Synthesis of C-2 and C-3 substituted quinolines and their evaluation as anti-HIV-1 agents.

Purvi Shah, Dharav Naik, Nisha Jariwala, Deepali Bhadane,Sanjay Kumar,Smita Kulkarni,Kamlesh Kumar Bhutani,Inder Pal Singh

Bioorganic Chemistry（2018）

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摘要

•Thirty-one substituted quinolines were synthesized exploring C-2 and C-3 positions.•Synthesized compounds included imines, amides and 1,3,4-oxadiazoles of quinoline.•All the compounds were evaluated for anti-HIV-1 potential.•31 showed activity against HIV-1VB59 (IC50 3.35 μM) and HIV-1UG070 (IC50 2.57 μM).•31 showed entry inhibition (IC50 1.40 μM) and cell fusion inhibition (IC50 0.96 μM).

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关键词

Quinoline,α,β-Unsaturated amide,1,3,4-Oxadiazole,Anti-HIV-1,Entry inhibition,Fusion inhibition

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