- 2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRp
[作者:Pacini, B; Avolio, S; Ercolani, C; Koch, U; Migliaccio, G; Narjes, F; Pacini, L; Tomei, L; Harper, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6245-6249 , 文章类型: Article,,卷期:2009年19-21]
- A series of 2-(3-thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acid inhibitors of the hepatitis C virus (HCV) NS5B polymerase enzyme are reported. Sulfonyl urea substituted analogs in this series proved to be the most po...
- N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: The development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models
[作者:Jones, P; Griffin, AM; Gawell, L; Lavoie, R; Delorme, D; Roberts, E; Brown, W; Walpole, C; Xiao, WH; Boulet, J; Labarre, M; Coupal, M; Butterworth, J; St-Onge, S; Hodzic, L; Salois, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5994-5998 , 文章类型: Article,,卷期:2009年19-21]
- We have investigated a series of phenolic diaryl amino piperidine delta opioid receptor agonists, establishing the importance of the phenol functional group and substitution on the piperdine nitrogen for delta agonist ac...
- Delta agonist hydroxy bioisosteres: The discovery of 3-((1-benzylpiperidin-4-yl){4-[(diethylamino)carbonyl]phenyl}amino)benzamide with improved delta agonist activity and in vitro metabolic stability
[作者:Griffin, AM; Brown, W; Walpole, C; Coupal, M; Adam, L; Gosselin, M; Salois, D; Morin, PE; Roumi, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5999-6003 , 文章类型: Article,,卷期:2009年19-21]
- We have investigated phenol replacements in a series of diaryl amino piperidine delta opioid agonists. From this study we have demonstrated that the hydroxy functional group can be replaced with a primary amide group, gi...
- Synthesis and biological evaluation of berberine analogues as novel up-regulators for both low-density-lipoprotein receptor and insulin receptor
[作者:Wang, YX; Wang, YP; Zhang, H; Kong, WJ; Li, YH; Liu, F; Gao, RM; Liu, T; Jiang, JD; Song, DQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6004-6008 , 文章类型: Article,,卷期:2009年19-21]
- Berberine (BBR) is a natural compound with up-regulating activity on both low-density-lipoprotein receptor (LDLR) and insulin receptor (InsR). This one-drug-multiple-target characteristic might be suitable for the treatm...
- Glucose-containing flavones-their synthesis and antioxidant and neuroprotective activities
[作者:Kim, SH; Kumar, CN; Kim, HJ; Kim, DH; Cho, J; Jin, C; Lee, YS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6009-6013 , 文章类型: Article,,卷期:2009年19-21]
- Due to high reactivity, reactive oxygen species can attack biological molecules leading to cell or tissue injury. In this study, glucose moiety was attached at the C-7 position of quercetin 3-O-methyl ether (1) and luteo...
- Carbonic anhydrase II-induced selection of inhibitors from a dynamic combinatorial library of Schiff's bases
[作者:Nasr, G; Petit, E; Supuran, CT; Winum, JY; Barboiu, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6014-6017 , 文章类型: Article,,卷期:2009年19-21]
- A dynamic combinatorial library (DCL) has been generated under thermodynamic control by using the aminocarbonyl/imine interconversion as reversible chemistry, combined with non-covalent binding within the active site of ...
- Tetrahydroquinoline sulfonamides as vasopressin 1b receptor anatgonists
[作者:Scott, JD; Miller, MW; Li, SW; Lin, SI; Vaccaro, HA; Hong, LW; Mullins, DE; Guzzi, M; Weinstein, J; Hodgson, RA; Varty, GB; Stamford, AW; Chan, TY; McKittrick, BA; Greenlee, WJ; Priestley, T; Parker, EM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6018-6022 , 文章类型: Article,,卷期:2009年19-21]
- Vasopressin 1b (V1b) antagonists have been postulated as possible treatments for depression and anxiety. A novel series of potent and selective V1b antagonists has been identified starting from an in-house screen hit. Th...
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