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A detailed review on HIV and its drugs was prepared. This broad spectrum of biochemical targets has been facilitated by the synthetic versatility of heterocyclic compounds, which has allowed the generation of a large number of structurally diverse derivatives. The objective of this review to systematically evaluate the pharmacological properties of various substituted heterocyclic compounds and collate these findings to be used as a guide for future structure-activity relationship and mode of action studies. This is the first review to comprehensively discuss the HIV and its drugs.