Design, synthesis, and biological evaluation of novel 4-hydro-quinoline-3-carboxamide derivatives as an immunomodulator

Bioorg Med Chem Lett. 2005 Jun 15;15(12):2980-5. doi: 10.1016/j.bmcl.2005.04.040.

Abstract

A series of novel quinoline-3-carboxamide derivatives were synthesized and evaluated for their immunomodulatory activity. The compounds were tested in vitro for effects on spleen lymphocyte proliferation and TNF-alpha production by macrophage. Three compounds showed immunomodulatory profiles similar to and more potent than those of linomide and FR137316 and were selected for further pharmacological studies in vivo.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Proliferation / drug effects*
  • Cells, Cultured
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Hydroxyquinolines / pharmacology
  • Immunologic Factors / chemical synthesis*
  • Immunologic Factors / chemistry
  • Immunologic Factors / pharmacology*
  • Lymphocytes / drug effects
  • Lymphocytes / immunology
  • Macrophages / drug effects
  • Macrophages / immunology
  • Macrophages / metabolism*
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Rats
  • Spleen / drug effects
  • Spleen / immunology
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Hydroxyquinolines
  • Immunologic Factors
  • Quinolines
  • Tumor Necrosis Factor-alpha
  • roquinimex