所选卤代噻吩查耳酮的胆碱酯酶抑制活性
Cholinesterase Inhibitory Activities of Selected Halogenated Thiophene Chalcones.
作者信息
Parambi Della G T, Aljoufi Fakhrya, Murugaiyah Vikneswaran, Mathew Githa E, Dev Sanal, Lakshminarayanan Balasubramanain, Hendawy Omnia M, Mathew Bijo
机构信息
Department of Pharmaceutical Chemistry, Jouf University, Sakaka, Al Jouf-2014, Saudi Arabia.
Department of Pharmacology, College of Pharmacy, Al- Jouf University, Sakaka, Al Jouf-2014, Saudi Arabia.
出版信息
Cent Nerv Syst Agents Med Chem. 2019;19(1):67-71. doi: 10.2174/1871524918666181119114016.
BACKGROUND
Dual-acting human monoamine oxidase B (hMAO-B) and cholinesterase (ChE) inhibitors are more effective than the classic one-drug one-target therapy for Alzheimer's disease (AD).
METHODS
The ChE inhibitory ability of some halogenated thiophene chalcone-based molecules known to be selective hMAO-B inhibitors was evaluated.
RESULTS
Based on the IC50 values, the selected compounds were found to moderately inhibit ChE, with IC50 values in the range of 14-70 µM. Among the synthesised molecules, T8 and T6 showed the most potent inhibitory activity against AChE and BChE, respectively.
CONCLUSION
Taken together, the data revealed that T8 could be further optimized to enhance its AChE inhibitory activity.
背景
双作用人单胺氧化酶B（hMAO-B）和胆碱酯酶（ChE）抑制剂比经典的单药单靶点疗法治疗阿尔茨海默病（AD）更有效。
方法
评估了一些已知为选择性hMAO-B抑制剂的卤代噻吩查尔酮类分子的ChE抑制能力。
结果
根据半数抑制浓度（IC50）值，发现所选化合物对ChE有中度抑制作用，IC50值在14 - 70 μM范围内。在合成的分子中，T8和T6分别对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）表现出最强的抑制活性。
结论
综上所述，数据表明T8可进一步优化以增强其AChE抑制活性。
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