Synthesis of novel tetrahydroisoquinoline bronchodilators

The discovery and synthesis of bronchodilator 71 using a functional tissue assay is described. 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 airw...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-09, Vol.20 (17), p.4999-5003
Hauptverfasser:	Dalence-Guzmán, Maria F., Toftered, Jörgen, Oltner, Viveca Thornqvist, Wensbo, David, Johansson, Martin H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Asthma Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Bronchi - drug effects Bronchodilator Bronchodilator Agents - chemical synthesis Bronchodilator Agents - chemistry Bronchodilator Agents - pharmacology COPD Humans In Vitro Techniques Isoquinolines - chemical synthesis Isoquinolines - chemistry Isoquinolines - pharmacology Medical sciences Palladium catalyzed cross-coupling Pharmacology. Drug treatments Respiratory system Structure-Activity Relationship Tetrahydroisoquinoline
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Beschreibung
Zusammenfassung:	The discovery and synthesis of bronchodilator 71 using a functional tissue assay is described. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.07.057