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Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2018-08-12 , DOI: 10.1016/j.bioorg.2018.08.009
Raju Suresh Kumar , Abdulrahman I. Almansour , Natarajan Arumugam , Dhaifallah M. Al-thamili , Alireza Basiri , D. Kotresha , Thota Sai Manohar , S. Venketesh , Mohammad Asad , Abdullah M. Asiri

Novel highly functionalized 2-amino-4H-pyrans were achieved in excellent yields under simple grinding at ambient temperature and were assessed for their potential for treating Alzheimer’s disease (AD). The 2-amino-4H-pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC50 of 1.98 ± 0.09 µM against acetylcholinesterase (AChE) and 10.62 ± 0.21 µM against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations.



中文翻译:

高度功能化的2-氨基-4 H-吡喃类作为有效的胆碱酯酶抑制剂

在环境温度下简单研磨下,即可以优异的收率获得新型高度官能化的2-氨基-4 H-吡喃,并评估了其治疗阿尔茨海默氏病(AD)的潜力。在两个芳基环上带有硝基的2-氨基-4 H-吡喃具有最高的活性,对乙酰胆碱酯酶(AChE)的IC 50为1.98±0.09 µM,对丁酰胆碱酯酶(BChE)的IC 50为10.62±0.21 µM。通过分子对接模拟揭示了AChE和BChE受体的活性。

更新日期:2018-08-12
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