HIV, a dreadful virus has infected billions of people worldwide. It is spreading like anything despite the advances in the drug discovery. Even though innumerable strategies were designed most of them were in vain as the HIV virus has got inbuilt genetic mutation capability. Alongside, the virus is getting resistance to the chemical drugs. The chemical drugs are synthesized so as to target a particular protein of HIV which is most essential for its life. Few classes of drugs target the viruses in their latent stage and thereby reducing viral load. Some important classes of chemical drugs entail diarylpyrimidines, methoxy indoles and methoxy azoindoles etc. Some of the natural products are also derivatized to afford potent anti-HIV drugs. FDA (Food and Drug Administration) has approved a large number of drugs after clinical investigation under different phases. According to mode of their action, they have been classified as antifibrotics, CCR5 antagonists, integrase inhibitors, latency reversing agents, maturation inhibitors, (NNRTIs), (NRTIs), protease inhibitors, rev inhibitors, etc. Here in we reported the chemicals drugs synthesized from the past to present which includes a wide variety of synthetic chemical drugs possessing anti HIV potency. Also, the various drugs approved by the FDA were described.