Design, synthesis and anticonvulsant activity of some new 5,7-dibromoisatin semicarbazone derivatives

Authors

  • Dheeraj Kumar Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • Vijay Kumar Sharma Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • Rajeev Kumar Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • Tejendra Singh Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • Hariram Singh Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • Amar Deep Singh Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India
  • R.K. Roy Dr. K. N. Modi Institute of Pharmaceutical Education and Research, Inside Cotton Mill Compound, Modinagar, Ghaziabad, Pin-201201, U. P., India

Keywords:

dibromoisatin, anticonvulsant, maximal electroshock, antidepressant activity

Abstract

A series of 5,7-dibromoisatin semicarbazones have been synthesized in good yield, involving aryl urea and aryl semicarbazide formation. The structures of the synthesized compounds were confirmed on the basis of their spectral data. All the compounds were evaluated for anticonvulsant and CNS depressant activities. Anticonvulsant activity was determined after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) induced seizure method and minimal motor impairment was determined by rotarod test. A computational study was carried out for prediction of pharmacokinetic properties and making them potentially promising agents for the treatment of epilepsy. Compounds (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(4-chlorophenyl)semicarbazide (DH-05), (Z)-1-(5,7-dibromo-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-11) and (Z)-1-(5,7-dibromo-1-methyl-2-oxoindolin-3-ylidene)-4-(3-chloro-4-fluorophenyl)semicarbazide (DH-12) exhibited prominent anticonvulsant effect in the series with little or no neurotoxicity and little CNS depressant effect as compared to standard drug.

Published

2013-07-11

How to Cite

Kumar, D., Sharma, V. K., Kumar, R., Singh, T., Singh, H., Singh, A. D., & Roy, R. (2013). Design, synthesis and anticonvulsant activity of some new 5,7-dibromoisatin semicarbazone derivatives. EXCLI Journal, 12, 628–640. Retrieved from https://www.excli.de/index.php/excli/article/view/1180

Issue

Section

Original articles