Anticonvulsant activity of newly synthesized benzoylhydrazones with 2H-chromene and coumarin moieties in ICR mice

European Chemistry Congress

June 16-18, 2016 Rome, Italy

Y Voinikov, Violina T Angelova, Pavlina A Andreeva- Gateva, Nikolay G Vassilev, Slavina Surcheva and Jana Tchekalarova

Medical University, Bulgaria
BAS-Institute of Organic Chemistry with Centre of Phytochemistry, Bulgaria
BAS-Institute of Neurobiology, Bulgaria

Posters & Accepted Abstracts: Chem Sci J

Abstract :

Several 2H-chromene and coumarin based benzoylhydrazones were synthesized and evaluated for their anticonvulsant activity and neurotoxicity. The structures of the newly synthesized compounds were confirmed by 1H and 13C NMR, FTIR and HRMS (ESI) spectroscopy. The initial anticonvulsant screening was performed using the maximal electroshock induced seizure tests (MES) and the subcutaneous pentylenetetrazol (scPTZ) test in ICR mice. As phenytoin was used as a standard drug, compounds 3a and 3c exhibited 50% and 100% protection, respectively, against tonic-clonic seizures and tendency to alleviate the mortality in the MES test at the highest dose of 300 mg/kg. Unlike diazepam (2.5 mg/kg), the compounds were unable to exhibit 100% suppression of clonic seizures in the scPTZ test, at the experimental doses. However, 3b demonstrated 50% while 3a - 37% protection against clonic seizures at a dose of 300 mg/kg in the scPTZ test. The mortality was also significantly diminished to 0 % and 13 %, respectively. Motor impairment, evaluated with the rotarod test, was minimal at 300 mg/kg. Taken together, the results suggest that the newly synthesized 2H-chromene- and coumarin based benzoylhydrazones could be efficient as adjuvants against secondarily generalized tonic-clonic seizures and primarily generalized seizures in humans. uli1985@abv.bg