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

Author(s): Shivani Mahajan, Shiv Gupta, Nisha Jariwala, Deepali Bhadane, Late K.K. Bhutani, Smita Kulkarni*, Inder Pal Singh*.

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 9 , 2018

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Graphical 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.

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Article Details

Year: 2018
Page: [937 - 944]
Pages: 8
DOI: 10.2174/1570180815666171212143339
Price: $58

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