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

Synthesis and biological evaluation of ?2-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold

A new series of ?2-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold was synthesized. Evaluation of the compounds using cell assays and an in vitro guinea pig trachea relaxation assay showed that 8-hydroxy-5-(2-hydroxy-1-((4-hydroxyphenethyl)amino)ethyl)quinolin-2(1H)-one (compound 5j) has the best pharmacological profile among all the evaluated compounds. The (S)-isomer of 5j was subsequently found to be the active enantiomer with a promising EC50 value of 1.26?nM in stimulating ?2-adrenoceptor-mediated cAMP accumulation and a substantially higher selectivity for the ?2 than for the ?1 subtype. The putative binding mode of (S)-5j revealed by molecular docking of the ?2-adrenoceptor resembles that in agonist binding. Taken together, these results showed that compound (S)-5j is a promising compound worthy of further study for the development of ?2-adrenoceptor agonists.

» Author: Xinyue Ge, Anthony Yiu-Ho Woo, Gang Xing, Yali Lu, Yongmei Mo, Ying Zhao, Yi Lan, Jinyan Li, Haining Yan, Li Pan, Yuyang Zhang, Bin Lin, Maosheng Cheng

» Reference: European Journal of Medicinal Chemistry, Volume 152

» Publication Date: 25/05/2018

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