个性化文献订阅>文章检索

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25条记录   Discovery of N-[2-Hydroxy-6-(4-methoxybenzamido)phenyl]-4-(4-methyl-1,4-diazepan-1-yl )benzamide (Darexaban, YM150) as a Potent and Orally Available Factor Xa Inhibitor [作者：HIRAYAMA FUKUSHI; KOSHIO HIROYUKI; ISHIHARA TSUKASA; HACHIYA SHUNICHIRO; SUGASAWA KEIZO; KOGA YUJI; SEKI NORIO; SHIRAKI RYOUTA; SHIGENAGA TAKESHI; IWATSUKI YOSHIYUKI; MORITANI YUMIKO; MORI KENICHI; KADOKURA TAKESHI; KAWASAKI TOMIHISA; MATSUMOTO YUZO; SAKAMOTO SHUICHI; TSUKAMOTO SHINICHI,期刊：Journal of Medicinal Chemistry, 页码：8051-8065 , 文章类型： Article，,卷期：2011年54-23] Inhibitors of factor Xa (FXa), a crucial serine protease in the coagulation cascade, have attracted a great deal of attention as a target for developing antithrombotic agents. We previously reported findings from our opt... Newly Synthesized Curcumin Derivatives: Crosstalk between Chemico-physical Properties and Biological Activity [作者：FERRARI ERIKA; PIGNEDOLI FRANCESCA; IMBRIANO CAROL; MARVERTI GAETANO; BASILE VALENTINA; VENTURI ETTORE; SALADINI MONICA,期刊：Journal of Medicinal Chemistry, 页码：8066-8077 , 文章类型： Article，,卷期：2011年54-23] New curcumin analogues (ester and acid series) were synthesized with the aim to improve the chemical stability in physiological conditions and potential anticancer activity. Cytotoxicity against different tumorigenic cel... Development of Melanoma-Targeted Polymer Micelles by Conjugation of a Melanocortin 1 Receptor (MC1R) Specific Ligand [作者：BARKEY NATALIE M; TAFRESHI NARGES K; JOSAN JATINDER S; DE SILVA CHANNA R; SILL KEVIN N; HRUBY VICTOR J; GILLIES ROBERT J; MORSE DAVID L; VAGNER JOSEF,期刊：Journal of Medicinal Chemistry, 页码：8078-8084 , 文章类型： Article，,卷期：2011年54-23] The incidence of malignant melanoma is rising faster than that of any other cancer in the United States. Because of its high expression on the surface of melanomas, MC1R has been investigated as a target for selective im... Multidentate (18)F-Polypegylated Styrylpyridines As Imaging Agents for A beta Plaques in Cerebral Amyloid Angiopathy (CAA) [作者：ZHA ZHIHAO; CHOI SEOK RYE; PLOESSL KARL; LIEBERMAN BRIAN P; QU WENCHAO; HEFTI FRANZ; MINTUN MARK; SKOVRONSKY DANIEL; KUNG HANK F,期刊：Journal of Medicinal Chemistry, 页码：8085-8098 , 文章类型： Article，,卷期：2011年54-23] beta-Amyloid plaques (A beta plaques) in the brain are associated with cerebral amyloid angiopathy (CAA). Imaging agents that could target the A beta plaques in the living human brain would be potentially valuable as bio... Antibacterial Optimization of 4-Aminothiazolyl Analogues of the Natural Product GE2270 A: Identification of the Cycloalkylcarboxylic Acids [作者：LAMARCHE MATTHEW J; LEEDS JENNIFER A; AMARAL KERRI; BREWER JASON T; BUSHELL SIMON M; DEWHURST JANETTA M; DZINKFOX JOANNE; GANGL ERIC; GOLDOVITZ JULIE; JAIN AKASH; MULLIN STEVE; NECKERMANN GEORG; OSBORNE COLIN; PALESTRANT DEBORAH; PATANE MICHAEL A; RANN ELIN M; SACHDEVA MEENA; SHAO JIAN; TIAMFBOK STACEY; WHITEHEAD LEWIS; YU DONGHUI,期刊：Journal of Medicinal Chemistry, 页码：8099-8109 , 文章类型： Article，,卷期：2011年54-23] 4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for their activity against Gram positive bacterial infections. Optimization