Analogues of Acifran: Agonists of the High and Low Affinity Niacin Receptors, GPR109a and GPR109b

详细信息    查看全文

• 作者：Jae-Kyu Jung ; Benjamin R. Johnson ; Tracy Duong ; Marc Decaire ; Jane Uy ; Tawfik Gharbaoui ; P. Douglas Boatman ; Carleton R. Sage ; Ruoping Chen ; Jeremy G. Richman ; Daniel T. Connolly ; Graeme Semple
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：April 5, 2007
• 年：2007
• 卷：50
• 期：7
• 页码：1445 - 1448
• 全文大小：47K
• 年卷期：v.50,no.7(April 5, 2007)
• ISSN：1520-4804

文摘

Recently identified GPCRs, GPR109a and GPR109b, thehigh and low affinity receptors for niacin, may represent good targetsfor the development of HDL elevating drugs for the treatment ofatherosclerosis. Acifran, an agonist of both receptors, has been testedin human subjects, yet until recently very few analogs had been reported.We describe a series of acifran analogs prepared using newly developedsynthetic pathways and evaluated as agonists for GPR109a andGPR109b, resulting in identification of compounds with improvedactivity at these receptors.