Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines
A new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Conf...
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| Format: | Article |
| Language: | English |
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Elsevier
2015-03-01
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| Series: | Biotechnology Reports |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2215017X14000496 |
| _version_ | 1818284960953401344 |
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| author | Karthikeyan Elumalai Mohammed Ashraf Ali Manogaran Elumalai Kalpana Eluri Sivaneswari Srinivasan |
| author_facet | Karthikeyan Elumalai Mohammed Ashraf Ali Manogaran Elumalai Kalpana Eluri Sivaneswari Srinivasan |
| author_sort | Karthikeyan Elumalai |
| collection | DOAJ |
| description | A new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (4a–l) was substantiated by TLC, different spectral data IR, 1H NMR, mass spectra and elemental analysis. The synthesized compounds were evaluated for acetyl and butyl cholinesterase (AChE and BuChE) inhibitor activity. The titled compounds exhibited weak, moderate or high AChE and BuChE inhibitor activity. Especially, compound (4l) showed the best AChE and BuChE inhibitory activity of all the 1,2,3,4-tetrahydropyrimidine derivatives, with an IC50 value of 0.11 μM and 3.4 μM. |
| first_indexed | 2024-12-13T01:01:07Z |
| format | Article |
| id | doaj.art-13e06f9aff684ad3a45200c86c45891d |
| institution | Directory Open Access Journal |
| issn | 2215-017X |
| language | English |
| last_indexed | 2024-12-13T01:01:07Z |
| publishDate | 2015-03-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Biotechnology Reports |
| spelling | doaj.art-13e06f9aff684ad3a45200c86c45891d2022-12-22T00:04:41ZengElsevierBiotechnology Reports2215-017X2015-03-015C1610.1016/j.btre.2014.10.007Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidinesKarthikeyan Elumalai0Mohammed Ashraf Ali1Manogaran Elumalai2Kalpana Eluri3Sivaneswari Srinivasan4New Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, IndiaNew Drug Discovery Research, Department of Medicinal Chemistry, Sunrise University, Alwar, Rajasthan 301030, IndiaFaculty of Pharmaceutical Sciences, UCSI University, Cheras, Kuala Lumpur 56000, MalaysiaFaculty of Pharmaceutical Sciences, UCSI University, Cheras, Kuala Lumpur 56000, MalaysiaCollege of Pharmacy, Sree Vidyanikethan Educational Trust, Tirupati 517102, IndiaA new series of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-(3-oxobutanoyl)pyrazine-2-carboxamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (4a–l) was substantiated by TLC, different spectral data IR, 1H NMR, mass spectra and elemental analysis. The synthesized compounds were evaluated for acetyl and butyl cholinesterase (AChE and BuChE) inhibitor activity. The titled compounds exhibited weak, moderate or high AChE and BuChE inhibitor activity. Especially, compound (4l) showed the best AChE and BuChE inhibitory activity of all the 1,2,3,4-tetrahydropyrimidine derivatives, with an IC50 value of 0.11 μM and 3.4 μM.http://www.sciencedirect.com/science/article/pii/S2215017X14000496PyrazinamideTetrahydropyrimidinesBiginelli reactionAcetyl cholinesterase inhibitor |
| spellingShingle | Karthikeyan Elumalai Mohammed Ashraf Ali Manogaran Elumalai Kalpana Eluri Sivaneswari Srinivasan Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines Biotechnology Reports Pyrazinamide Tetrahydropyrimidines Biginelli reaction Acetyl cholinesterase inhibitor |
| title | Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines |
| title_full | Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines |
| title_fullStr | Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines |
| title_full_unstemmed | Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines |
| title_short | Acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1,2,3,4-tetrahydropyrimidines |
| title_sort | acetylcholinesterase enzyme inhibitor activity of some novel pyrazinamide condensed 1 2 3 4 tetrahydropyrimidines |
| topic | Pyrazinamide Tetrahydropyrimidines Biginelli reaction Acetyl cholinesterase inhibitor |
| url | http://www.sciencedirect.com/science/article/pii/S2215017X14000496 |
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