In this section, you can access to the latest technical information related to the FUTURE project topic.

Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent ?2-adrenoceptor agonists

A series of novel ?2-adrenoceptor agonists with a 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one moiety was designed, synthesized and evaluated for biological activity in human embryonic kidney 293 cells and isolated guinea pig trachea. Compounds 9g and (R)-18c exhibited the most excellent ?2-adrenoceptor agonistic effects and high ?2/?1-selectivity with EC50 values of 36?pM for 9g and 21?pM for (R)-18c. They produced potent airway smooth muscle relaxant effects with fast onset of action and long duration of action in an in vitro guinea pig trachea model of bronchodilation. These results support further development of the two compounds into drug candidates.

» Author: Gang Xing, Li Pan, Ce Yi, Xiaoran Li, Xinyue Ge, Ying Zhao, Yichuang Liu, Jinyan Li, Anthony Woo, Bin Lin, Yuyang Zhang, Maosheng Cheng

» Reference: 10.1016/j.bmc.2018.10.043

» Publication Date: 01/11/2018

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