Acta Pharm. 55 (2005) 27-46

Biological activities of isatin and its derivatives

SURENDRA NATH PANDEYA^1*, SIVAKUMAR SMITHA²,  MAYANK JYOTI²   and SESHAIAH KRISHNAN SRIDHAR³

snpandeya@rediffmail.com

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

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