1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents

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dc.contributor.authorNovikov, Mikhail S.
dc.contributor.authorIvanova, Olga N.
dc.contributor.authorIvanov, Alexander V.
dc.contributor.authorOzerov, Alexander A.
dc.contributor.authorValuev-Elliston, Vladimir T.
dc.contributor.authorTemburnikar, Kartik Waman
dc.contributor.authorGurskaya, Galina V.
dc.contributor.authorKochetkov, Sergey N.
dc.contributor.authorPannecouque, Christophe
dc.contributor.authorBalzarini, Jan
dc.contributor.authorSeley-Radtke, Katherine
dc.date.accessioned2025-07-30T19:22:47Z
dc.date.issued2011-08-17
dc.description.abstractNon-nucleoside reverse transcriptase inhibitors (NNRTI) are key components in highly active antiretroviral therapy for treating HIV-1. Herein we present the synthesis for a series of N1-alkylated uracil derivatives bearing ω-(2-benzyl- and 2-benzoylphenoxy)alkyl substituents as novel NNRTIs. These compounds displayed anti-HIV activity similar to that of nevirapine and several of them exhibited activity against the K103N/Y181C RT mutant HIV-1 strain. Further evaluation revealed that the inhibitors were active against most nevirapine-resistant mono- and di-substituted RTs with the exception of the V106A RT. Thus, the candidate compounds can be regarded as potential lead compounds against the wild-type virus and drug-resistant forms.
dc.description.sponsorshipThis work was supported by Ministry of Education and Science of Russian Federation (state contract 16.512.11.2192), by the Russian Foundation for Basic Research (grant 10-04-0056), by the Presidium of the Russian Academy of Sciences (Programme ‘Molecular and Cellular Biology’) and by the K. U. Leuven (GOA no. 10/ 014). A.I. was supported by grant of President of Russian Federation (MR-5035.2011.4). The authors like to thank Inna Karpenko and Natalia Zakirova (EIMB), and Lizette van Berckelaer, Kristien Minner and Kris Uyttersprot (Rega) for their dedicated technical assistance.
dc.description.urihttps://pmc.ncbi.nlm.nih.gov/articles/PMC7127633/
dc.format.extent9 pages
dc.genrejournal articles
dc.identifierdoi:10.13016/m2x4fc-zrop
dc.identifier.citationNovikov, Mikhail S., Olga N. Ivanova, Alexander V. Ivanov, Alexander A. Ozerov, Vladimir T. Valuev-Elliston, Kartik Temburnikar, Galina V. Gurskaya, et al. “1-[2-(2-Benzoyl- and 2-Benzylphenoxy)Ethyl]Uracils as Potent Anti-HIV-1 Agents.” Bioorganic & Medicinal Chemistry 19, no. 19 (October 1, 2011): 5794–5802. https://doi.org/10.1016/j.bmc.2011.08.025.
dc.identifier.urihttps://doi.org/10.1016/j.bmc.2011.08.025
dc.identifier.urihttp://hdl.handle.net/11603/39599
dc.language.isoen_US
dc.publisherElsevier
dc.relation.isAvailableAtThe University of Maryland, Baltimore County (UMBC)
dc.relation.ispartofUMBC Faculty Collection
dc.relation.ispartofUMBC Chemistry & Biochemistry Department
dc.relation.ispartofUMBC Student Collection
dc.rightsThis item is likely protected under Title 17 of the U.S. Copyright Law. Unless on a Creative Commons license, for uses protected by Copyright Law, contact the copyright holder or the author.
dc.subjectUracil
dc.subjectHIV-1
dc.subjectNon-nucleoside reverse transcriptase inhibitors
dc.subjectReverse transcriptase
dc.subjectBenzophenone
dc.title1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents
dc.typeText
dcterms.creatorhttps://orcid.org/0000-0002-0154-3459

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