AIDS (Acquired Immuno Deficiency Syndrome) has found to be most fatal syndrome. The main causative agent of AIDS is HIV-1 integrase. Incorporation of viral DNA into the host cell genome could be translated as the basis of life-long infection. Therefore, this biochemical event, catalyzed by the enzyme integrase, is a pivotal step in viral life cycle and thus worthy of being exploited to develop anti-HIV chemotherapy. The review presented on different categories of compounds that have been studied for the inhibition of the HIV-1 integrase to develop anti-HIV agents. The categories are Oligonucleotides, Curcumin Analogues, Polyhydroxylated Aromatic Compounds, Diketo Acid,) Caffeoyl-based Inhibitors, Hydrazides and Amides, Tetracycline, Depsides and Depsidones.