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Research Paper | Pharmaceutical Science | India | Volume 7 Issue 5, May 2018
Synthesis, Characterisation and its Anti Bacterial Activity of Dalfampridine Genotoxic Impurity 1, 2-DI (PYRIDINE-4-YL) Hydrazine
Mythili A [3] | Dr. Vijayabaskaran M [2] | Dr. Yogesh D B [2]
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.
Keywords: Dalfampridine, Genotoxic impurities, Oxidation, Nitration, Azo coupling, Reduction, Deoxygenation, LC-MS, 1H NMR, Melting point, Anti bacterial activity, Agar well cup method
Edition: Volume 7 Issue 5, May 2018,
Pages: 8 - 12