efforts focused on improving... Evaluation and Discovery of Novel Synthetic Chalcone Derivatives as Anti-Inflammatory Agents [作者：WU JIANZHANG; LI JIANLING; CAI YUEPIAO; PAN YONG; YE FAQING; ZHANG YALI; ZHAO YUNJIE; YANG SHULIN; LI XIAOKUN; LIANG GUANG,期刊：Journal of Medicinal Chemistry, 页码：8110-8123 , 文章类型： Article，,卷期：2011年54-23] Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study rev... p-(4-Azipentyl)propofol: A Potent Photoreactive General Anesthetic Derivative of Propofol [作者：STEWART DEIRDRE S; SAVECHENKOV PAVEL Y; DOSTALOVA ZUZANA; CHIARA DAVID C; GE RILE; RAINES DOUGLAS E; COHEN JONATHAN B; FORMAN STUART A; BRUZIK KAROL S; MILLER KEITH W,期刊：Journal of Medicinal Chemistry, 页码：8124-8135 , 文章类型： Article，,卷期：2011年54-23] We synthesized 2,6-diisopropyl-4-[3-(3-methyl-3H-diazirin-3-yl)propyl]phenol (p-(4-azipentyl)propofol), or p-4-AziC5-Pro, a novel photoactivable derivative of the general anesthetic propofol. p-4-AziC5-Pro has an anesthe... Molecular Determinants of Ligand Binding Modes in the Histamine H(4) Receptor: Linking Ligand-Based Three-Dimensional Quantitative Structure-Activity Relationship (3D-QSAR) Models to in Silico Guided Receptor Mutagenesis Studies [作者：ISTYASTONO ENADE P; NIJMEIJER SASKIA; LIM HERMAN D; VAN DE STOLPE ANDREA; ROUMEN LUC; KOOISTRA ALBERT J; VISCHER HENRY F; DE ESCH IWAN J P; LEURS ROB; DE GRAAF CHRIS,期刊：Journal of Medicinal Chemistry, 页码：8136-8147 , 文章类型： Article，,卷期：2011年54-23] The histamine H(4) receptor (H(4)R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H(3) receptor (H(3)R), two acidic residues in the HA binding po... Structure-Activity Relationships in Toll-Like Receptor 2-Agonists Leading to Simplified Monoacyl Lipopeptides [作者：AGNIHOTRI GEETANJALI; CRALL BREANNA M; LEWIS TYLER C; DAY TIMOTHY P; BALAKRISHNA RAJALAKSHMI; WARSHAKOON HEMAMALI J; MALLADI SUBBALAKSHMI S; DAVID SUNIL A,期刊：Journal of Medicinal Chemistry, 页码：8148-8160 , 文章类型： Article，,卷期：2011年54-23] Toll-like receptor 2-agonistic lipopeptides typified by S-[2,3-bis(palmitoyloxy)-(2RS)-propyl]-R-cystein-yl-S-serine (PAM(2)CS) compounds are potential vaccine adjuvants. In continuation of previously reported structure ... Synthesis and Structure-Activity Relationship (SAR) of (5,7-Disubstituted 3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidin-2-yl)-methylamines as Potent Serotonin 5-HT(6) Receptor (5-HT(6)R) Antagonists [作者：IVACHTCHENKO ALEXANDRE V; GOLOVINA ELENA S; KADIEVA MADINA G; KYSIL VOLODYMYR M; MITKIN OLEG D; TKACHENKO SERGEY E; OKUN ILYA M,期刊：Journal of Medicinal Chemistry, 页码：8161-8173 , 文章类型： Article，,卷期：2011年54-23] Syntheses, biological evaluation as 5-HT(6) receptor (5-HT(6)R) antagonists, and structure activity relationships for a series of novel 5,7-disubstituted (3-arylsulfonyl-pyrazolo[1,5-a]pyrimidins are disclosed. The molec... Fragment-Based Discovery of Indole Inhibitors of Matrix Metalloproteinase-13 [作者：TAYLOR STEVEN J; ABEYWARDANE ASITHA; LIANG SHUANG; MUEGGE INGO; PADYANA ANIL K; XIONG ZHAOMING; HILLDRZEWI MELISSA; FARMER BENNETT; LI XIANG; COLLINS BRANDON; LI JOHN XIANG; HEIMRIETHER ALEXANDER; PROUDFOOT JOHN; ZHANG QIANG; GOLDBERG DANIEL; ZUVELAJELASKA LJILJANA; ZAHER HANI; LI JUN; FARROW