A small chemical library of quinolone acid derivatives were synthesized as potential HIV-1 integrase inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. Their structures were characterized by NMR, MS and HRMS. The result indicates that quinolone acid derivatives having 3,4,5-trihydroxylated aromatic substituent on the N-1 position of quinolone ring exhibit good inhibition with IC50 of 2.6 μM.

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Six β-diketo derivatives of mono-substituted calix[4]arene were synthesized as potential HIV-1 integrase inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. Their structures were characterized by NMR and HRMS. All the title compounds as potential HIV-1 integrase inhibitors proved to be active in the micromolar range (6.7–37.6 μM) on the strand transfer step.

HIV-1 integrase (IN), which has no cellular counterpart, has been intensely studied over the past 15 years and has been fully validated as a therapeutic target with the first FDA approved IN inhibitor raltegravir. The quinolone acid GS-9137 (elvitegravir), which most probably will became the next candidate of IN inhibitors, is in the process of enrolling patients in the phase III clinical trials. This review focuses on small-molecules of quinolone acid derivatives, which have the similar pharmacophore of β-diketoacids, as integrase inhibitors with antiviral activity.