1424798-83-3Relevant articles and documents
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
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.
, p. 1150 - 1158 (2013/03/29)
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.
