Article
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
Bioorganic & medicinal chemistry - 1 Mar 2013
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
Abstract excerpt
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...
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