Radtke
Department of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, Pavshikh Bortsov Sq., 1, Volgograd 400131, Russia.
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)=0.27 μM) 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.
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