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Four Binding Site Hypothesis for Anticonvulsant Activity   Harish Rajak

Four Binding Site Hypothesis for Anticonvulsant Activity

76 страниц. 2012 год.
LAP Lambert Academic Publishing
Despite the development of several new anticonvulsants, over 30% of people with epilepsy do not have seizure control and others do so only at the expense of significant dose-related toxicity and unusual adverse effects. The semicarbazones based pharmacophoric model for anticonvulsant activity comprises of following four essential binding sites: (i) An aryl hydrophobic binding site; (ii) A hydrogen bonding domain; (iii)An electron donor group and (iv) Another hydrophobic-hydrophilic site regulating the pharmacokinetic properties of the anticonvulsant. In pursuit for better antiepileptic drug and the importance of semicarbazones as anticonvulsant pharmacophore, a series of novel semicarbazone were designed, synthesized and evaluated for their anticonvulsant activity. The results of the present studying confirmed that the pharmacophoric model with four binding sites is vital for anticonvulsant activity.
 
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