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.
Dalence-Guzmán
Maria F
MF
Respiratorius AB, Magistratsvägen 10, SE 226 43 Lund, Sweden.
Toftered
Jörgen
J
Oltner
Viveca Thornqvist
VT
Wensbo
David
D
Johansson
Martin H
MH
D001980:Bronchi / Q000187:drug effects; D001993:Bronchodilator Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D001993:Bronchodilator Agents; D007546:Isoquinolines