Synthesis and anti-inflammatory activity of novel (4-hydroxyphenyl)(2,4-dimethoxyphenyl) methanone derivatives

Arch Pharm (Weinheim). 2009 Aug;342(8):476-83. doi: 10.1002/ardp.200900021.

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.

MeSH terms

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

Substances

  • Anti-Inflammatory Agents
  • Benzophenones
  • Piperidines
  • piperidine
  • benzophenone
  • Carrageenan