N¹,N³-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase
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Novikov, Mikhail S., Vladimir T. Valuev-Elliston, Denis A. Babkov, Maria P. Paramonova, Alexander V. Ivanov, Sergey A Gavryushov, Anastasia L. Khandazhinskaya, et al. “N¹,N³-Disubstituted Uracils as Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase.” Bioorganic & Medicinal Chemistry 21, no. 5 (March 1, 2013): 1150–58. https://doi.org/10.1016/j.bmc.2012.12.027.
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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 (EC₅₀=0.27μM) 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.