Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative
A new pyridine alkaloid derivative named as 2-(6-benzyl-4-oxo-5-phenyl-1,4-dihydro pyridine-3-yl)-benzoic acid ethylester (3) has been prepared by the reaction of ninhydrin with 1,3-diphenylacetonep-tosylhydrazone and the structure has been established with the help of spectral analysis and X-ray an...
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India
2015
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| Online Access: | http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/1/Asian_journal_of_chemistry_%284092-4096%29.pdf |
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iium-464442017-08-21T03:33:10Z http://irep.iium.edu.my/46444/ Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative Ghalib, Gaza Murad Hashim, Rokiah Mehdi, Sayed Hasan Da Silva, M. Fátima C. Guedes Sulaiman, Othman How, Fiona Ni Foong Kawamura, Fumio Jawad, Ali Algamal, Yousif Chan, Kit-Lam Murugaiyah, Vikneswaran QD Chemistry A new pyridine alkaloid derivative named as 2-(6-benzyl-4-oxo-5-phenyl-1,4-dihydro pyridine-3-yl)-benzoic acid ethylester (3) has been prepared by the reaction of ninhydrin with 1,3-diphenylacetonep-tosylhydrazone and the structure has been established with the help of spectral analysis and X-ray analysis. The title compound demonstrated potent inhibitory activity against butyrylcholinesterase (BChE; IC50 = 4.91 µM) comparable to physostigmine (IC50 = 4.72 x 10-1 µM). However it showed moderate inhibitory activity against acetylcholinesterase (AChE; IC50 = 82.00 µM)). It was BChE selective over AChE, in contrast to physostigmine, which was more AChE selective. Being a potent and selective BChE inhibitor, it may serve as a new class of drug for prevention of the progression of neurodegeneration as well for symptomatic treatment of Alzheimer patient. India 2015-07 Article PeerReviewed application/pdf en http://irep.iium.edu.my/46444/1/Asian_journal_of_chemistry_%284092-4096%29.pdf Ghalib, Gaza Murad and Hashim, Rokiah and Mehdi, Sayed Hasan and Da Silva, M. Fátima C. Guedes and Sulaiman, Othman and How, Fiona Ni Foong and Kawamura, Fumio and Jawad, Ali and Algamal, Yousif and Chan, Kit-Lam and Murugaiyah, Vikneswaran (2015) Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative. Asian Journal of Chemistry, 27 (11). pp. 4092-4096. ISSN 0970-7077 E-ISSN 0975-427X http://www.asianjournalofchemistry.co.in/User/ViewFreeArticle.aspx?ArticleID=27_11_35 10.14233/ajchem.2015.19102 |
| repository_type |
Digital Repository |
| institution_category |
Local University |
| institution |
International Islamic University Malaysia |
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IIUM Repository |
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Online Access |
| language |
English |
| topic |
QD Chemistry |
| spellingShingle |
QD Chemistry Ghalib, Gaza Murad Hashim, Rokiah Mehdi, Sayed Hasan Da Silva, M. Fátima C. Guedes Sulaiman, Othman How, Fiona Ni Foong Kawamura, Fumio Jawad, Ali Algamal, Yousif Chan, Kit-Lam Murugaiyah, Vikneswaran Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| description |
A new pyridine alkaloid derivative named as 2-(6-benzyl-4-oxo-5-phenyl-1,4-dihydro pyridine-3-yl)-benzoic acid ethylester (3) has been prepared by the reaction of ninhydrin with 1,3-diphenylacetonep-tosylhydrazone and the structure has been established with the help of spectral analysis and X-ray analysis. The title compound demonstrated potent inhibitory activity against butyrylcholinesterase (BChE; IC50 = 4.91 µM) comparable to physostigmine (IC50 = 4.72 x 10-1 µM). However it showed moderate inhibitory activity against acetylcholinesterase (AChE; IC50 = 82.00 µM)). It was BChE selective over AChE, in contrast to physostigmine, which was more AChE selective. Being a potent and selective BChE inhibitor, it may serve as a new class of drug for prevention of the progression of neurodegeneration as well for symptomatic treatment of Alzheimer patient. |
| format |
Article |
| author |
Ghalib, Gaza Murad Hashim, Rokiah Mehdi, Sayed Hasan Da Silva, M. Fátima C. Guedes Sulaiman, Othman How, Fiona Ni Foong Kawamura, Fumio Jawad, Ali Algamal, Yousif Chan, Kit-Lam Murugaiyah, Vikneswaran |
| author_facet |
Ghalib, Gaza Murad Hashim, Rokiah Mehdi, Sayed Hasan Da Silva, M. Fátima C. Guedes Sulaiman, Othman How, Fiona Ni Foong Kawamura, Fumio Jawad, Ali Algamal, Yousif Chan, Kit-Lam Murugaiyah, Vikneswaran |
| author_sort |
Ghalib, Gaza Murad |
| title |
Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| title_short |
Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| title_full |
Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| title_fullStr |
Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| title_full_unstemmed |
Synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| title_sort |
synthesis, crystal structure and cholinesterase enzymes inhibitory activities of new pyridine alkaloid derivative |
| publisher |
India |
| publishDate |
2015 |
| url |
http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/ http://irep.iium.edu.my/46444/1/Asian_journal_of_chemistry_%284092-4096%29.pdf |
| first_indexed |
2023-09-18T21:06:08Z |
| last_indexed |
2023-09-18T21:06:08Z |
| _version_ |
1777410945721565184 |