Synthesis and cholinesterase inhibitory activity study of new piperidone grafted spiropyrrolidines |
| |
| Institution: | 1. Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia;2. Département de chimie, Faculté des Sciences de Monastir, Avenue de l''Environnement, 5019 Monastir, Tunisia;3. Department of Chemistry, Faculty of Science, Assiut University, 71516 Assiut, Egypt;4. Department of Chemistry, College of Science, United Arab Emirates University, P.O. Box 15551, Al Ain, United Arab Emirates;5. Department of Chemistry, Faculty of Science and Arts, King Khalid University, Mohail, Assir, Saudi Arabia;6. Department of Chemistry, Jamoum University College, Umm Al-Qura University, 21955 Makkah, Saudi Arabia |
| |
| Abstract: | Alzheimer’s disease (AD) is a prevalent neurodegenerative disorder, which affected 35 million people in the world. The most practiced approach to improve the life expectancy of AD patients is to increase acetylcholine neurotransmitter level at cholinergic synapses by inhibition of cholinesterase enzymes. A series of unreported piperidone grafted spiropyrrolidines 8(a-p) were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. Therein, compounds 8h and 8l displayed more potent AChE enzyme inhibition than standard drug with IC50 values of 1.88 and 1.37 µM, respectively. Molecular docking simulations for 8l possessing the most potent AChE inhibitory activities, disclosed its interesting binding templates to the active site channel of AChE enzymes. These compounds are remarkable AChE inhibitors and have potential as AD drugs. |
| |
| Keywords: | Spiropyrrolidines AChE and BChE activities Molecular docking Ionic liquid |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
