Dr. R.A. Hajare*, S.A. Polshettiwar
Shri BSPM B.Pharmacy College, Ambajogai, Dist Beed, Maharastra, India
Maharastra Institute of Pharmacy, Kothrud, Pune, India
E-mail: [email protected]
A series of different schiffs bases of 5-substituted-1H indole-2, 3 dione were synthesized by refluxing ethanol with different aromatic primary amine and hydrazine. Then a series of different mannich bases were synthesized from schiffs bases of different 5-substituted-1H indole-2, 3 dione with different secondary aromatic amines in presence of formaldehyde. Structures of the synthesized compounds were confirmed by FT-IR, 1H-NMR, 13C NMR and mass spectral data. Compound 1a-p were screened for anti-convulsant activity, with increased in latency time and reduction in duration of convulsion as like the standard drug when compared, sod.valporate 300mg/kg. PTZ at a dose of 90mg/kg produced severe clonic convulsions in 88% of the mice injected, with a mean onset time of 3.61 ± 0.5 min and 80% mortality. Clonic convulsive activity lasted 2.3 ± 0.45 min and was followed by a postictal period of decreased motor activity and subsequently. Test result revealed that compounds at dose of 300 mg/kg, the severity and duration of the convulsive episode following PTZ were not observed.
Key words: 5-substituted-1H indole-2, 3 diones, schiffs bases, mannich bases, anti-convulsant.
Epilepsy is defined as a group of disorders in which there are recurrent episodes of altered cerebral function associated with paroxysmal excessive and hypersynchronus discharge of cerebral neurons (Lowenstein et al., 2002). The clinical accompaniments of these episodes seizures vary in manifestation from brief lapses of awareness to prolonged bouts of unconsciousness, limb jerking & incontinence. Each episode of neurological dysfunction is called a seizure. Seizure may be convulsive when they are accompanied by motor manifestations or may be manifested by other changes in neurologic function. (i.e. sensory, cognitive, emotional events)(Losher et al., 1993). Seizures are thought to arise from the cerebral cortex & not other central nervous system structures such as thalamus, brainstem or cerebellum. Isatin (1H-indole-2, 3-dione) and its derivatives demonstrate a diverse array of biological activities (Verma et al., 2004). Isatin and its 5-halo derivatives were reacted to form the schiff’s bases, mannich bases to form C-N, C=N bonds, from the spectral studies, Isatin undergoes reaction at C-3 and N-1 position and discuss the anti-convulsant activity (Pajouhesh et al., 1983).