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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22条记录   Discovery of 6 alpha-Ethyl-23(S)-methylcholic Acid (S-EMCA, INT-777) as a Potent and Selective Agonist for the TGR5 Receptor, a Novel Target for Diabesity [作者：PELLICCIARI ROBERTO; GIOIELLO ANTIMO; MACCHIARULO ANTONIO; THOMAS CHARLES; ROSATELLI EMILIANO; NATALINI BENEDETTO; SARDELLA ROCCALDO; PRUZANSKI MARK; RODA ALDO; PASTORINI ELISABETTA; SCHOONJANS KRISTINA; AUWERX JOHAN,期刊：Journal of Medicinal Chemistry, 页码：7958-7961 , 文章类型： Article，,卷期：2009年52-24] In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C-23(S)methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic... Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists [作者：EVANS KAREN A; BUDZIK BRIAN W; ROSS SEAN A; WISNOSKI DAVID D; JIN JIAN; RIVERO RALPH A; VIMAL MYTHILY; SZEWCZYK GEORGE R; JAYAWICKREME CHANNA; MONCOL DAVID L; RIMELE THOMAS J; ARMOUR SUSAN L; WEAVER SUSAN P; GRIFFIN ROBERT J; TADEPALLI SARVA M; JEUNE MICHAEL R; SHEARER TODD W; CHEN ZIBIN B; CHEN LIHONG; ANDERSON DONALD L; BECHERER J DAVID; DE LOS FRAILES MAITE; JAVIER COLILLA FRANCISCO,期刊：Journal of Medicinal Chemistry, 页码：7962-7965 , 文章类型： Article，,卷期：2009年52-24] A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled receptor is described. Subsequent optimization ... Conformationally Constrained Mimetics of Laminin Peptide YIGSR as Precursors for Antimetastatic Disintegrins [作者：BELLA ANGELO; LEWIS HELEN; PHU JENNIFER; BOTTRILL ANDREW R; MISTRY SHARAD C; PULLAR CHRISTINE E; RYADNOV MAXIM G,期刊：Journal of Medicinal Chemistry, 页码：7966-7969 , 文章类型： Article，,卷期：2009年52-24] Conformationally constrained mimetics of the laminin cell-adhesion site, YIGSR, are described. The site is the natural antagonist of the integrin-associated laminin receptor 1 (LAMR1) known to mediate metastatic tumor ad... Potent and Orally Active Small-Molecule Inhibitors of the MDM2-p53 Interaction [作者：YU SHANGHAI; QIN DONGGUANG; SHANGARY SANJEEV; CHEN JIANYONG; WANG GUOPING; DING KE; MCEACHERN DONNA; QIU SU; NIKOLOVSKACOLESKA ZANETA; MILLER REBECCA; KANG SANMAO; YANG DAJUN; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：7970-7973 , 文章类型： Article，,卷期：2009年52-24] We report herein the design of potent and orally active small-molecule inhibitors of the MDM2-p53 interaction, Compound 5 binds to MDM2 with a K-i of 0.6 nM, activates p53 at concentrations its low as 40 nM, and potently... Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic Acid: An Orally Active, Selective Very Late Antigen-4 Antagonist [作者：MURO FUMIHITO; IIMURA SHIN; SUGIMOTO YUUICHI; YONEDA YOSHIYUKI; CHIBA JUN; WATANABE TOSHIYUKI; SETOGUCHI MASAKI; IIGOU YUTAKA; MATSUMOTO KEIKO; SATOH ATSUSHI; TAKAYAMA GENSUKE; TAIRA TOMOE; YOKOYAMA MIKA; TAKASHI TOHRU; NAKAYAMA ATSUSHI; MACHINAGA NOBUO,期刊：Journal of Medicinal Chemistry, 页码：7974-7992 , 文章类型： Article，,卷期：2009年52-24] We have focused on optimization of the inadequate pharmacokinetic profile of trans-4-substituted cyclohexanecarboxylic acid 5, which is commonly observed in many small molecule very late antigen-4 (VLA-4) antagonists. We... In Vitro and In Vivo Isotope Effects with Hepatitis C Protease Inhibitors: Enhanced Plasma Exposure of Deuterated Telaprevir versus Telaprevir in Rats [作者：MALTAIS FRANCOIS; JUNG YOUNG CHUN; CHEN MINZHANG; TANOURY JERRY; PERNI ROBERT B; MANI NAGRAJ; LAITINEN LEENA; HUANG HUI; LIAO SHENGKAI; GAO HONGYING; TSAO HONG; BLOCK ERIC; MA CHIEN; SHAWGO REBECCA S; TOWN CHRISTOPHER; BRUMMEL CHRISTOPHER L; HOWE DAVID; PAZHANISAMY S; RAYBUCK SCOTT; NAMCHUK MARK; BENNANI YOUSSEF L,期刊：Journal of Medicinal Chemistry, 页码：7993-8001 , 文章类型： Article，,卷期：2009年52-24] Telaprevir 2 (VX-950), an inhibitor of the hepatitis C virus (HCVa) NS3-4A protease, is in phase 3 clinical trials. One of the major metabolites of 2 is its P1-(R)-diastereoisomer, 3 (VRT-394), containing an inversion at...