Bouyssou Thierry, Rudolf Klaus, Hoenke Christoph, Lustenberger Philipp, Schnapp Andreas, Konetzki Ingo
Department of Pulmonary Diseases Research, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach, Germany.
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5237-40. doi: 10.1016/j.bmcl.2009.06.104. Epub 2009 Jul 4.
Beta2-adrenoceptor agonists with basic and acidic groups attached via an alkyl linker to the phenyl ethanolamine core were prepared and investigated in vitro and in vivo. The compounds exhibited a high potency in a functional cellular assay and a bronchoprotective effect in a guinea pig model which lasted over the complete study period of 5h.
制备了通过烷基连接基连接到苯乙醇胺核心上带有碱性和酸性基团的β2-肾上腺素能受体激动剂,并进行了体外和体内研究。这些化合物在功能性细胞试验中表现出高效能,在豚鼠模型中具有支气管保护作用,该作用在长达5小时的整个研究期间持续存在。