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Uthai Wichai. Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2017.
Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives
Name: Salinee Khamsaeng
Organization :
Naresuan University. Faculty of Science
Email :
salineekh55@email.nu.ac.th
Name: Worawan Kitphati
Organization :
Mahidol University. Faculty of Pharmacy
Organization :
Mahidol University. Faculty of Pharmacy
Name: Uthai Wichai
Organization :
Naresuan University. Faculty of Science
LCSH:
Acetylcholinesterase
LCSH:
Alzheimer's disease
LCSH:
Benzaldehyde
LCSH:
Choline
LCSH:
Acetic acid
Abstract:
The acetylcholinesterase (AChE), the importance enzyme for central nervous
system, converts acetylcholine to choline and acetic acid. Inhibition of acetylcholinesterase
increases cholinergic transmission; consequently, relives the symptom of Alzhemers disease.
Currently, several drugs are approved to use for treatment of AD including galantamine,
tacrine and donepezil. They exhibited some disadvantages such as poor intestinal absorption,
low gastrointestinal disturbances and low bioavailability. Previously, vanillin (miLogP =
1.07), a widely used spice for food ingredients, was investigated on AChE inhibitor and it
showed moderate activity. This led us to investigate fluorinated vanillin derivatives in order
to improve AChE inhibition by replacing OCH3 with F on aromatic residue maintaining logP
< 5.0 (Lipinskis rule).
In this investigation, 3-fluoro-4-hydroxybenzaldehyde (2) was synthesized via formylation
reaction using 4-fluorophenol as starting material to obtain desired products with 41% yield.
Then, 2 was converted to 3-fluoro-4-hydroxybenzylamine hydrochloride (6) in order to
improve the solubility. After that, AChE inhibition was evaluated and it was found that 6
(IC50=1.27±0.04 mM) exhibited higher AChE inhibition than 4-hydroxybenzlamine salt (7) as
control (IC50=2.62 ± 0.23 mM). This was probably due to dipole moment change on aromatic
residue resulting in an enhancement of aromatic π-π interaction with AChE.
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2017
Modified:
2562-08-21
Issued:
2019-08-21
บทความ/Article
application/pdf
BibliograpyCitation :
In Chemical Society of Thailand under the Patronage of Her Royal Hghness Princess Chulabhorn Mahidol and King Mongkut's University of Technology North Bangkok Faculty of Applied Science. Pure and Applied Chemistry International Conference (PACCON 2017) (pp.1143-1148). Bangkok : Chemical Society of Thailand under the Patronage of Her Royal Hghness Princess Chulabhorn Mahidol
eng
©copyrights King Mongkut's University of Technology North Bangkok
RightsAccess:
ใช้เวลา
0.035851 วินาที
Salinee Khamsaeng
| Title | Contributor | Type |
|---|---|---|
| Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Salinee Khamsaeng;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article |
Worawan Kitphati
| Title | Contributor | Type |
|---|---|---|
| Synthesis and biological evaluation of 3-triazolyl-coumarin derivatives as acetylcholinesterase and B-Amyloid aggregation inhibitors
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Suthira Yanaso;Nattasit Tongpan;Jaturong Pratuangdejkul;Worawan Kitphati;Kittisak Sripha | บทความ/Article | |
| Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Salinee Khamsaeng;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article | |
| Biological activity of vanillin derivative
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Suwichan Majakorn;Wikorn Panyain;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article |
Nuntavan Bunyapraphatsara
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| Biosynthesis of C22-polyunsaturated fatty acids (PUFAs) in the moss physcomitrella patens by the algae paviova sp 5-elongasa :
มหาวิทยาลัยสงขลานครินทร์. สำนักทรัพยากรการเรียนรู้คุณหญิงหลง อรรถกระวีสุนทร Songsri Kaewsuwan;Nuntavan Bunyapraphatsara | งานวิจัย/Research report | |
| Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Salinee Khamsaeng;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article | |
| Biological activity of vanillin derivative
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Suwichan Majakorn;Wikorn Panyain;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article |
Uthai Wichai
| Title | Contributor | Type |
|---|---|---|
| Acetylcholinesterase inhibition of fluorinated benzaldehyde derivatives
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Salinee Khamsaeng;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article | |
| Biological activity of vanillin derivative
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Suwichan Majakorn;Wikorn Panyain;Worawan Kitphati;Nuntavan Bunyapraphatsara;Uthai Wichai | บทความ/Article |