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  • Title: Synthesis and anti-inflammatory activity of novel (4-hydroxyphenyl)(2,4-dimethoxyphenyl) methanone derivatives.
    Author: Vinaya K, Naika R, Kumar CS, Ranganath SR, Prasad SB, Krishna V, Rangappa KS.
    Journal: Arch Pharm (Weinheim); 2009 Aug; 342(8):476-83. PubMed ID: 19526563.
    Abstract:
    In the scope of the research program aiming to perform the synthesis and pharmacological evaluation of novel possible anti-inflammatory compounds, in this manuscript, we report the synthesis of novel carboxamide 9a-d and thioamide 10a-d derivatives from the benzophenone and piperidine nucleus. Variation in the functional group at the N-terminal of piperidine led to two sets of compounds, bearing the carboxamide and thioamide, respectively. The characterization of this new class of compounds was performed with (1)H-NMR, LC-MS, IR, and elemental analysis. The newly synthesized compounds were screened for their anti-inflammatory activity by carrageenan-induced foot pad oedema assay and were compared with a standard drug. All the compounds exhibited anti-inflammatory activity at the dose of 30 mg/kg p.o. with varying degree from 52 to 67% inhibition of oedema. The compounds 9d and 10d with dichloro and fluoro substitution showed more potent activity at 30 mg/kg p.o. than the standard drug.
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