Synthesis of novel tetrahydroisoquinoline bronchodilators

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.

The discovery and synthesis of bronchodilator 71 using a functional tissue assay is described.Figure optionsDownload as PowerPoint slide