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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30条记录   Function of the D-Alanine:D-Alanine Ligase Lid Loop: A Molecular Modeling and Bioactivity Study [作者：HRAST MARTINA; VEHAR BLAZ; TURK SAMO; KONC JANEZ; GOBEC STANISLAV; JANEZIC DUSANKA,期刊：Journal of Medicinal Chemistry, 页码：6849-6856 , 文章类型： Article，,卷期：2012年55-15] D-Alanine:D-alanine ligase (Ddl) is an essential ATP-dependent bacterial enzyme involved in peptidoglycan biosynthesis. Discovery of Ddl inhibitors not competitive with ATP has proven to be difficult because the Ddl bimo... Conformationally-Locked N-Glycosides with Selective beta-Glucosidase Inhibitory Activity: Identification of a New Non-Iminosugar-Type Pharmacological Chaperone for Gaucher Disease [作者：CASTILLA JAVIER; RISQUEZ ROCIO; CRUZ DEYSI; HIGAKI KATSUMI; NANBA EIJI; OHNO KOUSAKU; SUZUKI YOSHIYUKI; DIAZ YOLANDA; ORTIZ MELLET CARMEN; GARCIA FERNANDEZ JOSE M; CASTILLON SERGIO,期刊：Journal of Medicinal Chemistry, 页码：6857-6865 , 文章类型： Article，,卷期：2012年55-15] A series of conformationally locked N-glycosides having a cis-1,2-fused pyranose-1,3-oxazoline-2-thione structure and bearing different substituents at the exocyclic sulfur has been prepared. The polyhydroxylated bicycli... 3-Oxoisoindoline-1-carboxamides: Potent, State-Dependent Blockers of Voltage-Gated Sodium Channel Na(V)1.7 with Efficacy in Rat Pain Models [作者：MACSARI ISTVAN; BESIDSKI YEYGENI; CSJERNYIK GABOR; NILSSON LINDA I; SANDBERG LARS; YNGVE ULRIKA; AHLIN KRISTOFER; BUETERS TJERK; ERIKSSON ANDERS B; LUND PERERIC; VENYIKE ELISABET; OERTHER SANDRA; BLAKEMAN KARIN HYGGE; LUO LEI; ARVIDSSON PER I,期刊：Journal of Medicinal Chemistry, 页码：6866-6880 , 文章类型： Article，,卷期：2012年55-15] The voltage-gated sodium channel Na(V)1.7 is believed to be a critical mediator of pain sensation based on clinical genetic studies and pharmacological results. Clinical utility of nonselective sodium channel blockers is... Critical Effect of Peptide Cyclization on the Potency of Peptide Inhibitors against Dengue Virus NS2B-NS3 Protease [作者：XU SHAOQIONG; LI HUA; SHAO XIAOXIA; FAN CHONGXU; ERICKSEN BRYAN; LIU JINSONG; CHI CHENGWU; WANG CHUNGUANG,期刊：Journal of Medicinal Chemistry, 页码：6881-6887 , 文章类型： Article，,卷期：2012年55-15] Dengue virus (DENY) infection is a serious public health threat worldwide that demands effective treatment. In the search for potent virus protease inhibitors, several cone snail venoms were screened against serotype 2 D... Designing Allosteric Regulators of Thrombin. Monosulfated Benzofuran Dimers Selectively Interact With Arg173 of Exosite 2 to Induce Inhibition [作者：AZIZ MAY H ABDEL; SIDHU PREETPAL SINGH; LIANG AIYE; KIM JI YEONG; MOSIER PHILIP D; ZHOU QIBING; FARRELL DAVID H; DESAI UMESH R,期刊：Journal of Medicinal Chemistry, 页码：6888-6897 , 文章类型： Article，,卷期：2012年55-15] Earlier, we reported on the design of sulfated benzofuran dimers (SBDs) as allosteric inhibitors of thrombin (Sidhu et al. J. Med. Chem. 2011 54 5522-5531). To identify the site of binding of SBDs, we studied thrombin in... Discovery of Potent Inhibitors of Human and Mouse Fatty Acid Amide Hydrolases [作者：BUTINI STEFANIA; BRINDISI MARGHERITA; GEMMA SANDRA; MINETTI PATRIZIA; CABRI WALTER; GALLO GRAZIA; VINCENTI SILVIA; TALAMONTI EMANUELA; BORSIN FRANCO; CAPRIOLI ANTONIO; STASI MARIA ANTONIETTA; DI SERIO STEFANO; ROS SINDU; BORRELLI GIUSEPPE; MARAMAI SAMUELE; FEZZA FILOMENA; CAMPIANI GIUSEPPE; MACCARRONE MAURO,期刊：Journal of Medicinal Chemistry, 页码：6898-6915 , 文章类型： Article，,卷期：2012年55-15] Fatty acid amide hydrolase (FAAH, EC 3.5.1.99) is the main enzyme catabolizing endocannabinoid fatty acid amides. FAAH inactivation promotes beneficial effects upon pain and anxiety without the side effects accompanying ... Novel N-Linked Aminopiperidine Inhibitors of Bacterial Topoisomerase Type II with Reduced pK(a): Antibacterial Agents with an Improved Safety Profile [作者：RECK FOLKERT; ALM RICHARD A; BRASSIL PATRICK; NEWMAN JOSEPH V; CIACCIO PAUL; MCNULTY JOHN; BARTHOW HERBERT; GOTETI KOSALARAM; BREEN JOHN; COMITAPREVOIR JANE LLE; CRONIN MARK; EHMANN DAVID E; GENG BOLIN; GODFREY ANDREW AYDON; FISHER STEWART L,期刊：Journal of Medicinal Chemistry, 