Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88. Issue 7 (1st April 2015)

• Record Type: Journal Article
• Authors: 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.;
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 7(2015)
• Page Start: 1448
• Page End: 1452
• Publication Date: 2015-04-01
• Subjects: GPR88 -- Agonist -- Schizophrenia -- Phenylglycinol -- Phenyl amine; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.01.036
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: 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.