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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共36条记录   Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonists: Mesylpropoxy Appendage Lowers Lipophilicity and Improves ADME Properties [作者：CHRISTIANSEN ELISABETH; DUEHANSEN MARIA E; URBAN CHRISTIAN; GRUNDMANN MANUEL; SCHROEDER RALF; HUDSON BRIAN D; MILLIGAN GRAEME; CAWTHORNE MICHAEL A; KOSTENIS EVI; KASSACK MATTHIAS U; ULVEN TROND,期刊：Journal of Medicinal Chemistry, 页码：6624-6628 , 文章类型： Article，,卷期：2012年55-14] FFA1 (GPR40) is a new target for treatment of type 2 diabetes. We recently identified the potent FFA1 agonist TUG-469 (5). Inspired by the structurally related TAK-875, we explored the effects of a mesylpropoxy appendage... Novel Imidazol-1-ylmethyl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as Potent and Selective CYP11B1 Inhibitors for the Treatment of Cushing's Syndrome [作者：YIN LINA; LUCAS SIMON; MAURER FRAUKE; KAZMAIER ULI; HU QINGZHONG; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：6629-6633 , 文章类型： Article，,卷期：2012年55-14] CYP11B1 inhibition is a promising therapy for Cushing's syndrome. Starting from etomidate, references I and II, the title compounds were designed and synthesized. Cyclopropyl analogue 4 was identified as a CYP11B1 inhibi... New Nitrogen Containing Substituents at the Indole-2-carboxamide Yield High Potent and Broad Spectrum Indolylarylsulfone HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors [作者：LA REGINA GIUSEPPE; COLUCCIA ANTONIO; BRANCALE ANDREA; PISCITELLI FRANCESCO; FAMIGLINI VALERIA; COSCONATI SANDRO; MAGA GIOVANNI; SAMUELE ALBERTA; GONZALEZ EMMANUEL; CLOTET BONAVENTURA; SCHOLS DOMINIQUE; ESTE JOSE A; NOVELLINO ETTORE; SILVESTRI ROMANO,期刊：Journal of Medicinal Chemistry, 页码：6634-6638 , 文章类型： Article，,卷期：2012年55-14] New indolylarylsulfone (IAS) derivatives bearing nitrogen containing substituents at the indole-2-carboxamide inhibited the HIV-1 WT in MT-4 cells at low nanomolar concentrations. In particular, compound 9 was uniformly ... Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases [作者：ROSE NATHAN R; WOON ESTHER C Y; TUMBER ANTHONY; WALPORT LOUISE J; CHOWDHURY RASHEDUZZAMAN; LI XUAN SHIRLEY; KING OLIVER N F; LEJEUNE CLARISSE; NG STANLEY S; KROJER TOBIAS; CHAN MUN CHIANG; RYDZIK ANNA M; HOPKINSON RICHARD J; CHE KA HING; DANIEL MICHELLE; STRAINDAMERELL CLAIRE; GILEADI CARINA; KOCHAN GRAZYNA; LEUNG IVANHOE K H; DUNFORD JAMES; YEOH KAR KHENG; RATCLIFFE PETER J; BURGESSBROWN NICOLA; VON DELFT FRANK; MULLER SUSANNE; MARSDEN BRIAN; BRENNAN PAUL E; MCDONOUGH MICHAEL A; OPPERMANN UDO; KLOSE ROBERT J; SCHOFIELD CHRISTOPHER J; KAWAMURA AKANE,期刊：Journal of Medicinal Chemistry, 页码：6639-6643 , 文章类型： Article，,卷期：2012年55-14] The JmjC oxygenases catalyze the N-demethylation of N-epsilon-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform f...