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Dr. Abdelmotaal Abdelmajeid El-Shiekh Abdelmotaal Abdelmajeid :: Publications: |
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| Title: | Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41.
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| Authors: | Shibo Jiang, Srinivasa R. Tala, Hong Lu, Peng Zou, Ilker Avan, Tarek S. Ibrahim, Nader E. Abo-Dya, Abdelmotaal Abdelmajeid, Asim K. Debnath, Alan R. Katritzky |
| Year: | 2011 |
| Keywords: | Not Available |
| Journal: | Bioorganic & medicinal chemistry letters |
| Volume: | 21 |
| Issue: | 22 |
| Pages: | 6895-8. |
| Publisher: | Not Available |
| Local/International: | International |
| Paper Link: | Not Available |
| Full paper | Abdelmotaal Abdelmajeid El-Shiekh Abdelmotaal Abdelmajeid_Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans_pyrroles as HIV-1 fusion inhibitors targeting gp41.html |
| Supplementary materials | Not Available |
| Abstract: |
Based on molecular docking analysis of earlier results, we designed a series of 2,5-disubstituted furans/pyrroles (5a-h) as HIV-1 entry inhibitors. Compounds were synthesized by Suzuki-Miyaura cross coupling, followed by a Knoevenagel condensation or Wittig reaction. Four of these compounds were found to be effective in inhibiting HIV-1 infection, with the best compounds being 5f and 5h, which exhibited significant inhibition on HIV-1(IIIB) infection at micromolar levels with low cytotoxicity. These compounds are also effective in blocking HIV-1 mediated cell-cell fusion and the gp41 six-helix bundle formation, suggesting that they are also HIV-1 fusion inhibitors targeting gp41 and have potential to be developed as a new class of anti-HIV-1 agents. |
