- 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...
- 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...
- 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....
- 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...
- 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 ...
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