Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists

Bioorg Med Chem Lett. 2002 Jun 3;12(11):1533-5. doi: 10.1016/s0960-894x(02)00203-2.

Abstract

A series of phthalimide acid derivatives was synthesized and evaluated as leukotriene D(4) receptor antagonists. The tetrazolephthalimide LASSBio 552 (7) was shown to be able to inhibit the contractile activity induced by 100 nM of LTD(4) in guinea-pig tracheal strips with an IC(50) = 31.2 microM. In addition, LASSBio 552 (7) has been showed to present a better efficacy than zafirlukast (1) used as standard.

Publication types

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

MeSH terms

  • Animals
  • Anti-Asthmatic Agents / chemical synthesis*
  • Anti-Asthmatic Agents / chemistry
  • Anti-Asthmatic Agents / pharmacology*
  • Drug Design
  • Guinea Pigs
  • In Vitro Techniques
  • Indoles
  • Leukotriene Antagonists*
  • Membrane Proteins*
  • Models, Molecular
  • Molecular Conformation
  • Muscle Contraction / drug effects
  • Phenylcarbamates
  • Phthalimides / chemical synthesis*
  • Phthalimides / chemistry
  • Phthalimides / pharmacology*
  • Receptors, Leukotriene / chemistry
  • Sulfonamides
  • Tetrazoles / chemistry
  • Tosyl Compounds / pharmacology
  • Trachea / drug effects
  • Trachea / physiology

Substances

  • Anti-Asthmatic Agents
  • Indoles
  • Leukotriene Antagonists
  • Membrane Proteins
  • Phenylcarbamates
  • Phthalimides
  • Receptors, Leukotriene
  • Sulfonamides
  • Tetrazoles
  • Tosyl Compounds
  • phthalimide
  • cysteinyl leukotriene receptor 2
  • leukotriene D4 receptor
  • zafirlukast