Respiratorius AB, Magistratsvägen 10, SE 226 43 Lund, Sweden.
Bioorg Med Chem Lett. 2010 Sep 1;20(17):4999-5003. doi: 10.1016/j.bmcl.2010.07.057. Epub 2010 Jul 19.
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.
本文描述了一系列新型四氢异喹啉酰胺的合成及支气管舒张作用。评估了这些化合物对离体人小气道 LTD4 收缩的舒张作用。一些化合物表现出高效的支气管舒张特性。肉桂酰胺 71 被选为进一步研究的候选物，作为一种新型的支气管舒张剂，有望用于治疗肺部疾病。
