Evaluation and Synthesis of Polar Aryl- and Heteroaryl Spiroazetidine-Piperidine Acetamides as Ghrelin Inverse Agonists

[Image: see text] Several polar heteroaromatic acetic acids and their piperidine amides were synthesized and evaluated as ghrelin or type 1a growth hormone secretagogue receptor (GHS-R1a) inverse agonists. Efforts to improve pharmacokinetic and safety profile was achieved by modulating physicochemic...

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發表在:ACS Med Chem Lett
Main Authors: Orr, Suvi T. M., Beveridge, Ramsay, Bhattacharya, Samit K., Cameron, Kimberly O., Coffey, Steven, Fernando, Dilinie, Hepworth, David, Jackson, Margaret V., Khot, Vishal, Kosa, Rachel, Lapham, Kimberly, Loria, Paula M., McClure, Kim F., Patel, Jigna, Rose, Colin, Saenz, James, Stock, Ingrid A., Storer, Gregory, von Volkenburg, Maria, Vrieze, Derek, Wang, Guoqiang, Xiao, Jun, Zhang, Yingxin
格式: Artigo
語言:Inglês
出版: American Chemical Society 2014
在線閱讀:https://ncbi.nlm.nih.gov/pmc/articles/PMC4329598/
https://ncbi.nlm.nih.gov/pubmed/25699143
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500414n
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