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.

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.