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15条记录   Discovery of a Potent HIV Integrase Inhibitor That Leads to a Prodrug with Significant anti-HIV Activity [作者：SEO BYUNG I; UCHIL VINOD R; OKELLO MAURICE; MISHRA SANJAY; MA XIAOHUI; NISHONOV MALIK; SHU QINGNING; CHI GUOCHEN; NAIR VASU,期刊：ACS Medicinal Chemistry Letters, 页码：877-881 , 文章类型： Article，,卷期：2011年2-12] Worldwide research efforts in drug discovery involving HIV integrase have produced only one compound, raltegravir, that has been approved for clinical use in HIV/AIDS. As resistance, toxicity, and drug-drug interactions ... Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam [作者：GICHINGA MOSES G; OLSON JEREMY P; BUTALA ELIZABETH; NAVARRO HERNAN A; GILMOUR BRIAN P; MASCARELLA S WAYNE; CARROLL F IVY,期刊：ACS Medicinal Chemistry Letters, 页码：882-884 , 文章类型： Article，,卷期：2011年2-12] In an effort to discover potent and selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonists, 15 tetrahydropyrimidinone analogues of 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)-urea... Copper-Free Click for PET: Rapid 1,3-Dipolar Cycloadditions with a Fluorine-18 Cyclooctyne [作者：CARPENTER RICHARD D; HAUSNER SVEN H; SUTCLIFFE JULIE L,期刊：ACS Medicinal Chemistry Letters, 页码：885-889 , 文章类型： Article，,卷期：2011年2-12] The strain-promoted click 1,3-dipolar cycloaddition reactions involving azides and cyclooctynes for the synthesis of triazoles offer the advantage of being able to be performed in biological settings via copper-free chem... Development of Polar Adenosine A(2A) Receptor Agonists for Inflammatory Bowel Disease: Synergism with A(2B) Antagonists [作者：ELTAYEB ALI; MICHAEL SEBASTIAN; ABDELRAHMAN ALIAA; BEHRENSWERTH ANDREA; GOLLOS SABRINA; NIEBER KAREN; MUELLER CHRISTA E,期刊：ACS Medicinal Chemistry Letters, 页码：890-895 , 文章类型： Article，,卷期：2011年2-12] Adenosine A(2A) receptor agonists for the local treatment of inflammatory bowel disease (IBS) were designed and synthesized. Polar groups were introduced to prevent peroral absorption and subsequent systemic, e.g., hypot... Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB [作者：NAKAYAMA MARIKO; YAMADA SHOYA; OHSAWA FUMINORI; OHTA YUI; KAWATA KOHEI; MAKISHIMA MAKOTO; KAKUTA HIROKI,期刊：ACS Medicinal Chemistry Letters, 页码：896-900 , 文章类型： Article，,卷期：2011年2-12] We discovered a potent retinoid X receptor (RXR) antagonist, 6-[N-ethyl-N-(5-isobutoxy-4-isopropyl-2-(E)-styrylphenyl)amino]nicotinic acid (13e), that is structurally closely related to the RXR full agonist 6-[N-ethyl-N-... Synthesis of Marine-Derived 3-Alkylpyridinium Alkaloids with Potent Antiprotozoal Activity [作者：RODENKO BORIS; ALSALABI MOHAMMED I; TEKA IBRAHIM A; HO WILLIAM; ELSABBAGH NASSER; ALI JUMA A M; IBRAHIM HASAN M S; WANNER MARTIN J; KOOMEN GERRITJAN; DE KONING HARRY P,期刊：ACS Medicinal Chemistry Letters, 页码：901-906 , 文章类型： Article，,卷期：2011年2-12] Given the pressing need for new antiprotozoal drugs without cross-resistance with current (failing) chemotherapy, we