页码：6916-6933 , 文章类型： Article，,卷期：2012年55-15] Novel non-fluoroquinolone inhibitors of bacterial type II topoisornerases (DNA gyrase and topoisomerase IV) are of interest for the development of new antibacterial agents that are not impacted by target-mediated cross-r... Antibiotic Optimization and Chemical Structure Stabilization of Thiomuracin A [作者：LAMARCHE MATTHEW J; LEEDS JENNIFER A; DZINKFOX JOANNE; GANGL ERIC; KRASTEL PHILIPP; NECKERMANN GEORG; PAESTRANT DEBORAH; PATANE MICHAEL A; RANN ELM N M; TIARNFOOK STACEY; YU DONGHUI,期刊：Journal of Medicinal Chemistry, 页码：6934-6941 , 文章类型： Article，,卷期：2012年55-15] Synthetic studies of the antimicrobial secondary metabolite thiomuracin A (1) were initiated to improve chemical stability and physicochemical properties. Functional group modifications of 1 included removing the C2-C7 s... Zwitterions Can Be Predominant in Membrane Penetration of Drugs: Experimental Proof [作者：MAZAK KAROLY; NOSZAL BELA,期刊：Journal of Medicinal Chemistry, 页码：6942-6947 , 文章类型： Article，,卷期：2012年55-15] The complete set of species-specific partition coefficients was determined, and the predominant contribution of zwitterionic species to the overall lipophilicity was experimentally proven for the first time. The compound... Optimization of 4-Aminoquinoline/Clotrimazole-Based Hybrid Antimalarials: Further Structure-Activity Relationships, in Vivo Studies, and Preliminary Toxicity Profiling [作者：GEMMA SANDRA; CAMODECA CATERINA; COCCONE SALVATORE SANNA; JOSHI BHUPENDRA P; BERNETTI MATTEO; MORETTI VITTORIA; BROGI SIMONE; DE MARCOS MARIA CRUZ BONACHE; SAVINI LUISA; TARAMELLI DONATELLA; BASILICO NICOLETTA; PARAPINI SILVIA; ROTTMANN MATTHIAS; BRUN RETO; LAMPONI STEFANIA; CACCIA SILVIO; GUISO GIOVANNA; SUMMERS ROBERT L; MARTIN ROVENA E; SAPONARA SIMONA; GORELLI BEATRICE; NOVELLINO ETTORE; CAMPIANI GIUSEPPE; BUTINI STEFANIA,期刊：Journal of Medicinal Chemistry, 页码：6948-6967 , 文章类型： Article，,卷期：2012年55-15] Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development of a novel antima... Design of Fully Synthetic, Self-Adjuvanting Vaccine Incorporating the Tumor-Associated Carbohydrate Tn Antigen and Lipoamino Acid-Based Toll-like Receptor 2 Ligand [作者：ABDELAAL ABUBAKER M; ELNAGGAR DINA; ZAMAN MEHFUZ; BATZLOFF MICHAEL; TOTH ISTVAN,期刊：Journal of Medicinal Chemistry, 页码：6968-6974 , 文章类型： Article，,卷期：2012年55-15] Overexpression of certain tumor-associated carbohydrate antigens (TACA) caused by malignant transformation offers promising targets to develop novel antitumor vaccines, provided the ability to break their inherent low im... Discovery of a Series of 2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as Novel Molecular Switches that Modulate Modes of K(v)7.2 (KCNQ2) Channel Pharmacology: Identification of (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a Potent, Brain Penetrant K(v)7.2 Channel Inhibitor [作者：CHEUNG YIUYIN; YU HAIBO; XU KAIPING; ZOU BEIYAN; WU MENG; MCMANUS OWEN B; LI MIN; LINDSLEY CRAIG W; HOPKINS COREY R,期刊：Journal of Medicinal Chemistry, 页码：6975-6979 , 文章类型： Article，,卷期：2012年55-15] A potent and selective inhibitor of KCNQ2, (S)-5 (ML252, IC50 = 69 nM), was discovered after a high-throughput screen of the MLPCN library was performed. SAR studies revealed a small structural change (ethyl group to hyd... Biological Evaluation of Dodecaborate-Containing L-Amino Acids for Boron Neutron Capture Therapy [作者：HATTORI YOSHIHIDE; KUSAKA SHINTARO; MUKUMOTO MARI; UEHARA KOUKI; ASANO TOMOYUKI; SUZUKI MINORU; MASUNAGA SHINICHIRO; ONO KOJI; TANIMORI SHINJI; KIRIHATA MITSUNORI,期刊：Journal of Medicinal Chemistry, 页码：6980-6984 , 文章类型： Article，,卷期：2012年55-15] To develop a boron carrier for practical purposes, new boron-containing amino acids with an undecahydro-closo-dodecaboranylthio ([(B12H11S)-B-10](2-)-) unit in the side chain of the a-amino acid have already been designe... First Total Synthesis of Protoapigenone and Its Analogues as Potent Cytotoxic Agents (vol 50, pg 3921, 2007) [作者：LIN ANSHEN; NAKAGAWAGOTO KYOKO; CHANG FANGRONG; YU DONGLEI; MORRISNATSCHKE SUSAN L; WU CHINCHUNG; CHEN SHULI; WU YANGCHANG; LEE KUOHSIUNG,期刊：Journal of Medicinal Chemistry, 页码：6985-6985 , 文章类型： Correction，,卷期：2012年55-15]