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Design, Synthesis, Docking Studies and Biological Activities Novel 2,3-Diaryl-4-Quinazolinone Derivatives as Anti-HIV-1 Agents.

BACKGROUND
Although major efforts devoted to the efficient treatment of HIV-1 infection, it has remained one of the leading causes of deaths around the world. So development of anti-HIV-1 agents featuring novel structure is essential.


OBJECTIVE
To synthesize novel quinazolinone derivatives and evaluate their anti-HIV-1 activity.


METHOD
In this study, we designed and synthesized a series of novel 2,3-diaryl-4-quinazolinone derivatives using a one-pot multicomponent reaction. Then, the resulting derivatives were evaluated for anti-HIV-1 activity using Hela cell based single cycle replication assay.


RESULTS
Most of the compounds showed efficacy against HIV-1 replication and the compound 9c exhibited the highest activity with EC50 value of 37 μM. Docking studies indicated that synthesized compounds can interact with the key residues of the HIV-1 integrase active site. The binding poses of the most active compound was consistent with the HIV-1 integrase inhibitors.


CONCLUSION
Based on our results, these derivatives represent novel lead compounds for the development of new promising anti-HIV-1 agents.