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14
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5
Objective: In this study we aimed to synthesize some hydrazide derivatives of imidazo[1,2-a]pyridine and to evaluate their anti-cholinesterase activities. Method: The reaction of imidazo[1,2-a]pyridine-2-carboxylic acid hydrazides with various benzaldehydes gave N-(benzylidene)imidazo[1,2-a]pyridine-2-carboxylic acid hydrazide derivatives. The chemical structures of the compounds were elucidated by IR, 1H-NMR, FAB+-MS spectral data and elemental analysis. In the pharmacological study, anti-cholinesterase activities of these compounds have been evaluated by using modified Ellman’s spectrophotometric method. Results: Three of the synthesized compounds (2, 3 and 4) can be identified as promising anticholinesterase agents due to their inhibitory effect on AChE with IC50 value of 74.42±4.29, 43.26±7.28 and 18.29±2.31 μM, respectively when compared with Donepezil (IC50=0.058±0.002 μM). Conclusion: The halogen substitutions on phenyl ring have a crucial influence on anticholinesterase activity.
Objective: In this study we aimed to synthesize some hydrazide derivatives of imidazo[1,2-a]pyridine and to evaluate their anti-cholinesterase activities. Method: The reaction of imidazo[1,2-a]pyridine-2-carboxylic acid hydrazides with various benzaldehydes gave N-(benzylidene)imidazo[1,2-a]pyridine-2-carboxylic acid hydrazide derivatives. The chemical structures of the compounds were elucidated by IR, 1H-NMR, FAB+-MS spectral data and elemental analysis. In the pharmacological study, anti-cholinesterase activities of these compounds have been evaluated by using modified Ellman's spectrophotometric method. Results: Three of the synthesized compounds (2, 3 and 4) can be identified as promising anticholinesterase agents due to their inhibitory effect on AChE with IC50 value of 74.42±4. 29, 43.26±7.28 and 18.29±2.31 μM, respectively when compared with Donepezil (IC50=0.058±0.002 μM). Conclusion: The halogen substitutions on phenyl ring have a crucial influence on anticholinesterase activity.
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