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Kittisak Sripha. Synthesis and biological evaluation of 3-triazolyl-coumarin derivatives as acetylcholinesterase and B-Amyloid aggregation inhibitors. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2017.
Synthesis and biological evaluation of 3-triazolyl-coumarin derivatives as acetylcholinesterase and B-Amyloid aggregation inhibitors
Name: Suthira Yanaso
Organization :
Mahidol university. Faculty of Pharmacy
Name: Nattasit Tongpan
Organization :
Huachiew Chalermprakiet university. Faculty of Pharmacy
Name: Jaturong Pratuangdejkul
Organization :
Mahidol university. Faculty of Pharmacy
Name: Worawan Kitphati
Organization :
Mahidol university. Faculty of Pharmacy
Name: Kittisak Sripha
Organization :
Mahidol university. Faculty of Pharmacy
Email :
kittisak.srp@mahidol.ac.th
keyword:
3-triazolyl-coumarin derivatives
LCSH:
Beta-amyloid protein
LCSH:
Acetylcholinesterase
LCSH:
Alzheimer disease
Abstract:
Five new 3-triazolyl-coumarin derivatives (C1-C5) were designed and synthesized
as duo-actions, acetylcholinesterase and β-amyloid aggregation inhibitors, for the effective
treatment of Alzheimers disease. All compounds were synthesized using click reaction and
obtained in moderate to high yield (ranging from 44 to 80%). The modified Ellman and
Thioflavin T fluorescence methods were used for screening acetylcholinesterase and β-amyloid
aggregation inhibitory activities, respectively. Among the test compounds, only C3 displayed
high potency against Aβ1-42 aggregation with inhibition value of 79%. The interference of Aβ
aggregation process of the best inhibitor, C3, was described by a molecular docking study using
Discovery Studio program. It was observed that coumarin ring of C3 formed π-π interaction
with Phe19 which involved intramolecular Aβ fibril formation. Unfortunately, the anti-AChE
of C3 was not attractive since the inhibition value of 16% was observed. Last but not least, this
study demonstrated the potent Aβ aggregation inhibitors, the newly synthesized C3, could be a
promising candidate for the development of lead molecule against Alzheimers disease.
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2017
Modified:
2562-08-20
Issued:
2019-08-20
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.1111-1116). 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
0.024021 วินาที
Suthira Yanaso
| 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 |
Nattasit Tongpan
| 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 |
Jaturong Pratuangdejkul
| 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 |
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 |
Kittisak Sripha
| 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 |