ArticleBioorganic & medicinal chemistry2011
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
Article in Bioorganic & medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Review
- Antiviral Activity of NInternational journal of molecular sciences · 2022Article
- Uracil-Containing Heterodimers of a New Type: Synthesis and Study of Their Anti-Viral Properties.Molecules (Basel, Switzerland) · 2020Article
- Benzophenone: a ubiquitous scaffold in medicinal chemistry.MedChemComm · 2018Review
- Hydrophobic-core PEGylated graft copolymer-stabilized nanoparticles composed of insoluble non-nucleoside reverse transcriptase inhibitors exhibit strong anti-HIV activity.Nanomedicine : nanotechnology, biology, and medicine · 2016Article
- Double Variational Binding--(SMILES) Conformational Analysis by Docking Mechanisms for Anti-HIV Pyrimidine Ligands.International journal of molecular sciences · 2015Article
- Synthesis and anti-HCMV activity of 1-[ω-(phenoxy)alkyl]uracil derivatives and analogues thereof.Bioorganic & medicinal chemistry · 2013Article
- N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.Bioorganic & medicinal chemistry · 2013Article
- Endo-S-c-di-GMP analogues-polymorphism and binding studies with class I riboswitch.Molecules (Basel, Switzerland) · 2012Article
- Screening of Potential HIV-1 Inhibitors/Replication Blockers Using Secure Lentiviral in Vitro System.Acta naturae · 2011Article
- Benzophenone derivatives of pyrimidines as effective non-nucleoside inhibitors of wild-type and drug-resistant HIV-1 reverse transcriptase.Doklady. Biochemistry and biophysicsArticle
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Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Non-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.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.