NEIL A,期刊：Journal of Medicinal Chemistry, 页码：8174-8187 , 文章类型： Article，,卷期：2011年54-23] Matrix metalloproteases (MMPs) play an important role in cartilage homeostasis under both normal and inflamed disease states and, thus, have become attractive targets for the treatment of arthritic diseases. Herein, we d... Pharmacological Validation of Trypanosoma brucei Phosphodiesterases B1 and B2 as Druggable Targets for African Sleeping Sickness [作者：BLAND NICHOLAS D; WANG CUIHUA; TALLMAN CRAIG; GUSTAFSON ALDEN E; WANG ZHOUXI; ASHTON TRENT D; OCHIANA STEFAN O; MCALLISTER GREGORY; COTTER KRISTINA; FANG ANNA P; GECHIJIAN LARA; GARCEAU NORMAN; GANGURDE RAJIV; ORTENBERG RON; ONDRECHEN MARY JO; CAMPBELL ROBERT K; POLLASTRI MICHAEL P,期刊：Journal of Medicinal Chemistry, 页码：8188-8194 , 文章类型： Article，,卷期：2011年54-23] Neglected tropical disease drug discovery requires application of pragmatic and efficient methods for development of new therapeutic agents. In this report, we describe our target repurposing efforts for the essential ph... Crystal Structure-Based Virtual Screening for Fragment-like Ligands of the Human Histamine H(1) Receptor [作者：DE GRAAF CHRIS; KOOISTRA ALBERT J; VISCHER HENRY F; KATRITCH VSEVOLOD; KUIJER MARTIEN; SHIROISHI MITSUNORI; IWATA SO; SHIMAMURA TATSURO; STEVENS RAYMOND C; DE ESCH IWAN J P; LEURS ROB,期刊：Journal of Medicinal Chemistry, 页码：8195-8206 , 文章类型： Article，,卷期：2011年54-23] The recent crystal structure determinations of druggable class A G protein-coupled receptors (GPCRs) have opened up excellent opportunities in structure-based ligand discovery for this pharmaceutically important protein ... Investigating the Antimalarial Action of 1,2,4-Trioxolanes with Fluorescent Chemical Probes [作者：HARTWIG CARMONY L; LAUTERWASSER ERICA M W; MAHAJAN SUMIT S; HOKE JONATHAN M; COOPER ROLAND A; RENSLO ADAM R,期刊：Journal of Medicinal Chemistry, 页码：8207-8213 , 文章类型： Article，,卷期：2011年54-23] The 1,2,4-trioxolanes are a new class of synthetic peroxidic antimalarials currently in human clinical trials. The well-known reactivity of the 1,2,4-trioxolane ring toward inorganic ferrous iron and ferrous iron heme is... Novel 3-Nitro-1H-1,2,4-triazole-Based Aliphatic and Aromatic Amines as Anti-Chagasic Agents [作者：PAPADOPOULOU MARIA V; TRUNZ BERNADETTE BOURDIN; BLOOMER WILLIAM D; MCKENZIE CAROLINE; WILKINSON SHANE R; PRASITTICHAI CHAIYA; BRUN RETO; KAISER MARCEL; TORREELE ELS,期刊：Journal of Medicinal Chemistry, 页码：8214-8223 , 文章类型： Article，,卷期：2011年54-23] A series of novel 2-nitro-1H-imidazole- and 3-nitro-1H-1,2,4-triazole-based aromatic and aliphatic amines were screened for antitrypanosomal activity and mammalian cytotoxicity by the Drugs for Neglected Diseases initiat... Hypoxia Activated Prodrugs of a 9-Aza-anthrapyrazole Derivative That Has Promising Anticancer Activity [作者：ELDAKDOUKI MOHAMMAD H; ADAMSKI NICHOLAS; FOSTER LECIA; HACKER MILES P; ERHARDT PAUL W,期刊：Journal of Medicinal Chemistry, 页码：8224-8227 , 文章类型： Article，,卷期：2011年54-23] Mono- and his-N-oxides of a 9-aza-anthrapyrazole derivative having two 2-(dimethylamino)ethyl appendages were prepared by using a mild oxaziridine reagent. Biochemical and cell culture assays indicate that the bis-oxide ...