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Arch Pharm (Weinheim) ; 342(8): 476-83, 2009 Aug.
Article in English | MEDLINE | ID: mdl-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.


Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Anti-Inflammatory Agents/pharmacology , Benzophenones/chemical synthesis , Benzophenones/pharmacology , Piperidines/chemical synthesis , Piperidines/pharmacology , Animals , Carrageenan , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Edema/chemically induced , Edema/drug therapy , Male , Molecular Structure , Rats , Rats, Inbred Strains , Structure-Activity Relationship
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