Related Experiment Video
Updated: May 14, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
Mikhail S Novikov1, Vladimir T Valuev-Elliston, Denis A Babkov
1Department of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, Pavshikh Bortsov Sq., 1, Volgograd 400131, Russia.
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.
Related Concept Videos
Inhibitors of Viral Protein Synthesis
Retrovirus Life Cycles
Viruses with RNA Genomes
Retroviruses
Subviral Agents
Inhibitors of Bacterial DNA Synthesis

