Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.

作者信息

Alikhani Vahid, Beer David, Bentley David, Bruce Ian, Cuenoud Bernard M, Fairhurst Robin A, Gedeck Peter, Haberthuer Sandra, Hayden Claire, Janus Diana, Jordan Lynne, Lewis Christine, Smithies Kirsty, Wissler Elke

机构信息

Novartis Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom.

出版信息

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4705-10. doi: 10.1016/j.bmcl.2004.06.086.

DOI:10.1016/j.bmcl.2004.06.086

PMID:15324892

Abstract

The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the beta-phenethyl-amino-substituent has been extended beyond the methyl ether residue present in the parent compound are described. Evaluation of these analogues as beta(2)-adrenoceptor agonists was used to provide an insight into the factors controlling the magnitude and duration of receptor activation.

摘要