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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20条记录   Drug Discovery 2012 and Beyond [作者：ROTELLA DAVID P,期刊：ACS Medicinal Chemistry Letters, 页码：172-173 , 文章类型： Editorial Material，,卷期：2012年3-3] The America Invents Act-Overview and Implications [作者：HOLLINGER SUSANNE,期刊：ACS Medicinal Chemistry Letters, 页码：174-176 , 文章类型： Editorial Material，,卷期：2012年3-3] A-Ring Dihalogenation Increases the Cellular Activity of Combretastatin-Templated Tetrazoles [作者：BEALE THOMAS M; ALLWOOD DANIEL M; BENDER ANDREAS; BOND PETER J; BRENTON JAMES D; CHARNOCKJONES D STEPHEN; LEY STEVEN V; MYERS REBECCA M; SHEARMAN JAMES W; TEMPLE JILL; UNGER JESSICA; WATTS CIORSDAIDH A; XIAN JIAN,期刊：ACS Medicinal Chemistry Letters, 页码：177-181 , 文章类型： Article，,卷期：2012年3-3] The combretastatins have been investigated for their antimitotic and antivascular properties, and it is widely postulated that a 3,4,5-trimethoxyaryl A-ring is essential to maintain potent activity. We have synthesized n... The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease? [作者：RAMPA ANGELA; BARTOLINI MANUELA; BISI ALESSANDRA; BELLUTI FEDERICA; GOBBI SILVIA; ANDRISANO VINCENZA; LIGRESTI ALESSIA; DI MARZO VINCENZO,期刊：ACS Medicinal Chemistry Letters, 页码：182-186 , 文章类型： Article，,卷期：2012年3-3] The treatment of Alzheimer's disease (AD) still remains an area of significant unmet need, with drugs that only target the symptoms of the disease. Therefore, there is considerable need for disease-modifying therapies. T... Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia [作者：DOUNAY ARNY B; ANDERSON MARIE; BECHLE BRUCE M; CAMPBELL BRIAN M; CLAFFEY MICHELLE M; EVDOKIMOV ARTEM; EVRARD EDELWEISS; FONSECA KARI R; GAN XINMIN; GHOSH SOMRAJ; HAYWARD MATTHEW M; HORNER WELDON; KIM JIYOUNG; MCALLISTER LAURA A; PANDIT JAYVARDHAN; PARADIS VANESSA; PARIKH VINOD D; REESE MATTHEW R; RONG SUOBAO; SALAFIA MICHELLE A; SCHUYTEN KATHERINE; STRICK CHRISTINE A; TUTTLE JAMISON B; VALENTINE JAMES; WANG HONG; ZAWADZKE LAURA E; VERHOEST PATRICK R,期刊：ACS Medicinal Chemistry Letters, 页码：187-192 , 文章类型： Article，,卷期：2012年3-3] Kynurenine aminotransferase (KAT) 11 has been identified as a potential new target for the treatment of cognitive impairment associated with schizophrenia and other psychiatric disorders. Following a high-throughput scre... BACE1 Inhibitor Peptides: Can an Infinitely Small k(cat) Value Turn the Substrate of an Enzyme into Its Inhibitor? [作者：HAMADA YOSHIO; ISHIURA SHOICHI; KISO YOSHIAKI,期刊：ACS Medicinal Chemistry Letters, 页码：193-197 , 文章类型： Article，,卷期：2012年3-3] Recently, we reported substrate-based pentapeptidic beta-secretase (BACE1) inhibitors with a hydroxymethylcarbonyl isostere as a substrate transition-state mimic. These inhibitors showed potent BACE1 inhibitory activity ... Discovery of a Potent Thiadiazole Class of Histamine H-3 Receptor Antagonist for the Treatment of Diabetes [作者：RAO ASHWIN U; SHAO NING; ASLANIAN ROBERT G; CHAN TINYAU; DEGRADO SYLVIA J; WANG LI; MCKITTRICK BRIAN; SENIOR MARY; WEST ROBERT E JR; WILLIAMS SHIRLEY M; WU RENLONG; HWA JOYCE; PATEL BHUNESHWARI; ZHENG SHUQIN; SONDEY CHRISTOPHER; PALANI ANANDAN,期刊：ACS Medicinal Chemistry Letters, 页码：198-202 , 文章类型： Article，,卷期：2012年3-3] A series of novel 2-piperidinopiperidine thiadiazoles were synthesized and evaluated as new leads of histamine H-3 receptor antagonists. The 4-(5-([1,4'-bipiperidin]-1'-yl)-1,3,4-thiadiazol-2-yl)-2-(pyridin-2-yl)morpholi... Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye [作者：ZHONG MIN; GADEK THOMAS R; BUI MINNA; SHEN WANG; BURNIER JOHN; BARR KENNETH J; HANAN EMILY J; OSLOB JOHAN D; YU CHUL H; ZHU JIANG; ARKIN MICHELLE R; EVANCHIK MARC J; FLANAGAN W MIKE; HOCH UTE; HYDE JENNIFER; PRABHU SAILETA; SILVERMAN JEFFREY A; WRIGHT JASMIN,期刊：ACS Medicinal Chemistry Letters, 页码：203-206 , 文章类型： Article，,卷期：2012年3-3] LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunolog... Hydrophobic Interactions Improve Selectivity to ER alpha for Benzothiophene SERMs [作者：CHALMERS MICHAEL J; WANG YONG; NOVICK SCOTT; SATO MASAHIKO; BRYANT HENRY U; MONTROSERAFIZDEH CHAHRZAD; GRIFFIN PATRICK R; DODGE JEFFREY A,期刊：ACS Medicinal Chemistry Letters, 