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Design, Synthesis and anti-HIV-1 Activity of Modified Styrylquinolines

[ Vol. 15 , Issue. 9 ]

Author(s):

Shivani Mahajan, Shiv Gupta, Nisha Jariwala, Deepali Bhadane, Late K.K. Bhutani, Smita Kulkarni* and Inder Pal Singh*   Pages 937 - 944 ( 8 )

Abstract:


Background: Drug resistance and reservoirs of latent viral infection have prevented total eradication of the HIV-virus which underlines the need for continuous efforts in the discovery of new anti-HIV agents. The present study deals with the synthesis of novel compounds based on naturally occurring scaffolds and their evaluation as potential anti-HIV agents.

Objective: Design and synthesis of styrylquinoline scaffold based new molecules and evaluation of their anti-HIV-1 activity.

Methods: A series of forty three new styrylquinolines (SQLs) was designed and synthesized. The newly synthesized compounds were tested for anti-HIV-1 activity against HIV-1VB59 and HIV- 1UG070 primary isolates in TZM-bl cell lines.

Results: The most active compounds 9 and 34 (IC50 = 0.5-4.0 µM), also exhibited significant inhibition activity against HIV-1VB51 primary isolate in PBMCs (IC50 = 7.3 µM). Compounds 9 and 34 were also found to inhibit HIV-1 entry into host cells and fusion inhibitory activities. The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents.

Conclusion: The study encourages further exploration of SQL nucleus to design anti-HIV-1 agents.

Keywords:

Styrylquinoline, Anti-HIV-1, HIV-1VB59, HIV-1UG070, HIV-1VB51, SQL.

Affiliation:

Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S. A. S. Nagar-160 062, Punjab, Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S. A. S. Nagar-160 062, Punjab, Department of Molecular Virology, National AIDS Research Institute (NARI), Bhosari, Pune-411 026, Maharashtra, Department of Molecular Virology, National AIDS Research Institute (NARI), Bhosari, Pune-411 026, Maharashtra, Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S. A. S. Nagar-160 062, Punjab, Department of Molecular Virology, National AIDS Research Institute (NARI), Bhosari, Pune-411 026, Maharashtra, Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S. A. S. Nagar-160 062, Punjab

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