In recent years, the discovery, identification, and development of biologically active compounds have gained a lot of importance. Numerous scaffolds have been synthesized using naphthalene, which has also been shown to have a wide range of therapeutic properties, including antimicrobial, antiviral, antiprotozoal, antidiabetic, anticancer, anti-inflammatory, antihypertensive, antipsychotic, antidepressant, anticonvulsant, and anti-neurodegenerative effects. The naphthalene-based compounds Naphyrone, tolnaftate, naftifine, nafcillin, terbinafine, propranolol, nabumetone, nafimidone, naproxen, duloxetine, lasofoxifene, and bedaquiline, among others, have also been approved by the FDA and are being marketed as medicines. Naphthalenes are a class of arenas in which two benzene rings are fused in an ortho position. Naphthalene is a white substance with a strong, pungent odour that is traditionally generated from coal tar. Thus, the naphthalene scaffold emerges as an essential building block in drug development due to its wide range of biological activities due to its structural modifications. This review examines the pharmacological properties of various chemically modified naphthalene-based compounds.