Nicotinamide N-oxides as CXCR2 antagonists

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1951-4. doi: 10.1016/s0960-894x(01)00326-2.

Abstract

A series of nicotinamide N-oxides was synthesized and shown to be novel, potent, and selective antagonists of the CXCR2 receptor. Furthermore, these compounds showed significant functional activity against GRO-alpha-driven human neutrophil chemotaxis. Compounds of this class may be useful for the treatment of inflammatory, auto-immune, and allergic disorders.

MeSH terms

  • Autoimmune Diseases / drug therapy
  • Binding Sites / physiology
  • Chemokine CXCL1
  • Chemokines, CXC*
  • Chemotactic Factors / metabolism*
  • Chemotaxis / drug effects*
  • Chemotaxis / physiology
  • Growth Substances / metabolism*
  • Humans
  • Hypersensitivity / drug therapy
  • Inflammation / drug therapy
  • Inhibitory Concentration 50
  • Intercellular Signaling Peptides and Proteins*
  • Interleukin-8 / metabolism*
  • Neutrophils / physiology
  • Niacinamide / analogs & derivatives*
  • Niacinamide / chemical synthesis
  • Niacinamide / pharmacology*
  • Protein Binding / physiology
  • Receptors, Interleukin-8B / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • CXCL1 protein, human
  • Chemokine CXCL1
  • Chemokines, CXC
  • Chemotactic Factors
  • Growth Substances
  • Intercellular Signaling Peptides and Proteins
  • Interleukin-8
  • Receptors, Interleukin-8B
  • Niacinamide
  • nicotinamide N-oxide