Acta Pharm. 55 (2005) 27-46

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Review article 

Biological activities of isatin and its derivatives


1Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221 005, India
2Department of Pharmaceutical Sciences, Faculty of Health and Medical Sciences, Allahabad Agricultural Institute-Du, Allahabad-211 007, India
3C. L. Baid Mehta College of Pharmacy, Jothi Nagar, Thorapakkam, Chennai-600 096, India
Received July 2, 2003      Accepted January 25, 2005

Isatin is an endogenous compound identified in humans that possesses wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activity and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin N-Mannich bases of isatin-3-thiosemicarbazones have shown antiviral and tuberculostatic activity. Methisazone is an effective compound against variola and vaccinia viruses. The N-dimethyl and morpholino derivative of 5-methyl isatin and trimethoprim exhibited an EC50 of more than 4.3 and 17.7 microgram mL-1 and 17.7 microgram mL-1, respectively. Isatin (3-o-nitrophenyl)hydrazone has shown activity against Walker carcinoma-256. Various substituted indolinones showed antitubercular activity against M. tuberculosis H37Rv with MIC ranging from 10-20 microgram mL-1. Isatin derivatives of Mannich bases had fibrinolytic, muscle relaxant, antiallergic, immunosuppressant, and antithrombotic activity. Isatin showed cardioinhibitory effect on frog heart, and hypotensive, respiratory depression and antidiuretic effects.

Keywords: isatin, Mannich bases, semicarbazones, anticonvulsant, antimicrobial, antitubercular effects