Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88

Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88

[Display omitted] Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs have been prepared and evaluate...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-04, Vol.25 (7), p.1448-1452
Hauptverfasser: Dzierba, Carolyn D., Bi, Yingzhi, Dasgupta, Bireshwar, Hartz, Richard A., Ahuja, Vijay, Cianchetta, Giovanni, Kumi, Godwin, Dong, Li, Aleem, Saadat, Fink, Cynthia, Garcia, Yudith, Green, Michael, Han, Jianxin, Kwon, Soojin, Qiao, Ying, Wang, Jiancheng, Zhang, Yulian, Liu, Ying, Zipp, Greg, Liang, Zhi, Burford, Neil, Ferrante, Meredith, Bertekap, Robert, Lewis, Martin, Cacace, Angela, Grace, James, Wilson, Alan, Nouraldeen, Amr, Westphal, Ryan, Kimball, David, Carson, Kenneth, Bronson, Joanne J., Macor, John E.
Format: Artikel
Sprache:eng
Schlagworte:
Agonist
Amines - chemical synthesis
Amines - chemistry
Amines - pharmacology
Dose-Response Relationship, Drug
Drug Design
Ethanolamines - chemical synthesis
Ethanolamines - chemistry
Ethanolamines - pharmacology
GPR88
HEK293 Cells
Humans
Molecular Structure
Phenyl amine
Phenylglycinol
Receptors, G-Protein-Coupled - agonists
Schizophrenia
Structure-Activity Relationship
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Zusammenfassung:[Display omitted] Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs have been prepared and evaluated for their GPR88 agonist activity and pharmacokinetic (PK) properties.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.01.036