Heterocyclic compounds are those cyclic compounds in which one or more of the ring carbons are replaced by another atom. Heterocyclic compounds are acquiring more importance in recent years because of their broad pharmacological activities. Among an extensive diversity of heterocycles that have been explored for developing pharmaceutically important molecule. Isatin (1H-indole-2, 3-dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. Indole has a benzene ring and pyrrole ring sharing one double bond. It is a heterocyclic system with 10 electrons from four double bonds and the lone pair from the nitrogen atom. It is built into proteins in the form of amino acid tryptophan. Isatin and its derivatives are used in organic synthesis and they are used in evaluating new product that possesses different, biological activities. In the past few decades, Isatin and its derivatives have received much attention due to their chemo- therapeutic values. Isatin derivatives that have been reported to show considerable pharmacological actions such as, anticonvulsant, antianixity and antipsychoactives activity. Indoles are the most ubiquitous compounds in nature, but also because they have a wide range of biological activities. Indoles act as lead compounds and are key building blocks in numerous pharmaceuticals. Indole derivatives constitute an important class of therapeutic agents in medicinal chemistry including antihypertensive, antiproliferative, antiviral, antitumor, analgesic, anti-inflammatory, antimicrobial, antifungal activities, etc. Although indole moiety is very small but is fascinated by scientists because of the diverse biological activities by not only indole but its various substituted derivatives as well. From these results, ideas for future molecular modifications leading to compounds with greater favorable pharmacological properties may be derived. In the present study, we have made an attempt to collect biological importance of isatin and Indole nucleus reported in the new millennium.
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