ArticleACS medicinal chemistry letters2019
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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Who cites it
9 citing papers in PubMed, 25 citations in OpenAlex.
- Exploring the Antitubercular, Antimicrobial Potency, ADME-T Calculations and Docking Studies of 1,2,4-Triazole-Bearing Benzimidazoles.Chemistry & biodiversity · 2026Article
- Evaluation of Antiproliferative Activity and Molecular Modeling Studies of Some Novel Benzimidazolone-Bridged Hybrid Compounds.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Benzimidazole Derivatives in Breast Cancer: Target-Specific Therapeutic Breakthroughs.Current topics in medicinal chemistry · 2025Review
- Synthesis, DFT Calculations,ACS omega · 2024Article
- Design, Synthesis, Molecular Modeling and Biological Evaluation of Novel Pyrazole Benzimidazolone Derivatives as Potent Antioxidants.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Polymorphic structures of 3-phenyl-1Acta crystallographica. Section E, Crystallographic communications · 2023Article
- Article
- Design, synthesis, bio-evaluation, andRSC advances · 2022Article
- LigTMap: ligand and structure-based target identification and activity prediction for small molecular compounds.Journal of cheminformatics · 2021Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Since the discovery of HIV as the etiological agent of AIDS, the virus has infected millions of people each year. Fortunately, with the use of HAART, viremia can be suppressed to below detectable levels in the infected individuals, which significantly improves their quality of life and prevents the onset of AIDS. However, HAART is not curative and issues relating to adherence and drug resistance may lead to the re-emergence of viremia, the development of AIDS, and ultimately death. To address a pressing need for the development of new and efficacious antiretroviral agents with activity against viruses bearing prevalent resistant mutations, we have designed two generations of benzimidazolone derivatives as HIV non-nucleoside reverse transcriptase inhibitors. The first generation benzimidazolone inhibitors were found to be potent inhibitors of wild-type HIV reverse transcriptase but were ineffective in the presence of common resistance mutations such as K103N and Y181C. A second generation benzimidazolone inhibitor (compound 42) not only showed inhibitory activity against wild-type HIV but also remained active against HIV containing the K103N, Y181C, and K103N/Y181C drug resistance mutations.
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Registered trials
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