Isatin is a heterocyclic moiety which can be used for the synthesis of a large variety of heterocyclic compounds such as quinolines, indoles and as raw material for medicinal important drugs. This review gives an overview of the advances of isatin for the synthesis of various heterocyclic compounds and shows the various biological potentials such as anticonvulsant, sedative, hypnotic, monoamine oxidase inhibitors, antianxiety, antipsychoactives activity etc. Isatin derivatives displayed as potent anticonvulsant potential in a large variety of preclinical anticonvulsant models. Present review article is an attempt to compile the various central nervous system potential of synthesized isatin analogs which will serve as a valuable source of information for the researchers working in this field.