Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Synthesis and screening of angularly fused pyrido[3',2':4,5]furo[3,2-d]pyrimidin-4(3H)-ones

Author(s): Vachala Seekarajapuram Dinakaran and Keloth Kaitheri Srinivasan

In the present study, a series of novel pyrido[3',2':4,5]furo[3,2-d]pyrimidin-4(3H)-ones were synthesised by condensing 3-amino-6-hydroxy-4-methyl furo[2,3-b]pyridine-2-carboxamide with different aromatic acids. The structure of the synthesized compounds was confirmed by spectral studies and the purity was checked by Thin layer chromatographic analysis. All the compounds (PFP-HM 1-7) were screened for their In vitroantioxidant and In vivoanti-inflammatory activities. Antioxidant activity of the synthesised compounds was assessed by DPPH method. Compound PFP-HM2 was found to be a potent antioxidant agent (IC50: 0.129 μM). The antiinflammatory activity was performed by rat paw oedema method. Ibuprofen was used as standard (100mg/kg body mass). Except compound PFP-HM3, all other compounds showed very good anti-inflammatory activity when compared with the standard. Compound PFP-HM6, at 1st h did not show any inhibition of inflammation. But after 2nd h, it showed 100% protection from inflammation. Compound PFP-HM 2 also showed very good percentage inhibition of inflammation from 1st h to 5th h (76-98.8%). These data revealed that the presence of 4- trifluoromethylphenyl, 4-chlorobenzyl, 3, 5-dimethoxyphenyl and 3-fluorophenyl substitutions in the fused pyrimidine systemplayed a major role in their biological activities.


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