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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96条记录   6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors [作者：Cai, JQ; Baugh, M; Black, D; Long, C; Bennett, DJ; Dempster, M; Fradera, X; Gillespie, J; Andrews, F; Boucharens, S; Bruin, J; Cameron, KS; Cumming, I; Hamilton, W; Jones, PS; Kaptein, A; Kinghorn, E; Maidment, M; Martin, I; Mitchell, A; Rankovic, Z; Robinson, J; Scullion, P; Uitdehaag, JCM; Vink, P; Westwood, P; van Zeeland, M; van Berkom, L; Bastiani, M; Meulemans, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4350-4354 , 文章类型： Article，,卷期：2010年20-15] 6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stab... LuxR-dependent quorum sensing: Computer aided discovery of new inhibitors structurally unrelated to N-acylhomoserine lactones [作者：Soulere, L; Sabbah, M; Fontaine, F; Queneau, Y; Doutheau, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4355-4358 , 文章类型： Article，,卷期：2010年20-15] A virtual screening, involving flexible docking sequences within the LuxR, TraR and LasR binding sites, was used as a structural binding sites similarity filter to specifically target conserved residues in the proteins o... Identification of glycosylated exendin-4 analogue with prolonged blood glucose-lowering activity through glycosylation scanning substitution [作者：Ueda, T; Ito, T; Tomita, K; Togame, H; Fumoto, M; Asakura, K; Oshima, T; Nishimura, SI; Hanasaki, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4631-4634 , 文章类型： Article，,卷期：2010年20-15] Exendin-4, a glucagon-like peptide 1 receptor agonist, is a potent therapeutic xenopeptide hormone for the treatment of type 2 diabetes. In order to further improve in vivo activity, we examined the introduction of sialy... Propenylamide and propenylsulfonamide cephalosporins as a novel class of anti-MRSA beta-lactams [作者：Pohlmann, J; Vasilevich, NI; Glushkov, AI; Kellenberger, L; Shapiro, S; Caspers, P; Page, MGP; Danel, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4635-4638 , 文章类型： Article，,卷期：2010年20-15] Novel C(3) propenylamide and propenylsulfonamide cephalosporins have been synthesized and tested for their ability to inhibit the penicillin-binding protein 2' (PBP2') from Staphylococcus epidermidis and the growth of a ... BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296 [作者：Clarke, B; Cutler, L; Demont, E; Dingwall, C; Dunsdon, R; Hawkins, J; Howes, C; Hussain, I; Maile, G; Matico, R; Mosley, J; Naylor, A; O'Brien, A; Redshaw, S; Rowland, P; Soleil, V; Smith, KJ; Sweitzer, S; Theobald, P; Vesey, D; Walter, DS; Wayne, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4639-4644 , 文章类型： Article，,卷期：2010年20-15] Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described a series of potent inhibitors based on an hydroxyethylamine (HEA) transiti... Deoxynojirimycin and its hexosaminyl derivatives bind to natural killer cell receptors rNKR-P1A and hCD69 [作者：Catelani, G; D'Andrea, F; Griselli, A; Guazzelli, L; Nemcova, P; Bezouska, K; Krenek, K; Kren, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4645-4648 , 文章类型： Article，,卷期：2010年20-15] Deoxynojirimycin (1) and two new related 4-O-hexosaminyl-containing disaccharide mimics, beta-D-TalNAc-( 1 -> 4)-DNJ (4) and beta-D-ManNAc-(1 -> 4)-DNJ (5), have been studied as agonists of natural killer (NK) cell recep... Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites [作者：Hodgetts, KJ; Blum, CA; Caldwell, T; Bakthavatchalam, R; Zheng, XZ; Capitosti, S; Krause, JE; Cortright, D; Crandall, M; Murphy, BA; Boyce, S; Jones, AB; Chenard, BL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4359-4363 , 文章类型： Article，,卷期：2010年20-15] The transient receptor potential cation channel, subfamily V, member 1 (TRPV1) is a non-selective cation channel that can be activated by a wide range of noxious stimuli, including capsaicin, acid, and heat. Blockade of ... Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif [作者：Klee, N; Wong, PE; Baragana, B; El Mazouni, F; Phillips, MA; Barrett, MP; Gilbert, IH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4364-4366 , 文章类型： Article，,卷期：2010年20-15] Trypanosoma brucei, the parasite that causes human African trypanosomiasis, is auxotrophic for purines and has specialist nucleoside transporters to import these metabolites. In particular, the P2 aminopurine transporter... 10-23 DNAzyme modified with (2 ' R)- and (2 ' S)-2 '-deoxy-2 '-C-methyluridine in the catalytic core [作者：Robaldo, L; Montserrat, JM; Iribarren, AM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4367-4370 , 文章类型： Article，,卷期：2010年20-15] The catalytic core of a 10-23 DNAzyme was modified using (2'R), (2'S)-2'-deoxy-2'-C-methyluridine and LNA-T. Catalytic activities under pseudo first order conditions were compared at different Mg2+ concentrations, indica... Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists [作者：Galambos, J; Wagner, G; Nogradi, K; Bielik, A; Molnar, L; Bobok, A; Horvath, A; Kiss, B; Kolok, S; Nagy, J; Kurko, D; Bakk, ML; Vastag, M; Saghy, K; Gyertyan, I; Gal, K; Greiner, I; Szombathelyi, Z; Keseru, GM; Domany, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4371-4375 , 文章类型： Article，,卷期：2010年20-15] Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of this class of compounds was successfully eliminated. Systema... Use of 2-[F-18]fluoroethylazide for the Staudinger ligation - Preparation and characterisation of GABA(A) receptor binding 4-quinolones [作者：Gaeta, A; Woodcraft, J; Plant, S; Goggi, J; Jones, P; Battle, M; Trigg, W; Luthra, SK; Glaser, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4649-4652 , 文章类型： Article，,卷期：2010年20-15] The labelling reagent 2-[F-18]fluoroethylazide was used in a traceless Staudinger ligation. This reaction was employed to obtain the GABA(A) receptor binding 6-benzyl-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid (2-[F-1... Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor [作者：Beswick, PJ; Billinton, A; Chambers, LJ; Dean, DK; Fonfria, E; Gleave, RJ; Medhurst, SJ; Michel, AD; Moses, AP; Patel, S; Roman, SA; Roomans, S; Senger, S; Stevens, AJ; Walter, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4653-4656 , 文章类型： Article，,卷期：2010年20-15] Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be a potent anti-hyperalgesic age... Design, synthesis, and structure-activity relationships of pyrazole derivatives as potential FabH inhibitors [作者：Lv, PC; Sun, JA; Luo, Y; Yang, Y; Zhu, HL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4657-4660 , 文章类型： Article，,卷期：2010年20-15] Fatty acid biosynthesis is essential for bacterial survival. FabH, beta-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthe... Synthesis, antidepressant evaluation and QSAR studies of novel 2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)-N-(substituted phenyl)acetamides [作者：Shelke, SM; Bhosale, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4661-4664 , 文章类型： Article，,卷期：2010年20-15] In search for novel antidepressants, a series of 2-(5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)-N-(substituted phenyl) acetamides was synthesized and screened for potential antidepressant activity by tail suspension test (T... Synthesis of polyhalo acridones as pH-sensitive fluorescence probes [作者：Huang, C; Yan, SJ; Li, YM; Huang, R; Lin, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4665-4669 , 文章类型： Article，,卷期：2010年20-15] Polyhalo isophthalonitriles were reacted with substituted anilines and subsequently cyclocondensed in the presence of sulfuric acid to give polyhalo acridones. These polyhalo acridones were proven to be useful as pH-sens... Carbonic anhydrase inhibitors. The X-ray crystal structure of human isoform II in adduct with an adamantyl analogue of acetazolamide resides in a less utilized binding pocket than most hydrophobic inhibitors [作者：Avvaru, BS; Wagner, JM; Maresca, A; Scozzafava, A; Robbins, AH; Supuran, CT; McKenna, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4376-4381 , 文章类型： Article，,卷期：2010年20-15] We investigated the inhibitory activity of several 1,3,4-thiadiazole-sulfonamides against all catalytically active CA (EC 4.2.1.1), CA I-XV. The tail derivatizing the 5-position in the 1,3,4-thiadiazole-2-sulfonamide sca...