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