N,N-dialkylaminosubstituted chromones and isoxazoles as potential anti-inflammatory agents

Farmaco. 1999 Jul 30;54(7):452-60. doi: 10.1016/s0014-827x(99)00051-8.

Abstract

The ability of some N,N-dialkylaminosubstituted chromones and isoxazoles to inhibit the protein kinase C (PKC) dependent signal transduction pathway was tested. As a cellular model, human neutrophils stimulated with either phorbol myristate acetate (PMA) or formylmethionine-leucine-phenylalanine (f-MLF) were used. The efficiency of the compounds was established by their capacity to reduce the O2- production by activated human neutrophils. Compounds carrying a 3-bis(2-methoxyethyl)amino group, a substituent found active in previously tested tricyclic compounds, do not show significant anti-PKC activity in this study. On the other hand, substitution with a 1-piperidinyl group leads all tested compounds to a high biological activity against stimulated neutrophils.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Chromones / chemical synthesis*
  • Chromones / pharmacology
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Humans
  • In Vitro Techniques
  • Isoxazoles / chemical synthesis*
  • Isoxazoles / pharmacology
  • Neutrophil Activation / drug effects
  • Neutrophils / drug effects
  • Neutrophils / metabolism
  • Protein Kinase C / antagonists & inhibitors
  • Superoxides / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Chromones
  • Enzyme Inhibitors
  • Isoxazoles
  • Superoxides
  • Protein Kinase C