have explored 3-tridecylpyridinium alkaloids (3TPAs), derivatives of viscosamine, as antiparasitic agen... Design, Synthesis, and Biological Evaluation of a Series of Novel AXL Kinase Inhibitors [作者：MOLLARD ALEXIS; WARNER STEVEN L; CALL LEE T; WADE MARK L; BEARSS JARED J; VERMA ANUPAM; SHARMA SUNIL; VANKAYALAPATI HARIPRASAD; BEARSS DAVID J,期刊：ACS Medicinal Chemistry Letters, 页码：907-912 , 文章类型： Article，,卷期：2011年2-12] The receptor tyrosine kinase AXL has emerged in recent years as an potential oncology target due to its overexpression in several types of cancers coupled with its ability to promote tumor growth and metastasis. To ident... Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist [作者：XUE CHUBIAO; WANG ANLAI; HAN QI; ZHANG YINGXIN; CAO GANFENG; FENG HAO; HUANG TAISHENG; ZHENG CHANGSHENG; XIA MICHAEL; ZHANG KE; KONG LINGQUAN; GLENN JOSEPH; ANAND RAJAN; MELONI DAVID; ROBINSON D J; SHAO LIXIN; STORACE LOU; LI MEI; HUGHES ROBERT O; DEVRAJ RAJESH; MORTON PHILIP A; ROGIER D JOSEPH; COVINGTON MARYANNE; SCHERLE PEGGY; DIAMOND SHARON; EMM TOM; YELESWARAM SWAMY; CONTEL NANCY; VADDI KRIS; NEWTON ROBERT; HOLLIS GREG; METCALF BRIAN,期刊：ACS Medicinal Chemistry Letters, 页码：913-918 , 文章类型： Article，,卷期：2011年2-12] We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent C... Potent and Selective Inhibitors of Long Chain L-2-Hydroxy Acid Oxidase Reduced Blood Pressure in DOCA Salt-Treated Rats [作者：BARAWKAR DINESH A; MERU ASHWIN; BANDYOPADHYAY ANISH; BANERJEE ABIR; DESHPANDE ANIL M; ATHARE CHANDRASHEKHAR; KODURU CHANDRASEKHAR; KHOSE GORAKSHA; GUNDU JAYASAGAR; MAHAJAN KOSHU; PATIL PRADEEP; KANDALKAR SACHIN R; NIRANJAN SANJAY; BHOSALE SHUBHANGI; DE SIDDHARTHA; MULCHOPADHYAY SUDIT; CHAUDHARY SUMIT; KOUL SUMMON; SINGH UMESH; CHUGH ANITA; PALLE VENKATA P; MOOKHTIAR KASIM A; VACCA JOSEPH; CHAKRAVARTY PRASUN K; NARGUND RAVI P; WRIGHT SAMUEL D; ROY SOPHIE; GRAZIANO MICHAEL P; SINGH SHEO B; CULLY DORIS; CAI TIANQUAN,期刊：ACS Medicinal Chemistry Letters, 页码：919-923 , 文章类型： Article，,卷期：2011年2-12] L-2-Hydroxy acid oxidase (Hao2) is a peroxisomal enzyme with predominant expression in the liver and kidney. Hao2 was recently identified as a candidate gene for blood pressure quantitative trait locus in rats. To invest... Toward Overcoming Staphylococcus aureus Aminoglycoside Resistance Mechanisms with a Functionally Designed Neomycin Analogue [作者：HANESSIAN STEPHEN; GIGUERE ALEXANDRE; GRZYB JUSTYNA; MAIANTI JUAN PABLO; SAAVEDRA OSCAR M; AGGEN JAMES B; LINSELL MARTIN S; GOLDBLUM ADAM A; HILDEBRANDT DARIN J; KANE TIMOTHY R; DOZZO PAOLA; GLIEDT MICAH J; MATIAS ROWENA D; FEENEY LEE ANN; ARMSTRONG ELIANA S,期刊：ACS Medicinal Chemistry Letters, 页码：924-928 , 文章类型： Article，,卷期：2011年2-12] Deoxygenation of the diol groups in rings A and D of neomycin in combination with the introduction of an N1-(L)-HABA group in the 2-deoxystreptamine subunit (ring B) leads to a novel and potent antibiotic (1) with activi... Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity [作者：CHEN GANG; CHO SUNG JIN; HUANG XIPING; JENSEN NIELS H; SVENNEBRING ANDREAS; SASSANO MARIA F; ROTH BRYAN L; KOZIKOWSKI ALAN P,期刊：ACS Medicinal Chemistry Letters, 页码：929-932 , 文章类型： Article，,卷期：2011年2-12] The 5-HT(2C) receptor is an attractive drug target in the quest for new therapeutics to treat a variety of human disorders. We have previously undertaken a structural optimization campaign that has led to some potent and... Discovery of Benzodiazepine Sulfonamide-Based Bombesin Receptor Subtype 3 Agonists and Their Unusual Chirality [作者：LIU PING; LANZA THOMAS J JR; CHIODA MARC; JONES CARRIE; CHOBANIAN HARRY R; GUO YAN; CHANG LINDA; KELLY THERESA M; KAN YANQING; PALYHA OKSANA; GUAN XIAOMING; MARSH DONALD J; METZGER JOSEPH M; RAMSAY KATIE; WANG SHENGPING; STRACK ALISON M; MILLER RANDY; PANG JIANMEI; LYONS KATHY; DRAGOVIC JASMINKA; NING JIAN G; SCHAFER WES A; WELCH CHRISTOPHER J; GONG XIAOYI; GAO YINGDUO; HORNAK VIKTOR; BALL RICHARD G; TSOU NANCY; REITMAN MARC L; WYVRATT MATTHEW J; NARGUND RAVI P; LIN LINUS S,期刊：ACS Medicinal Chemistry Letters, 页码：933-937 , 文章类型： Article，,卷期：2011年2-12] We report herein the discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 (BRS-3) agonists and their unusual chirality. Starting from a high-throughput screening lead, we prepared a series of BRS-3 a... Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids [作者：CROSIGNANI STEFANO; JORANDLEBRUN CATHERINE; CAMPBELL GORDON; PRETRE ADELINE; GRIPPIVALLOTTON TANIA; QUATTROPANI ANNA; BOUSCARYDESFORGES GWENAELLE; BOMBRUN AGNES; MISSOTTEN MARC; HUMBERT YVES; FREMAUX CHRISTELE; PAQUET MIKAEL; EL HARKANI KAMEL; BRADSHAW CHARLES G; CLEVA CHRISTOPHE; ABLA NADA; DAFF HAMINA; SCHOTT OLIVIER; PITTET PIERREANDRE; ARRIGHI JEANFRANCOIS; GAUDET MARILENE; JOHNSON ZOE,期刊：ACS Medicinal Chemistry Letters, 页码：938-942 , 文章类型： Article，,卷期：2011年2-12] Antagonism of the CRTH2 receptor represents a very attractive target for a variety of allergic diseases. Most CRTH2 antagonists known to date possess a carboxylic acid moiety, which is essential for binding. However, pot... Supramolecular Ferric Porphyrins as Cyanide Receptors in Aqueous Solution [作者：WATANABE KENJI; KITAGISHI HIROAKI; KANO KOJI,期刊：ACS Medicinal Chemistry Letters, 页码：943-947 , 文章类型： Article，,卷期：2011年2-12] All fundamental data about binding of the cyanide to a supramolecular complex composed of a per-O-methylated beta-cyclodextrin dimer having an imidazole linker (Im3CD) and an anionic ferric porphyrin (Fe((III))TPPS) indi... 10 '-Fluorovinblastine and 10 '-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids [作者：GOTOH HIROAKI; DUNCAN KATHARINE K; ROBERTSON WILLIAM M; BOGER DALE L,期刊：ACS Medicinal Chemistry Letters, 页码：948-952 , 文章类型： Article，,卷期：2011年2-12] A study on the impact of catharanthine C10 and C12 indole substituents on the biomimetic Fe(III)-mediated coupling with vindoline led to the discovery and characterization of two new and substantially more potent derivat...