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

Synthesis, biological evaluation and molecular modeling of 2-amino-2-phenylethanol derivatives as novel ?2-adrenoceptor agonists

A novel series of 2-amino-2-phenylethanol derivatives were developed as ?2-adrenoceptor agonists. Among them, 2-amino-3-fluoro-5-(2-hydroxy-1-(isopropylamino)ethyl)benzonitrile (compound 2f) exhibited the highest activity (EC50 = 0.25 nM) in stimulating ?2-adrenoceptor-mediated cellular cAMP production with a 763.6 fold selectivity over the ?1-adrenoceptor. The (S)-isomer of 2f was subsequently found to be 8.5 fold more active than the (R)-isomer. Molecular docking was performed to determine the putative binding modes of this new class of ?2-adrenoceptor agonists. Taken together, these data show that compound 2f is a promising lead compound worthy of further study for the development of ?2-adrenoceptor agonists.

» Author: Xinyue Ge, Yongmei Mo, Gang Xing, Lei Ji, Haiyan Zhao, Jianfang Chen, Bin He, Xuyao Chen, Ruijuan Xing, Xiaoqiang Li, Ying Zhao, Jinyan Li, Haining Yan, Anthony Yiu-Ho Woo, Yuyang Zhang, Bin Lin, Li Pan, Maosheng Cheng

» Reference: Bioorganic Chemistry

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