2D Pharmacophoric Design and Synthesis of Novel Pyrimidine Derivatives as Anticonvulsants

Title:2D Pharmacophoric Design and Synthesis of Novel Pyrimidine Derivatives as Anticonvulsants

Volume: 13 Issue: 2

Author(s): Chhanda C. Danta*, Satya B. Sahu and Trupti R. Swain

Affiliation:

• Department of Medicinal Chemistry, Dhadhichi College of Pharmacy, Cuttack-753002, Odisha,India

Keywords: 2D Pharmacophore, pyrimidines, anticonvulsant, neurotoxicity.

Abstract: 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.

Cite this article as:

Danta C. Chhanda*, Sahu B. Satya and Swain R. Trupti, 2D Pharmacophoric Design and Synthesis of Novel Pyrimidine Derivatives as Anticonvulsants, Current Bioactive Compounds 2017; 13 (2) . https://dx.doi.org/10.2174/1573407212666160527104556

DOI https://dx.doi.org/10.2174/1573407212666160527104556	Print ISSN 1573-4072
Publisher Name Bentham Science Publisher	Online ISSN 1875-6646