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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15条记录   Discovery of Substituted Biphenyl Oxazolidinone Inhibitors of Cholesteryl Ester Transfer Protein [作者：THOMPSON CHRISTOPHER F; ALI AMJAD; QURAISHI NAZIA; LU ZHIJIAN; HAMMOND MILTON L; SINCLAIR PETER J; ANDERSON MATT S; EVELAND SUZANNE S; GUO QIU; HYLAND SHERYL A; MILOT DENISE P; SPARROW CARL P; WRIGHT SAMUEL D,期刊：ACS Medicinal Chemistry Letters, 页码：424-427 , 文章类型： Article，,卷期：2011年2-6] Recently, there has been a strong interest in the ability to increase levels of high density lipoprotein-cholesterol (HDL-C). This interest stems from the hypothesis that such an elevation in HDL-C will decrease the like... Bisdionin C-A Rationally Designed, Submicromolar Inhibitor of Family 18 Chitinases [作者：SCHUETTELKOPF ALEXANDER W; ANDERSEN OLE A; RAO FRANCESCO V; ALLWOOD MATTHEW; RUSH CHRISTINA L; EGGLESTON IAN M; VAN AALTEN DAAN M F,期刊：ACS Medicinal Chemistry Letters, 页码：428-432 , 文章类型： Article，,卷期：2011年2-6] Chitinases of the GH18 family play important roles in a variety of pathogenic organisms and have also been shown to be involved in human asthma progression, making these enzymes potential drug targets. While a number of ... Thermodynamics of Ligand Binding and Efficiency [作者：REYNOLDS CHARLES H; HOLLOWAY M KATHARINE,期刊：ACS Medicinal Chemistry Letters, 页码：433-437 , 文章类型： Article，,卷期：2011年2-6] Analysis of the experimental binding thermodynamics for approximately 100 protein-ligand complexes provides important insights into the factors governing ligand affinity and efficiency. The commonly accepted correlation ... Novel Synthesis and Biological Evaluation of Enigmols as Therapeutic Agents for Treating Prostate Cancer [作者：GARNIERAMBLARD ETHEL C; MAYS SUZANNE G; ARRENDALE RICHARD F; BAILLIE MARK T; BUSHNEV ANATOLIY S; CULVER DEBORAH G; EVERS TAYLOR J; HOLT JASON J; HOWARD RANDY B; LIEBESKIND LANNY S; MENALDINO DAVID S; NATCHUS MICHAEL G; PETROS JOHN A; RAMARAJU HARSHA; REDDY G PRABHAKAR; LIOTTA DENNIS C,期刊：ACS Medicinal Chemistry Letters, 页码：438-443 , 文章类型： Article，,卷期：2011年2-6] Enigmol is a synthetic, orally active 1-deoxysphingoid base analogue that has demonstrated promising activity against prostate cancer. In these studies, the pharmacologic roles of stereochemistry and N-methylation in the... Discovery of a Selective S1P(1) Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate [作者：DEMONT EMMANUEL H; ANDREWS BENJAMIN I; BIT RINO A; CAMPBELL COLIN A; COOKE JASON W B; DEEKS NIGEL; DESAI SAPNA; DOWELL SIMON J; GASKIN PAM; GRAY JAMES R J; HAYNES ANDREA; HOLMES DUNCAN S; KUMAR UMESH; MORSE MARY A; OSBORNE GREG J; PANCHAL TERRY; PATEL BELA; PERBONI ALCIDE; TAYLOR SIMON; WATSON ROBERT; WITHERINGTON JASON; WILLIS ROBERT,期刊：ACS Medicinal Chemistry Letters, 页码：444-449 , 文章类型： Article，,卷期：2011年2-6] Gilenya (fingolimod, FTY720) was recently approved by the U.S. FDA for the treatment of patients with remitting relapsing multiple sclerosis (RRMS). It is a potent agonist of four of the five sphingosine 1-phosphate (SIP... Discovery of INCB3284, a Potent, Selective, and Orally Bioavailablle hCCR2 Antagonist [作者：XUE CHUBIAO; FENG HAO; CAO GANFENG; HUANG TAISHENG; GLENN JOSEPH; ANAND RAJAN; MELONI DAVID; ZHANG KE; KONG LINGQUAN; WANG ANLAI; ZHANG YINGXIN; ZHENG CHANGSHENG; XIA MICHAEL; CHEN LIHUA; TANAKA HIROYUKI; HAN QI; ROBINSON D J; MODI DILIP; STORACE LOU; SHAO LIXIN; SHARIEF VAQAR; LI MEI; GALYA LAURINE G; COVINGTON MARYANNE; SCHERLE PEGGY; DIAMOND SHARON; EMM TOM; YELESWARAM SWAMY; CONTEL NANCY; VADDI KRIS; NEWTON ROBERT; HOLLIS GREG; FRIEDMAN STEVEN; METCALF BRIAN,期刊：ACS Medicinal Chemistry Letters, 页码：450-454 , 文章类型： Article，,卷期：2011年2-6] We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in ant... The Impact of Ionization States of Matrix Metalloproteinase Inhibitors on Docking-Based Inhibitor Design [作者：ZHONG HAIZHEN; WEES MELISSA A; FAURE THERESA D; CARRILLO CAROL; ARBISER JACK; BOWEN J PHILLIP,期刊：ACS Medicinal Chemistry Letters, 页码：455-460 , 文章类型： Article，,卷期：2011年2-6] The