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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53条记录   1,5-Benzodiazepine inhibitors of HCV NS5B polymerase [作者：McGowan, D; Nyanguile, O; Cummings, MD; Vendeville, S; Vandyck, K; Van den Broeck, W; Boutton, CW; De Bondt, H; Quirynen, L; Amssoms, K; Bonfanti, JF; Last, S; Rombauts, K; Tahri, A; Hu, LL; Delouvroy, F; Vermeiren, K; Vandercruyssen, G; Van der Helm, L; Cleiren, E; Mostmans, W; Lory, P; Pille, G; Van Emelen, K; Fanning, G; Pauwels, F; Lin, TI; Simmen, K; Raboisson, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2492-2496 , 文章类型： Article，,卷期：2009年19-9] Optimization through parallel synthesis of a novel series of hepatitis C virus (HCV) NS5B polymerase inhibitors led to the identification of (R)-11-(4-benzyloxy-2-fluorophenyl)-6-hydroxy-3,3-dimethyl-10-(6-methylpyridine... Synthesis and biological evaluation of technetium-labeled D-glucose-MAG(3) derivative as agent for tumor diagnosis [作者：de Barros, ALB; Cardoso, VN; Mota, LD; Leite, EA; de Oliveira, MC; Alves, RJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2497-2499 , 文章类型： Article，,卷期：2009年19-9] A D-glucose-MAG3 derivative was successfully synthesized and radiolabeled in high labeling yield. Biodistribution studies in Ehrlich tumor-bearing mice were performed. This compound showed high accumulation in tumor tiss... Diversity-oriented synthesis of a cytisine-inspired pyridone library leading to the discovery of novel inhibitors of Bcl-2 [作者：Marcaurelle, LA; Johannes, C; Yohannes, D; Tillotson, BP; Mann, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2500-2503 , 文章类型： Article，,卷期：2009年19-9] Four enantiopure cytisine-inspired scaffolds can be accessed via a versatile pyrrolidine template derived from a stereocontrolled [3+2] azomethine ylide-alkene cycloaddition. Differential ester protection allows for the ... 4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors [作者：Liddle, J; Bamborough, P; Barker, MD; Campos, S; Cousins, RPC; Cutler, GJ; Hobbs, H; Holmes, DS; Ioannou, C; Mellor, GW; Morse, MA; Payne, JJ; Pritchard, JM; Smith, KJ; Tape, DT; Whitworth, C; Williamson, RA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2504-2508 , 文章类型： Article，,卷期：2009年19-9] The synthesis and SAR of a novel series of IKK2 inhibitors are described. Modi. cation around the hinge binding region of the 7-azaindole led to a series of potent and selective inhibitors with good cellular activity. (C... Inhibition of monoamine oxidase by (E)-styrylisatin analogues [作者：Van der Walt, EM; Milczek, EM; Malan, SF; Edmondson, DE; Castagnoli, N; Bergh, JJ; Petzer, JP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2509-2513 , 文章类型： Article，,卷期：2009年19-9] Previous studies have shown that (E)-8-(3-chlorostyryl) caffeine (CSC) is a specific reversible inhibitor of human monoamine oxidase B (MAO-B) and does not bind to human MAO-A. Since the small molecule isatin is a natura... Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3) [作者：Kuduk, SD; Di Marco, CN; Chang, RK; DiPardo, RM; Cook, SP; Cato, MJ; Jovanovska, A; Urban, MO; Leitl, M; Spencer, RH; Kane, SA; Bilodeau, MT; Hartman, GD; Bock, MG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2514-2518 , 文章类型： Article，,卷期：2009年19-9] A series of amiloride derivatives modified at the 5-position of the pyrazine ring were evaluated as inhibitors of acid-sensing ion channel-3 (ASIC3), a novel target for the treatment of chronic pain. (C) 2009 Elsevier Lt... The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety [作者：Ho, GD; Anthes, J; Bercovici, A; Caldwell, JP; Cheng, KC; Cui, XM; Fawzi, A; Fernandez, X; Greenlee, WJ; Hey, J; Korfmacher, W; Lu, SX; McLeod, RL; Ng, F; Torhan, AS; Tan, Z; Tulshian, D; Varty, GB; Xu, XY; Zhang, HT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2519-2523 , 文章类型： Article，,卷期：2009年19-9] The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1] octane) derivatives as optimized ligands. These compounds exhibit hig... 3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization [作者：Duplantier, AJ; Efremov, I; Candler, J; Doran, AC; Ganong, AH; Haas, JA; Hanks, AN; Kraus, KG; Lazzaro, JT; Lu, JM; Maklad, N; McCarthy, SA; O'Sullivan, TJ; Rogers, BN; Siuciak, JA; Spracklin, DK; Zhang, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2524-2529 , 文章类型： Article，,卷期：2009年19-9] The discovery, synthesis and SAR of a novel series of 3-benzyl-1,3-oxazolidin-2-ones as positive allosteric modulators (PAMs) of mGluR2 is described. Expedient hit-to-lead work on a single HTS hit led to the identificati... (+/-)-Nantenine analogs as antagonists at human 5-HT2A receptors: C1 and flexible congeners [作者：Chaudhary, S; Pecic, S; LeGendre, O; Navarro, HA; Harding, WW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2530-2532 , 文章类型： Article，,卷期：2009年19-9] C1 and flexible analogs of (+/-)-nantenine were synthesized and evaluated for antagonist activity at human 5-HT(2)A receptors in a calcium mobilization assay. This work has resulted in the identification of the most pote... Stereochemical effects of all-hydrocarbon tethers in i,i+4 stapled peptides [作者：Kim, YW; Verdine, GL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2533-2536 , 文章类型： Article，,卷期：2009年19-9] The stereochemical effects of the hydrocarbon crosslink on the conformation and cellular uptake of i,i+4 stapled peptides were studied. Compared to its S, S-configurated counterpart, the crosslink bearing the R,R-configu... The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents [作者：DeNinno, MP; Andrews, M; Bell, AS; Chen, Y; Eller-Zarbo, C; Eshelby, N; Etienne, JB; Moore, DE; Palmer, MJ; Visser, MS; Yu, LJ; Zavadoski, WJ; Gibbs, EM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2537-2541 , 文章类型： Article，,卷期：2009年19-9] Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors.... Synthesis and biological evaluation of novel 4-(hetero) aryl-2-piperazino quinazolines as anti-leishmanial and anti-proliferative agents [作者：Kumar, S; Shakya, N; Gupta, S; Sarkar, J; Sahu, DP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2542-2545 , 文章类型： Article，,卷期：2009年19-9] A series of new class of 4-(hetero) aryl-2-piperazino quinazolines were synthesized and assessed for in vitro activity against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among the c... Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a cb1 receptor antagonist with in vivo antiobesity effect [作者：Srivastava, BK; Soni, R; Patel, JZ; Joharapurkar, A; Sadhwani, N; Kshirsagar, S; Mishra, B; Takale, V; Gupta, S; Pandya, P; Kapadnis, P; Solanki, M; Patel, H; Mitra, P; Jain, MR; Patel, PR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2546-2550 , 文章类型： Article，,卷期：2009年19-9] A few thienyl substituted pyrazole derivatives were synthesized to aid in the characterization of the cannabinoid receptor antagonist and also to serve as potentially useful antiobesity agent. Structural requirements for... Structural modification of 3-arylisoquinolines to isoindolo[2,1-b]isoquinolinones for the development of novel topoisomerase 1 inhibitors with molecular docking study [作者：Van, HTM; Cho, WJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2551-2554 , 文章类型： Article，,卷期：2009年19-9] Isoindolo[2,1-b]isoquinolinones 9a-i were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular cyclization reaction. Among the synthesized compounds, 9d exhibited potent topoisom... New Rev-export inhibitor from Alpinia galanga and structure-activity relationship [作者：Tamura, S; Shiomi, A; Kaneko, M; Ye, Y; Yoshida, M; Yoshikawa, M; Kimura, T; Kobayashi, M; Murakami, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2555-2557 , 文章类型： Article，,卷期：2009年19-9] Bioassay-guided separation by use of the fission yeast expressing NES of Rev, an HIV-1 viral regulatory protein, disclosed 1'-acetoxychavicol acetate (ACA, 1) as a new inhibitor for nuclear export of Rev from the roots o... Synthesis and antibacterial activities of novel oxazolidinones having spiro[2,4]heptane moieties [作者：Kim, SY; Park, HB; Cho, JH; Yoo, KH; Oh, CH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2558-2561 , 文章类型： Article，,卷期：2009年19-9] The synthesis of a new series of oxazolidinones having spiro[2,4]heptane moieties is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of ...