Synthesis, Characterisation and its Anti Bacterial Activity of Dalfampridine Genotoxic Impurity 1, 2-DI (PYRIDINE-4-YL) Hydrazine
Journal: International Journal of Science and Research (IJSR) (Vol.7, No. 5)Publication Date: 2018-05-05
Authors : Mythili A; Vijayabaskaran M; Yogesh D B;
Page : 8-12
Keywords : Dalfampridine; Genotoxic impurities; Oxidation; Nitration; Azo coupling; Reduction; Deoxygenation; LC-MS; 1H NMR; Melting point; Anti bacterial activity; Agar well cup method;
Abstract
Objective Dalfampridine and its impurities are used as intermediates for synthesis of chemicals, pharmaceuticals and agrochemical industry, antineoplastic, anticoagulant, anti-inflammatory, antispasmodic and antiasthmatic drugs, fungicide and as additives for foodstuffs [1]. Moreover its derivatives mainly used to treat multiple sclerosis so [2], the drug availability should be within the limit as per ICH guidelines. In the present study was aimed to synthesize 1, 2-di (pyridine-4-yl) hydrazine and evaluate antibacterial activity by using agar cup method. Methods 1, 2-di (pyridine-4-yl) hydrazine synthesized by number of steps which is N-Oxidation, Nitration, Azo coupling and Deoxygenation followed by Reducion. Synthesized molecule was characterized by LC-MS, HPLC, 1H NMR and serially diluted test solution of three doses of 1, 2-di (pyridine-4-yl) hydrazine (50g/ml, 75g/ml and 100g/ml) were added in the cups which is present in bacteria spreaded petridish. All the plates stood incubated for 24 hrs at 370C [3]. MIC (Minimum Inhibitory Concentration) was measured and compared with gentamycin as a positive control. Results 1, 2-di (pyridine-4-yl) hydrazine molecule was synthesized and characterized as per methods. The synthesized 1, 2-di (pyridine-4-yl) hydrazine (100g/ml) was found to be effective and it exhibited significant antibacterial activity against its direction of Escherichia-coli Pseudomonas-aeruginosa Bacillus-subtilis Staphylococcus-aureus which activity is lesser than standard drug gentamycin. Whereas100g/ml dose showed higher anti bacterial activity with more zone of inhibition than 75g/ml and 50g/ml dose of synthesized molecule. Conclusions The results proposed 100g/ml of synthesized 1, 2-di (pyridine-4-yl) hydrazine showed significant antibacterial activity but less activity than standard drug gentamycin.
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