- Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E-coli
[作者:Aberg, V; Das, P; Chorell, E; Hedenstrom, M; Pinkner, JS; Hultgren, SJ; Almqvist, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3536-3540 , 文章类型: Article,,卷期:2008年18-12]
- Ring-fused 2-pyridones, termed pilicides, are small synthetic compounds that inhibit pilus assembly in uropathogenic Escherichia coli. Their biological activity is clearly dependent upon a carboxylic acid functionality. ...
- Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPAR alpha/gamma agonists
[作者:Ye, XY; Li, YX; Farrelly, D; Flynn, N; Gu, LQ; Locke, KT; Lippy, J; O'Malley, K; Twamley, C; Zhang, LT; Ryono, DE; Zahler, R; Hariharan, N; Cheng, PTW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3545-3550 , 文章类型: Article,,卷期:2008年18-12]
- Several series of substituted dehydropiperidine and piperidine-4-carboxylic acid analogs have been designed and synthesized as novel, potent dual PPAR alpha/gamma agonists. The SAR of these series of analogs is discussed...
- 4,5-disubstituted oxazolidinones: High affinity molecular effectors of RNA function
[作者:Anupam, R; Nayek, A; Green, NJ; Grundy, FJ; Henkin, TM; Means, JA; Bergmeier, SC; Hines, JV,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3541-3544 , 文章类型: Article,,卷期:2008年18-12]
- The T box transcription antitermination system is a riboswitch found primarily in Gram-positive bacteria which monitors the aminoacylation of the cognate tRNA and regulates a variety of amino acid-related genes. Novel 4,...
- Pleuromutilin derivatives having a purine ring. Part 1: New compounds with promising antibacterial activity against resistant Gram-positive pathogens
[作者:Hirokawa, Y; Kinoshita, H; Tanaka, T; Nakamura, T; Fujimoto, K; Kashimoto, S; Kojima, T; Kato, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3556-3561 , 文章类型: Article,,卷期:2008年18-12]
- In the course of our research aimed at the discovery of metabolic stable pleuromutilin derivatives with more potent antibacterial activity against Gram-positive pathogens than previous analogues, a series of compounds be...
- Substituted dipiperidine alcohols as potent CCR2 antagonists
[作者:Xia, MD; Hou, CF; DeMong, D; Pollack, S; Pan, M; Brackley, J; Singer, M; Matheis, M; Cavender, D; Wachter, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3562-3564 , 文章类型: Article,,卷期:2008年18-12]
- The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC50 values in th...
- Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase
[作者:Tipparaju, SK; Joyasawal, S; Forrester, S; Mulhearn, DC; Pegan, S; Johnson, ME; Mesecar, AD; Kozikowski, AP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3565-3569 , 文章类型: Article,,卷期:2008年18-12]
- Enoyl-ACP reductase (ENR), the product of the FabI gene, from Bacillus anthracis (BaENR) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis. A number of novel 2-pyridone derivatives were sy...
- Facile formation of hydrophilic derivatives of 5H-8,9-dimethoxy-5-[2-(N,N-dimethylamino)ethyl]-2,3-methylenedioxydibenzo[c,h] [1,6]naphthyridin-6-one (ARC-111) and its 12-aza analog via quaternary ammonium intermediates
[作者:Feng, W; Satyanarayana, M; Tsai, YC; Liu, AA; Liu, LF; LaVoie, EJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3570-3572 , 文章类型: Article,,卷期:2008年18-12]
- Several new TOP1-targeting agents were prepared using as intermediates the N,N,N-trimethyl quaternary ammonium salts of either ARC-111 or its 12-aza analog (ARC-31), 3 and 4, respectively. Direct displacement of the quat...
- Synthesis, biological evaluation and radiochemical labeling of a dansylhydrazone derivative as a potential imaging agent for apoptosis
[作者:Zeng, WB; Yao, ML; Townsend, D; Kabalka, G; Wall, J; Le Puil, M; Biggerstaff, J; Miao, WM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3573-3577 , 文章类型: Article,,卷期:2008年18-12]
- To develop a small molecule-based tracer for in vivo apoptosis imaging, dansylhydrazone (DFNSH) was synthesized in 93% yield in less than 30 min. The biological evaluation showed that DFNSH selectively binds to paclitaxe...
- 2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3)
[作者:Lum, C; Kahl, J; Kessler, L; Kucharski, J; Lundstrom, J; Miller, S; Nakanishi, H; Pei, YZ; Pryor, K; Roberts, E; Sebo, L; Sullivan, R; Urban, J; Wang, ZJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3578-3581 , 文章类型: Article,,卷期:2008年18-12]
- The discovery of two classes of pyrimidine-based inhibitors of GSK-3 is described. Optimization of these series led to inhibitors with IC50 < 10 nM and > 100-fold selectivity over Aurora A kinase. A proposed binding mode...
- Synthesis of new UV-B light absorbents: (Acetylphenyl) glycosides with antioxidant activities
[作者:Otani, T; Tsubogo, T; Furukawa, N; Saito, T; Uchida, K; Iwama, K; Kanai, Y; Yajima, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3582-3584 , 文章类型: Article,,卷期:2008年18-12]
- m-Acetylphenyl-beta-D-glucopyranosides and m-acetylphenyl-alpha/beta-D-mannopyranosides were synthesized by the Koenigs-Knorr, Mitsunobu, and Helferich reactions as key glycosylation reactions, respectively. Their spectr...
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