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Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-12-24 , DOI: 10.1016/j.bmcl.2017.12.051
Paul S. Humphries , Ross Bersot , John Kincaid , Eric Mabery , Kerryn McCluskie , Timothy Park , Travis Renner , Erin Riegler , Tod Steinfeld , Eric D. Turtle , Zhi-Liang Wei , Erik Willis

A series of novel carbazole-containing amides and ureas were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound 50 was selected for further profiling.



中文翻译:

含咔唑的酰胺和脲:发现隐花色素调节剂作为降糖药

合成了一系列新型的含咔唑的酰胺和脲。这些化合物的结构-活性关系研究导致了强效隐色调节剂的鉴定。基于所需的药代动力学/药效学参数和在db / db小鼠中的功效研究结果,选择化合物50进行进一步分析。

更新日期:2017-12-24
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