Author: 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.
Title: N(1),N(3)-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase Cord-id: 9bay2qaq Document date: 2013_3_1
ID: 9bay2qaq
Snippet: 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 analo
Document: 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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