In an effort to develop potent anticonvulsant agents, we have synthesized some novel schiff's bases of 3-{[2-({(E)-[substituted) phenyl] methylidene} amino) ethyl] amino} quinoxalin-2(1H)-one and evaluated for in vivo anticonvulsant activity. All the compounds were characterized by IR, 1 H NMR data. This activity was carried out on pentylenetetrazole-induced seizure model. Compounds (IIIb) and (IIIc) Showed maximum time for straub tail and clonic convulsions. That means they possess good activity compared with standard.Animals treated with compounds (IIIb) and (IIIe) were recovered from this activity.
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The term prodrug refers to a pharmacologically inactive compound that is converted to an active drug by a metabolic bio transformation. Prodrug design may be useful in circumventing problems associated such as Solubility, absorption and distribution, site specificity, Instability, prolonged release, Toxicity. Prodrug design comprises an area of drug research devoted to optimization of drug delivery. These are designed to maximize the amount of active drug that reaches its site of action, through manipulation of the physicochemical, biopharmaceutical or pharmacokinetic properties of the drug. Almost all drugs possess some undesirable physicochemical and biological properties. Their therapeutic efficacy can be improved by minimizing or eliminating the undesirable properties while retaining the desirable ones. This can be achieved through biological, physical or chemical means. The prodrug approach, a chemical approach using reversible derivatives, can be useful in the optimization of the clinical application of a drug. Hence prodrug approach gained attention as a technique for improving drug therapy.
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