- Discovery of Piragliatin-First Glucokinase Activator Studied in Type 2 Diabetic Patients
[作者:SARABU RAMAKANTH; BIZZARRO FRED T; CORBETT WENDY L; DVOROZNIAK MARK T; GENG WANPING; GRIPPO JOSEPH F; HAYNES NANCYELLEN; HUTCHINGS STANLEY; GAROFALO LISA; GUERTIN KEVIN R; HILLIARD DARRYL W; KABAT MAREK; KESTER ROBERT F; KA WANG; LIANG ZHENMIN; MAHANEY PAIGE E; MARCUS LINDA; MATSCHINSKY FRANZ M; MOORE DAVID; RACHA JAGDISH; RADINOV ROUMEN; REN YI; QI LIDA; PIGNATELLO MICHAEL; SPENCE CHERYL L; STEELE THOMAS; TENGI JOHN; GRIMSBY JOSEPH,期刊:Journal of Medicinal Chemistry, 页码:7021-7036 , 文章类型: Article,,卷期:2012年55-16]
- Glucokinase (GK) activation as a potential strategy to treat type 2 diabetes (T2D) is well recognized. Compound 1, a glucokinase activator (GKA) lead that we have previously disclosed, caused reversible hepatic lipidosis...
- Discovery and Optimization of 1,3,4-Trisubstituted-pyrazolone Derivatives as Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonists
[作者:HUANG HUANG; YU YING; GAO ZHENTING; ZHANG YONG; LI CHENJING; XU XING; JIN HUI; YAN WENZHONG; MA RUOQUN; ZHU JIN; SHEN XU; JIANG HUALIANG; CHEN LILI; LI JIAN,期刊:Journal of Medicinal Chemistry, 页码:7037-7053 , 文章类型: Article,,卷期:2012年55-16]
- LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 +/- 11.75 mu M). On the basis of 11, 26 new derivatives (12a-z) were desi...
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