Aim: Purpose of the present work is to synthesize the pro-pro-drugs of Glycine and evaluate for their anticonvulsant activity in albino rats with brain specific sustained release action in various biological fluids. Materials and Methods: Prepared and synthesized propro- drugs of Glycine nicotinate by esterification with different alcohols and admiration with nicotinic acid. In present work pro-prodrug of Glycine nicotinate were synthesized by taking the Dihydropyridine as carrier molecules. The synthesized compounds have been characterized by IR, IH-NMR, C, H, N analysis and Mass spectral techniques and evaluated for their anticonvulsant activity in albino rats by chemoconvulsion method as well for oxidation in various biological fluids. All the synthesized compounds were found to be active and stable in biological fluids. Oxidized form of the conjugate inside the brain act as pro-pro-drug, which on hydrolysis yields parent drug in sustained release manner. The significance of the work is to treat neurological disorder implicated by Glycine. Results: Pro-pro-drug of Glycine nicotinate were synthesized effectively and showed anticonvulsant activity in slow release manners. Conclusion: This work has given a new synthetic strategy and result of anticonvulsant screening was found encouraging.