Bioorganic and Medicinal Chemistry (2020)
Update date:2022-08-04
Topics:
Yi, Ce
Xing, Gang
Wang, Siqi
Li, Xiaoran
Liu, Yichuang
Li, Jinyan
Lin, Bin
Woo, Anthony Yiu-Ho
Zhang, Yuyang
Pan, Li
Cheng, Maosheng
A series of β2-adrenoceptor agonists with an 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one moiety is presented. The stimulatory effects of the compounds on human β2-adrenoceptor and β1-adrenoceptor were characterized by a cell-based assay. Their smooth muscle relaxant activities were tested on isolated guinea pig trachea. Most of the compounds were found to be potent and selective agonists of the β2-adrenoceptor. One of the compounds, (R)-18c, possessed a strong β2-adrenoceptor agonistic effect with an EC50 value of 24 pM. It produced a full and potent airway smooth muscle relaxant effect same as olodaterol. Its onset of action was 3.5 min and its duration of action was more than 12 h in an in vitro guinea pig trachea model of bronchodilation. These results suggest that (R)-18c is a potential candidate for long-acting β2-AR agonists.
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Doi:10.1002/chem.201803675
(2018)Doi:10.1016/S0022-328X(00)85955-0
(1981)Doi:10.1016/S0040-4039(01)89561-7
(1967)Doi:10.1021/jo00337a032
(1981)Doi:10.1016/j.tetlet.2004.08.037
(2004)Doi:10.1016/j.bmcl.2007.12.040
(2008)