ArticleBioorganic & medicinal chemistry letters2012
Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Article in Bioorganic & medicinal chemistry letters, 2012. 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.
- Structural and pharmacological evaluation of a novel non-nucleoside reverse transcriptase inhibitor as a promising long acting nanoformulation for treating HIV.Antiviral research · 2019Article
- From in silico hit to long-acting late-stage preclinical candidate to combat HIV-1 infection.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.Bioorganic & medicinal chemistry letters · 2017Article
- Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection.Molecular pharmacology · 2017Article
- Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.ACS medicinal chemistry letters · 2014Article
- Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters · 2014Article
- Optimization of the antiviral potency and lipophilicity of halogenated 2,6-diarylpyridinamines as a novel class of HIV-1 NNRTIS.ChemMedChem · 2014Article
- A mechanistic and structural investigation of modified derivatives of the diaryltriazine class of NNRTIs targeting HIV-1 reverse transcriptase.Biochimica et biophysica acta · 2014Article
- Picomolar inhibitors of HIV reverse transcriptase featuring bicyclic replacement of a cyanovinylphenyl group.Journal of the American Chemical Society · 2013Article
- Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.Bioorganic & medicinal chemistry letters · 2013Article
- Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.Bioorganic & medicinal chemistry letters · 2013Article
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Authors and funding
7 authors.
Funding
Abstract
The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a-9e, indicating an accessible modification approach that could improve anti-HIV potency against wild-type and resistant strains, aqueous solubility, and metabolic stability. A new compound 9e not only exhibited extremely high potency against wild-type virus (EC(50) 0.53 nM) and several resistant viral strains (EC(50) 0.36-3.9 nM), but also showed desirable aqueous solubility and metabolic stability, which were comparable or better than those of the anti-HIV-1 drug TMC278 (2). Thus, new compound 9e might be a potential drug candidate for further development of novel next-generation NNRTIs.
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