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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Pubblicato in:ACS Med Chem Lett
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2014
Accesso online: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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