Synthesis, Structural Analysis & Biological Evaluation of Anticonvulsant Activity of Pyrazole Derivatives Containing Thiourea
Journal Title: International Journal of Research in Pharmacy and Science - Year 2011, Vol 1, Issue 3
Abstract
Compounds were prepared in two steps. First, the chalcones were synthesized by direct condensation of aromatic aldehydes and the substituted acetophenone, using 20% potassium hydroxide in ethanol to form intermediate. Second, synthesis of compounds VN-1 to VN-5 was carried out by semithiacarbezide and above intermediate. 3-(4-Amino-phenyl)-5-(3-nitro-phenyl)-4,5-dihydro-pyrazole-1-carbothioicacid amide, (VN-2) revealed significant activity (75% protection), then 3-(4-Amino-phenyl)-5-(3-nitro-phenyl)-4, 5-dihydro-pyrazole-1-carbothioic acid (VN-2) showed 62.5% protection. Compound VN-3 showed mild/intermediate activity. Replacement of the 4-amino phenyl group by 4-bromo-phenyl and 2-bromo-4-methoxy-phenyl moiety as in VN-4 & VN-5 leads to decrease in % of protection of the compounds VN-4 and VN-5 respectively. Moreover, the 3-(4-Amino-phenyl) derivatives VN-1 and VN-2 were found to be more active. The order of percentage protection is VN-2 > VN-1> VN-3> VN-5 >VN-4. The spectroscopic analysis was performed for synthesized compounds. UV spectra of synthesized compounds were determined on UV shimadzu 1700 spectrophotometer and determined λmax of synthesized compounds. The IR spectra of synthesized compounds were obtained from FTIR, 2000A, ABB spectrophotometer (ZrCl2) in Smriti College of Pharmacy, Indore. The infra red spectra of each of the synthesized compounds shows characterisitic absorption in accordance to their structural functional groups. The 1H-NMR spectrums of synthesized compounds were shows chemical shifts is in good agreement with the structure of the synthesized compounds.
Authors and Affiliations
Vinayaditya Singh , Vikash Mishra
Keywords
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