作为GPR88激动剂的苯甘醇和苯胺的设计、合成与评估
Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.
作者信息
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
机构信息
Discovery, Bristol-Myers Squibb, 5 Research Parkway, Wallingford, CT 06492, USA.
Lexicon Pharmaceuticals, 350 Carter Rd, Princeton, NJ 08540, USA.
出版信息
Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28.
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.
GPR88活性的小分子调节剂（激动剂、拮抗剂或调节剂）作为治疗包括精神分裂症在内的多种精神疾病的潜在药物备受关注。一系列苯甘醇和苯胺类似物已被制备并评估其GPR88激动剂活性和药代动力学（PK）性质。
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