1104606-44-1Relevant articles and documents
Discovery of MK-1421, a potent, selective sstr3 antagonist, as a development candidate for type 2 diabetes
Shah, Shrenik K.,He, Shuwen,Guo, Liangqin,Truong, Quang,Qi, Hongbo,Du, Wu,Lai, Zhong,Liu, Jian,Jian, Tianying,Hong, Qingmei,Dobbelaar, Peter,Ye, Zhixiong,Sherer, Edward,Feng, Zhe,Yu, Yang,Wong, Frederick,Samuel, Koppara,Madiera, Maria,Karanam, Bindhu V.,Reddy, Vijay B.,Mitelman, Stan,Tong, Sharon X.,Chicchi, Gary G.,Tsao, Kwei-Lan,Trusca, Dorina,Feng, Yue,Wu, Margaret,Shao, Qing,Trujillo, Maria E.,Eiermann, George J.,Li, Cai,Pachanski, Michele,Fernandez, Guillermo,Nelson, Donald,Bunting, Patricia,Morissette, Pierre,Volksdorf, Sylvia,Kerr, Janet,Zhang, Bei B.,Howard, Andrew D.,Zhou, Yun-Ping,Pasternak, Alexander,Nargund, Ravi P.,Hagmann, William K.
supporting information, p. 513 - 517 (2015/05/27)
The imidazolyl-tetrahydro-β-carboline class of sstr3 antagonists have demonstrated efficacy in a murine model of glucose excursion and may have potential as a treatment for type 2 diabetes. The first candidate in this class caused unacceptable QTc interval prolongation in oral, telemetrized cardiovascular (CV) dogs. Herein, we describe our efforts to identify an acceptable candidate without CV effects. These efforts resulted in the identification of (1R,3R)-3-(4-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl)-1-(1-ethyl-pyrazol-4-yl)-1-(3-methyl-1,3,4-oxadiazol-3H-2-one-5-yl)-2,3,4,9-tetrahydro-1H-β-carboline (17e, MK-1421).
OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS
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Page/Page column 48-49, (2011/08/04)
Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.