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|標題:||QSAR for acetylcholinesterase and butyrylcholinesterase inhibition by cardiovascular drugs and benzodiazepines||作者:||Chiou, S.Y.
|關鍵字:||torpedo-californica;binding||Project:||Medicinal Chemistry Research||期刊/報告no：:||Medicinal Chemistry Research, Volume 14, Issue 5, Page(s) 297-308.||摘要:||
Five common cardiovascular drugs, lovastatin, simvastatin, amlodipine besylate, nifedipine, and hydralazine hydrochloride, and two common benzodiazepines, diazepam and chlordiazepoxide hydrochloride, are all reversible mixed-type inhibitors of acetylcholinesterase and butyrylcholinesterase. The pK(i) values for acetylcholinesterase and butyrylcholinesterase inhibitions by these drugs are linearly correlated with the molecular weights, with slopes of 0.005 and 0.0021, respectively. Therefore, van der Waals' interactions between acetylcholinesterase and these drugs are stronger than those between butyrylcholinesterase probably due to a small active site gorge and a significant peripheral anionic site for acetylcholinesterase. The fact that the pKi values for both butyrylcholinesterase and acetylcholinesterase inhibitions are linearly correlated with each other suggests that both enzyme inhibitions proceed via a common mechanism. Furthermore, acetylcholinesterase and butyrylcholinesterase inhibitors such as tacrine, donepezil, rivastigmine, and galantamine are currently used to manage Alzheimer's disease. Since amlodipine besylate is a very potent inhibitor of both cholinesterases, amlodipine besylate may, like donepezil, be useful in Alzheimer's disease treatment.
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