Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes

[Image: see text] 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, tel...

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Vydáno v:ACS Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2015
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4434471/
https://ncbi.nlm.nih.gov/pubmed/26005524
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500514w
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