N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.

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)=0.27 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.

SUBMITTER: Novikov MS 

PROVIDER: S-EPMC7125863 | biostudies-literature | 2013 Mar

REPOSITORIES: biostudies-literature