An important bioactive heterocycle having several uses in medicinal chemistry, synthetic organic chemistry, material chemistry, and natural product is indole along with its analogues. Many bioactive indole-based heterocycles have important antibacterial, anti-inflammatory, analgesic, antiviral, antimalarial, chemotherapeutic, antifungal, and anti-TB effects, as well as antioxidant capabilities. Several well-known medications, including tadalafil, rizatriptan, sumatriptan, and fluvastatin are indole- based potential bioactive compounds. Based on the existing and latest evidence, researchers have focused on developing indole-based compounds with novel biological and pharmacological properties for decades. Owing to useful bioactivities, we have described many bioactive indoles and their synthetic methods in this review article.
Keywords: Indole, pharmaceutical, heterocycles, biological activity, COX-1 & COX-2 (cyclooxygenase), agonistic effects, MCR technique.