Synthesis of novel tetrahydroisoquinoline bronchodilators

Bioorg Med Chem Lett. 2010 Sep 1;20(17):4999-5003. doi: 10.1016/j.bmcl.2010.07.057. Epub 2010 Jul 19.

Abstract

The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly efficacious bronchorelaxing properties. Cinnamide 71 was selected for further studies and constitutes a promising candidate as a novel bronchorelaxing agent for the treatment of pulmonary disorders.

MeSH terms

  • Bronchi / drug effects
  • Bronchodilator Agents / chemical synthesis*
  • Bronchodilator Agents / chemistry
  • Bronchodilator Agents / pharmacology
  • Humans
  • In Vitro Techniques
  • Isoquinolines / chemical synthesis*
  • Isoquinolines / chemistry
  • Isoquinolines / pharmacology
  • Structure-Activity Relationship

Substances

  • Bronchodilator Agents
  • Isoquinolines