页码：207-210 , 文章类型： Article，,卷期：2012年3-3] The discovery, pharmacology, and biophysical characterization of an estrogen receptor alpha (ER alpha) selective benzothiophene (BTP alpha) is described. BTP alpha (4) is a high-affinity ligand with 140-fold greater sele... Desmethyl Macrolides: Synthesis and Evaluation of 4,10-Didesmethyl Telithromycin [作者：VELVADAPU VENKATA; GLASSFORD IAN; LEE MISEON; PAUL TAPAS; DEBROSSE CHARLES; KLEPACKI DOROTA; SMALL MEAGAN C; MACKERELL ALEXANDER D JR; ANDRADE RODRIGO B,期刊：ACS Medicinal Chemistry Letters, 页码：211-215 , 文章类型： Article，,卷期：2012年3-3] Novel sources of antibiotics are required to keep pace with the inevitable onset of bacterial resistance. Continuing with our macrolide desmethylation strategy as a source of new antibiotics, we report the total synthesi... Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication [作者：SKERLJ RENATO; BRIDGER GARY; ZHOU YUANXI; BOURQUE ELYSE; MCEACHERN ERNEST; DANTHI SANJAY; LANGILLE JONATHAN; HARWIG CURTIS; VEALE DUANE; CARPENTER BRYON; BA TUYA; BEY MICHAEL; BAIRD IAN; WILSON TREVOR; METZ MARKUS; MACFARLAND RON; MOSI RENEE; BODART VERONIQUE; WONG REBECCA; FRICKER SIMON; HUSKENS DANA; SCHOLS DOMINIQUE,期刊：ACS Medicinal Chemistry Letters, 页码：216-221 , 文章类型： Article，,卷期：2012年3-3] A series of CCR5 antagonists representing the thiophene-3-yl-methyl ureas were designed that met the pharmacological criteria for HIV-1 inhibition and mitigated a human ether-a-go-go related gene (hERG) inhibition liabil... Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists [作者：HU SHUANGHUA; HUANG YAZHONG; DESHPANDE MILIND; LUO GUANGLIN; BRUCE MARC A; CHEN LING; MATTSON GAIL; IBEN LAWRENCE G; ZHANG JIE; RUSSELL JOHN W; CLARKE WENDY J; HOGAN JOHN B; ORTIZ ASTRID; FLINT OLIVER; HENWOOD ANDREW; GAO QI; ANTALZIMANYI ILDIKO; POINDEXTER GRAHAM S,期刊：ACS Medicinal Chemistry Letters, 页码：222-226 , 文章类型： Article，,卷期：2012年3-3] A novel class of bicyclo[3.1.0]hexanylpiperazine neuropeptide Y (NPY) Y1 antagonists has been designed and synthesized. Scatchard binding analysis showed these compounds to be noncompetitive with [I-125]PYY binding to th... NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with mu-Opioid Agonist Activity [作者：RENTON PAUL; GREEN BRENDA; MADDAFORD SHAWN; RAKHIT SUMAN; ANDREWS JOHN S,期刊：ACS Medicinal Chemistry Letters, 页码：227-231 , 文章类型： Article，,卷期：2012年3-3] A novel series of benzimidazole designed multiple ligands (DMLs) with activity at the neuronal nitric oxide synthase (nNOS) enzyme and the mu-opioid receptor was developed. Targeting of the structurally dissimilar heme-c... Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor [作者：DOCKENDORFF CHRIS; AISIKU OMOZUANVBO; VERPLANK LYNN; DILKS JAMES R; SMITH DANIEL A; GUNNINK SUSANNA F; DOWAL LOUISA; NEGRI JOSEPH; PALMER MICHELLE; MACPHERSON LAWRENCE; SCHREIBER STUART L; FLAUMENHAFT ROBERT,期刊：ACS Medicinal Chemistry Letters, 页码：232-237 , 文章类型： Article，,卷期：2012年3-3] A high-throughput screen of the NIH-MLSMR compound collection, along with a series of secondary assays to identify potential targets of hit compounds, previously identified a 1,3-diaminobenzene scaffold that targets prot... Inhibitors for Bacterial Cell-Wall Recycling [作者：YAMAGUCHI TAKAO; BLAZQUEZ BLAS; HESEK DUSAN; LEE MIJOON; LLARRULL LETICIA I; BOGGESS BILL; OLIVER ALLEN G; FISHER JED F; MOBASHERY SHAHRIAR,期刊：ACS Medicinal Chemistry Letters, 页码：238-242 , 文章类型： Article，,卷期：2012年3-3] Gram-negative bacteria have evolved an elaborate process for the recycling of their cell wall, which is initiated in the periplasmic space by the action of lytic transglycosylases. The product of this reaction, beta-D-N-... Molecular Docking and in Vitro Antileishmanial Evaluation of Chromene-2-thione Analogues [作者：VERMA RAJIV KUMAR; PRAJAPATI VIJAY KUMAR; VERMA GIRIJESH KUMAR; CHAKRABORTY DEBLINA; SUNDAR SHYAM; RAI MADHUKAR; DUBEY VIKASH KUMAR; SINGH MAYA SHANKAR,期刊：ACS Medicinal Chemistry Letters, 页码：243-247 , 文章类型： Article，,卷期：2012年3-3] Leishmaniases are an epidemic in various countries, and the parasite is developing resistance against available drugs. Thus, development of new drugs against Leishmania is an open area of investigation for synthetic orga...