2D Pharmacophoric Design and Synthesis of Novel Pyrimidine Derivatives as Anticonvulsants
Background: Convulsion is a central neurological disorder and it occurs due to excess firing of the neurons. Globally, the number of patients suffering by convulsion is increasing day by day. There is a current need of discovery and development of new potential anticonvulsant agents. Methods: A series of novel pyrimidine derivatives (1a to 2e) were synthesized from benzaldehyde, ethylacetoacetate, thiourea or urea through single pot operation following Biginelli reaction and subsequently the products were modified by two steps reaction to obtain the pharmacophoric demanded molecules. The newly synthesized compounds were characterized by FTIR, 1H and 13C NMR, ESI-MS and elemental analyses. The anticonvulsant activity of all the title compounds was investigated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) models and their neurotoxicity was also evaluated by rotarod method in albino mice. Results: Compounds 1a, 1b, 2a and 2b were found to be active as compared to phenytoin and carbamazepine as standards. Compound N-(diphenylmethylene)-6-methyl-4-phenyl-2-thioxo-1, 2, 3, 4- tetrahydropyrimidine-5-carbohydrazide (1b) has emerged as a lead in this series with no neurotoxicity. Conclusion: Compound 1b can further be evaluated by the researchers to test its potency and toxicity for future pursuit..
| Medienart: |
Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:13 |
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| Enthalten in: |
Current bioactive compounds - 13(2017), 2, Seite 130-136 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chhanda C. Danta [VerfasserIn] |
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OLC1995541494 |
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| 520 | |a Background: Convulsion is a central neurological disorder and it occurs due to excess firing of the neurons. Globally, the number of patients suffering by convulsion is increasing day by day. There is a current need of discovery and development of new potential anticonvulsant agents. Methods: A series of novel pyrimidine derivatives (1a to 2e) were synthesized from benzaldehyde, ethylacetoacetate, thiourea or urea through single pot operation following Biginelli reaction and subsequently the products were modified by two steps reaction to obtain the pharmacophoric demanded molecules. The newly synthesized compounds were characterized by FTIR, 1H and 13C NMR, ESI-MS and elemental analyses. The anticonvulsant activity of all the title compounds was investigated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) models and their neurotoxicity was also evaluated by rotarod method in albino mice. Results: Compounds 1a, 1b, 2a and 2b were found to be active as compared to phenytoin and carbamazepine as standards. Compound N-(diphenylmethylene)-6-methyl-4-phenyl-2-thioxo-1, 2, 3, 4- tetrahydropyrimidine-5-carbohydrazide (1b) has emerged as a lead in this series with no neurotoxicity. Conclusion: Compound 1b can further be evaluated by the researchers to test its potency and toxicity for future pursuit. | ||
| 700 | 0 | |a Satya B. Sahu |4 oth | |
| 700 | 0 | |a Trupti R. Swain |4 oth | |
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