发现吡唑基丙酰环己烯酰胺衍生物作为高亲和力烟酸受体 GPR109A 的完全激动剂。
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jun 1;20(11):3372-5. doi: 10.1016/j.bmcl.2010.04.013. Epub 2010 Apr 11.
PMID:20452209
Abstract
A series of pyrazolyl propionyl cyclohexenamides were discovered as full agonists for the high affinity niacin receptor GPR109A. The structure-activity relationship (SAR) studies were aimed to improve activity on GPR109A, reduce Cytochrome P450 2C8 (CYP2C8) and Cytochrome P450 2C9 (CYP2C9) inhibition, reduce serum shift and improve pharmacokinetic (PK) profiles.
摘要
一系列吡唑基丙酰环己烯酰胺被发现是高亲和力烟碱受体 GPR109A 的完全激动剂。构效关系 (SAR) 研究旨在提高对 GPR109A 的活性，降低细胞色素 P450 2C8 (CYP2C8) 和细胞色素 P450 2C9 (CYP2C9) 的抑制作用，减少血清转移并改善药代动力学 (PK) 特征。
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