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Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.

Publication ,  Journal Article
Sun, L-Q; Qin, B; Huang, L; Qian, K; Chen, C-H; Lee, K-H; Xie, L
Published in: Bioorg Med Chem Lett
April 1, 2012

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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Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

April 1, 2012

Volume

22

Issue

7

Start / End Page

2376 / 2379

Location

England

Related Subject Headings

  • Solubility
  • Rilpivirine
  • Reverse Transcriptase Inhibitors
  • Rats
  • Pyrimidines
  • Nitriles
  • Molecular Structure
  • Microsomes, Liver
  • Medicinal & Biomolecular Chemistry
  • Inhibitory Concentration 50
 

Citation

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Sun, L.-Q., Qin, B., Huang, L., Qian, K., Chen, C.-H., Lee, K.-H., & Xie, L. (2012). Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett, 22(7), 2376–2379. https://doi.org/10.1016/j.bmcl.2012.02.055
Sun, Lian-Qi, Bingjie Qin, Li Huang, Keduo Qian, Chin-Ho Chen, Kuo-Hsiung Lee, and Lan Xie. “Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorg Med Chem Lett 22, no. 7 (April 1, 2012): 2376–79. https://doi.org/10.1016/j.bmcl.2012.02.055.
Sun L-Q, Qin B, Huang L, Qian K, Chen C-H, Lee K-H, et al. Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2376–9.
Sun, Lian-Qi, et al. “Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorg Med Chem Lett, vol. 22, no. 7, Apr. 2012, pp. 2376–79. Pubmed, doi:10.1016/j.bmcl.2012.02.055.
Sun L-Q, Qin B, Huang L, Qian K, Chen C-H, Lee K-H, Xie L. Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2376–2379.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

April 1, 2012

Volume

22

Issue

7

Start / End Page

2376 / 2379

Location

England

Related Subject Headings

  • Solubility
  • Rilpivirine
  • Reverse Transcriptase Inhibitors
  • Rats
  • Pyrimidines
  • Nitriles
  • Molecular Structure
  • Microsomes, Liver
  • Medicinal & Biomolecular Chemistry
  • Inhibitory Concentration 50