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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17条记录   Novel Cyclic Phosphinic Acids as GABA(C) rho Receptor Antagonists: Design, Synthesis, and Pharmacology [作者：GAVANDE NAVNATH; YAMAMOTO IZUMI; SALAM NOERIS K; AI TUHOA; BURDEN PETER M; JOHNSTON GRAHAM A R; HANRAHAN JANE R; CHEBIB MARY,期刊：ACS Medicinal Chemistry Letters, 页码：11-16 , 文章类型： Article，,卷期：2011年2-1] Understanding the role of GABA(C) receptors in the central nervous system is limited due to a lack of specific ligands. Novel gamma-aminobutyric acid (GABA) analogues based on 3-(aminomethyl)-1-oxo-1-hydroxy-phospholane ... Study of Kaempferol Glycoside as an Insulin Mimic Reveals Glycon To Be the Key Active Structure [作者：YAMASAKI KAZUAKI; HISHIKI RYOGO; KATO EISUKE; KAWABATA JUN,期刊：ACS Medicinal Chemistry Letters, 页码：17-21 , 文章类型： Article，,卷期：2011年2-1] Diabetes mellitus is increasing in prevalence with patient numbers rising throughout the world. Current treatments for-diabetes mellitus focus on control of blood glucose levels. Certain kinds of flavonoids or their glyc... First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases [作者：HILLE ULRIKE E; ZIMMER CHRISTINA; VOCK CARSTEN A; HARTMANN ROLF W,期刊：ACS Medicinal Chemistry Letters, 页码：2-6 , 文章类型： Article，,卷期：2011年2-1] Outgoing from an etomidate-based design concept, we succeeded in the development of a series of highly active and selective inhibitors of CYP11B1, the key enzyme of cortisol biosynthesis, as potential drugs for the treat... Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277 [作者：LINIGER MARC; NEUHAUS CHRISTIAN; HOFMANN TATJANA; FRANSIOLIIGNAZIO LUCA; JORDI MICHEL; DRUECKES PETER; TRAPPE JOERG; FABBRO DORIANO; ALTMANN KARLHEINZ,期刊：ACS Medicinal Chemistry Letters, 页码：22-27 , 文章类型： Article，,卷期：2011年2-1] The natural product L-783277 is a resorcylic lactone type covalent kinase inhibitor We prepared the 5'-deoxy analogue of L-783277 (1) in a stereoselective fashion. Remarkably, this analogue retains almost the full kinase... Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors [作者：BURGER MATTHEW T; KNAPP MARK; WAGMAN ALLAN; NI ZHIJIE; HENDRICKSON THOMAS; ATALLAH GORDANA; ZHANG YANCHEN; FRAZIER KELLY; VERHAGEN JOELLE; PFISTER KEITH; NG SIMON; SMITH AARON; BARTULIS SARAH; MERRIT HANNE; WEISMANN MARION; XIN XIAOHUA; HAZNEDAR JOSHUA; VOLIVA CHARLES F; IWANOWICZ ED; PECCHI SABINA,期刊：ACS Medicinal Chemistry Letters, 页码：34-38 , 文章类型： Article，,卷期：2011年2-1] Phospoinositide-3-kinases (PI3K) are important oncology targets due to the deregulation of this signaling pathway in a wide variety of human cancers. series of 2 morpholino, 4-substituted, 6-(3-hydroxyphenyl) pyrimidines... Short-Chain HDAC Inhibitors Differentially Affect Vertebrate Development and Neuronal Chromatin [作者：FASS DANIEL M; SHAH RISHITA; GHOSH BALARAM; HENNIG KRISTA; NORTON STEPHANIE; ZHAO WENNING; REIS SURYA A; KLEIN PETER S; MAZITSCHEK RALPH; MAGLATHLIN REBECCA L; LEWIS TIMOTHY A; HAGGARTY STEPHEN J,期刊：ACS Medicinal Chemistry Letters, 页码：39-42 , 文章类型： Article，,卷期：2011年2-1] Carboxylic acids with known central nervous system and histone deacetylase (HDAC) inhibitory activities were converted to hydroxamic acids and tested using a suite of in vitro biochemical assays with recombinant HDAC iso... Automated Lead Optimization of MMP-12 Inhibitors Using a Genetic Algorithm [作者：PICKETT STEPHEN D; GREEN DARREN V S; HUNT DAVID L; PARDOE DAVID A; HUGHES IAN,期刊：ACS Medicinal Chemistry Letters, 页码：28-33 , 文章类型： Article，,卷期：2011年2-1] Traditional lead optimization projects involve long synthesis and testing cycles, favoring extensive structure-activity relationship (SAR) analysis and molecular design steps, in an attempt to limit the number of cycles ... SARs at the Monoamine Transporters for a Novel Series of Modafinil Analogues [作者：CAO JIANJING; PRISINZANO THOMAS E; OKUNOLA OLUYOMI M; KOPAJTIC THERESA; SHOOK MATTHEW; KATZ JONATHAN L; NEWMAN AMY HAUCK,期刊：ACS Medicinal Chemistry Letters, 页码：48-52 , 文章类型： Article，,卷期：2011年2-1] A series of modafinil (1) analogues were synthesized wherein (1) para-halo substitutents were added to the aryl rings, (2) the sulfoxide function was removed, and (3) the primary amide group was replaced with secondary a... Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands [作者：OISHI SHINYA; MISU RYOSUKE; TOMITA KENJI; SETSUDA SHOHEI; MASUDA RYO; OHNO HIROAKI; NANIWA YOUSUKE; IEDA NAHOKO; INOUE NAOKO; OHKURA SATOSHI; UENOYAMA YOSHIHISA; TSUKAMURA HIROKO; MAEDA KEIICHIRO; HIRASAWA AKIRA; TSUJIMOTO GOZOH; FUJII NOBUTAKA,期刊：ACS Medicinal Chemistry Letters, 页码：53-57 , 文章类型： Article，,卷期：2011年2-1] Kisspeptin is a member of the RFamide neuropeptide family that is implicated in gonadotropin secretion. Because kisspeptin-GPR54 signaling is implicated in the neuroendocrine regulation of reproduction, GPR54 ligands rep... Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile [作者：CARCACHE DAVID; VRANESIC IVO; BLANZ JOACHIM; DESRAYAUD SANDRINE; FENDT MARKUS; GLATTHAR RALF,期刊：ACS Medicinal Chemistry Letters, 页码：58-62 , 文章类型： Article，,卷期：2011年2-1] A focused chemical optimization effort of a compound 1 based on metabolite elucidation is described, resulting in 15i, a highly potent and selective mGlu5 receptor antagonist with an improved pharmacokinetic profile comp... Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity [作者：SEBHAT IYASSU K; FRANKLIN CHRISTOPHER; LO MICHAEL M C; CHEN DAVID; JEWELL JAMES P; MILLER RANDY; PANG JIANMEI; PALYHA OKSANA; KAN YANQING; KELLY THERESA M; GUAN XIAOMING; MARSH DONALD J; KOSINSKI JENNIFER A; METZGER JOSEPH M; LYONS KATHRYN; DRAGOVIC JASMINKA; GUZZO PETER R; HENDERSON ALAN J; REITMAN MARC L; NARGUND RAVI P; WYVRATT MATTHEW J; LIN LINUS S,期刊：ACS Medicinal Chemistry Letters, 页码：43-47 , 文章类型： Article，,卷期：2011年2-1] We report the development and characterization of compound 22 (MK-5046), a potent, selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological testing using diet-induced obese mice, compou... N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase [作者：TANG JING; MADDALI KASTHURAIAH; DREIS CHRISTINE D; SHAM YUK Y; VINCE ROBERT; POMMIER YVES; WANG ZHENGQIANG,期刊：ACS Medicinal Chemistry Letters, 页码：63-67 , 文章类型： Article，,卷期：2011年2-1] A new molecular scaffold featuring an N-hydroxyimide functionality and capable of inhibiting both reverse transcriptase (RT) and integrase (IN) of human immunodeficiency virus (HIV) was rationally designed based on 1-[(2... Desmethyl Macrolides: Synthesis and Evaluation of 4,8,10-Tridesmethyl Telithromycin [作者：VELVADAPU VENKATA; PAUL TAPAS; WAGH BHARAT; KLEPACKI DOROTA; GUVENCH OLGUN; MACKERELL ALEXANDER JR; ANDRADE RODRIGO B,期刊：ACS Medicinal Chemistry Letters, 页码：68-72 , 文章类型： Article，,卷期：2011年2-1] There is an urgent need to discover new drugs to address the pressing problem of antibiotic resistance. Macrolide antibiotics such as erythromycin (1) are safe, broad spectrum antibiotics used in the clinic since 1954. H... A kappa Opioid Pharmacophore Becomes a Spinally Selective kappa-delta Agonist When Modified with a Basic Extender Arm [作者：TANG YE; YANG JIE; LUNZER MARY M; POWERS MICHAEL D; PORTOGHESE PHILIP S,期刊：ACS Medicinal Chemistry Letters, 页码：7-10 , 文章类型： Article，,卷期：2011年2-1] We have explored the concept of a molecular extender arm attached to a kappa opioid agonist pharmacophore 3 (ICI-199,441) in an effort to potentially interact, with a complementary group on a neighboring opioid receptor.... Stereochemical Survey of Digitoxin Monosaccharides [作者：WANG HUAYU LEO; XIN WENJUN; ZHOU MAOQUAN; STUECKLE TODD A; ROJANASAKUL YON; ODOHERTY GEORGE A,期刊：ACS Medicinal Chemistry Letters, 页码：73-78 , 文章类型： Article，,卷期：2011年2-1] A stereochemically diverse array of monosaccharide analogues of the trisaccharide-based cardiac glycoside natural product digitoxin has been synthesized using a de novo asymmetric approach. The analogues were tested for ... Development of Selective LH Receptor Agonists by Heterodimerization with a FSH Receptor Antagonist [作者：BONGER KIMBERLY M; HOOGENDOORN SASCHA; VAN KOPPEN CHRIS J; TIMMERS C MARCO; VAN DER MAREL GIJSBERT A; OVERKLEEFT HERMAN S,期刊：ACS Medicinal Chemistry Letters, 页码：85-89 , 文章类型： Article，,卷期：2011年2-1] The structural resemblance of the luteinizing hormone receptor (LHR) and follicle stimulating hormone receptor (FSHR) impedes selective agonistic targeting of one of those by low molecular weight (LMW) ligands. In the pr...