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Pathumwadee Yotmanee. Design, synthesis, biological evaluation and docking study of piperine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2020.
Design, synthesis, biological evaluation and docking study of piperine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
Name: Kanokporn Lehboon
Organization :
Ramkhamhaeng University. Faculty of Science
Name: Vachiraporn Ajavakom
Organization :
Ramkhamhaeng University. Faculty of Science
Name: Pathumwadee Yotmanee
Organization :
Ramkhamhaeng University. Faculty of Science
Email :
pathumwadeei@gmail.com
ThaSH:
Acetylcholinesterase
ThaSH:
Alkaloids
ThaSH:
Antioxidants
Abstract:
Alzheimer's disease (AD) caused by low level of acetylcholine (ACh) that can be enhanced by inhibiting the activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. At the present study, the structural modification of natural piperine (1) as potent anti-cholinesterase were synthesized to give the desired analogues 2 - 4 in acceptable yields. These analogues were then submitted for biological evaluation and molecular docking study. It was found that the inhibitory activity against AChE and BChE was consistency between docking Gold score and IC50 values. An ordering of AChE inhibitory activity was galantamine > 3 > 4 > 1 > 2. The key residues of the AChE active site attached to the piperine analogues were W286, Y133 and W86 residues locating in peripheral anionic site (PAS) and anionic site (AS) regions. For BChE, the piperine analogues have binding stability in the ordering of 2- 4 > 1 - 3. All piperine analogues were oriented in the same direction in BChE active site, which attached to the key residues i.e., P285, Y332 and H438 in PAS region. These results revealed the important data for further investigation in order to develop the piperine analogues as potent AChE and BChE inhibitors.
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2020
Modified:
2024-10-22
Issued:
2024-10-22
บทความ/Article
application/pdf
BibliograpyCitation :
In the Chemical Society of Thailand under the Patronage of Professor Dr. HRH Princess Chulabhorn in association, Thammasat University Faculty of Science and Technology. The Pure and Applied Chemistry International Conference 2020 (PACCON 2020) (PT28-34). Bangkok : Thammasat University
eng
©copyrights King Mongkut's University of Technology North Bangkok
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0.031424 วินาที
Kanokporn Lehboon
| Title | Contributor | Type |
|---|---|---|
| Theoretical evaluation of novel racemic tetrahydrocurcuminiod dihydropyrimidione (THC-DHPM) analogues as promising acetylcholinesterase inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Kanokporn Lehboon;Pathumwadee Yotmanee | บทความ/Article | |
| Design, synthesis, biological evaluation and docking study of piperine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Kanokporn Lehboon;Vachiraporn Ajavakom;Pathumwadee Yotmanee | บทความ/Article |
Vachiraporn Ajavakom
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis, biological evaluation and docking study of piperine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Kanokporn Lehboon;Vachiraporn Ajavakom;Pathumwadee Yotmanee | บทความ/Article |
Pathumwadee Yotmanee
| Title | Contributor | Type |
|---|---|---|
| Theoretical evaluation of novel racemic tetrahydrocurcuminiod dihydropyrimidione (THC-DHPM) analogues as promising acetylcholinesterase inhibitor
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Kanokporn Lehboon;Pathumwadee Yotmanee | บทความ/Article | |
| Design, synthesis, biological evaluation and docking study of piperine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Kanokporn Lehboon;Vachiraporn Ajavakom;Pathumwadee Yotmanee | บทความ/Article |