influence of ionization states of hydroxamates and retrohydroxamates and the presence of zinc ions in the active site were investigated using the wild-type and E402Q mutant of MMP-9. The deprotonated hydroxamates sho... Disubstituted Bis-THF Moieties as New P2 Ligands in Non peptidal HIV-1 Protease Inhibitors [作者：HOHLFELD KONRAD; TOMASSI CYRILLE; WEGNER JORG KURT; KESTELEYN BART; LINCLAU BRUNO,期刊：ACS Medicinal Chemistry Letters, 页码：461-465 , 文章类型： Article，,卷期：2011年2-6] A series of darunavir analogues featuring a substituted bis-THF ring as P2 ligand have been synthesized and evaluated. High affinity protease inhibitors (PIs) with an interesting activity on wild-type HIV and a panel of ... Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity [作者：MORASKI GARRETT C; MARKLEY LOWELL D; HIPSKIND PHILIP A; BOSHOFF HELENA; CHO SANGHYUN; FRANZBLAU SCOTT G; MILLER MARVIN J,期刊：ACS Medicinal Chemistry Letters, 页码：466-470 , 文章类型： Article，,卷期：2011年2-6] A set of nine 2,7-dimethylimidazo[1,2-a]pyridine-3-carboxamides and one 2,6-dimethylimidazo[1,2-a]pyrimidine-3-carboxamide were synthesized. The compounds were evaluated for their in vitro antituberculosis activity versu... Discovery of a Potent Pyrazolopyridine Series of gamma-Secretase Modulators [作者：QIN JUN; ZHOU WEI; HUANG XIANHAI; DHONDI PAWAN; PALANI ANANDAN; ASLANIAN ROBERT; ZHU ZHAONING; GREENLEE WILLIAM; COHENWILLIAMS MARY; JONES NICHOLAS; HYDE LYNN; ZHANG LILI,期刊：ACS Medicinal Chemistry Letters, 页码：471-476 , 文章类型： Article，,卷期：2011年2-6] The synthesis and structure activity relationship of a novel series of pyrazolopyridines are reported. These compounds represent a new class of gamma-secretase modulators that demonstrate good in vitro potency in inhibit... Potent CXCR4 Antagonists Containing Amidine Type Peptide Bond Isosteres [作者：INOKUCHI ERIKO; OISHI SHINYA; KUBO TATSUHIKO; OHNO HIROAKI; SHIMURA KAZUYA; MATSUOKA MASAO; FUJII NOBUTAKA,期刊：ACS Medicinal Chemistry Letters, 页码：477-480 , 文章类型： Article，,卷期：2011年2-6] A series of FC131 [cyclo(-D-Tyr-Arg-Arg-Nal-Gly-)] analogues containing amidine type peptide bond isosteres were synthesized as selective CXC chemokine receptor type 4 (CXCR4) antagonists. An isosteric amidine substructu... N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy [作者：AMATO GEORGE; ROELOFFS ROSEMARIE; RIGDON GREG C; ANTONIO BRETT; MERSCH THERESA; MCNAUGHTONSMITH GRANT; WICKENDEN ALAN D; FRITCH PAUL; SUTO MARK J,期刊：ACS Medicinal Chemistry Letters, 页码：481-484 , 文章类型： Article，,卷期：2011年2-6] A series of N-pyridyl benzamide KCNQ2/Q3 potassium channel openers were identified and found to be active in animal models of epilepsy and pain. The best compound 12 [ICA-027243, N-(6-chloro-pyridin-3-yl)-3,4-difluoro-be... Ranking High Affinity Ligands of Low Solubility by NMR Spectroscopy [作者：LANDRIEU ISABELLE; HANOULLE XAVIER; FRITZINGER BERND; HORVATH DRAGOS; WIERUSZESKI JEANMICHEL; LIPPENS GUY,期刊：ACS Medicinal Chemistry Letters, 页码：485-487 , 文章类型： Article，,卷期：2011年2-6] Cyclosporine A (CsA) and its chemical analogues EthVal4Cs, MeVal4Cs, and Me(D-Ala)3EthVal4Cs (Alisporivir) all interact with cyclophilin A (CypA). The latter Alisporivir is a nonimmunosuppressive CsA derivative that has ... The Implication of the First Agonist Bound Activated GPCR X-ray Structure on GPCR in Silico Modeling [作者：TAUTERMANN CHRISTOFER S; PAUTSCH ALEXANDER,期刊：ACS Medicinal Chemistry Letters, 页码：414-418 , 文章类型： Article，,卷期：2011年2-6] The very recently published first X-ray structure of the beta 2 adrenergic receptor in its active state hosting a small molecule (PDB ID: 3P0G) reveals a lot of information about the G-protein-coupled receptor (GPCR) act... Peptide-Chlorambucil Conjugates Combat Pgp-Dependent Drug Efflux [作者：FONSECA SONALI B; KELLEY SHANA O,期刊：ACS Medicinal Chemistry Letters, 页码：419-423 , 文章类型： Article，,卷期：2011年2-6] Cancer drugs, such as the ovarian cancer drug adriamycin, are effective at slowing disease progression and improving remission rates in patients. However, drug resistance often arises, limiting the activity of these agen...