- Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: Part 2, optimization for blood pressure reduction in spontaneously hypertensive rats
[作者:Ginn, JD; Bosanac, T; Chen, R; Cywin, C; Hickey, E; Kashem, M; Kerr, S; Kugler, S; Li, XA; Prokopowicz, A; Schlyer, S; Smith, JD; Turner, MR; Wu, F; Young, ERR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5153-5156 , 文章类型: Article,,卷期:2010年20-17]
- Phenylglycine substituted isoquinolones 1 and 2 have previously been described as potent dual ROCK1/ROCK2 inhibitors. Here we describe the further SAR of this series to improve metabolic stability and rat oral exposure. ...
- New halogenated 3-phenylcoumarins as potent and selective MAO-B inhibitors
[作者:Matos, MJ; Vina, D; Janeiro, P; Borges, F; Santana, L; Uriarte, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5157-5160 , 文章类型: Article,,卷期:2010年20-17]
- With the aim to find out the structural features for the MAO inhibitory activity and selectivity, in the present communication we report the synthesis and pharmacological evaluation of a new series of bromo-6-methyl-3-ph...
- Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists)
[作者:Gerspacher, M; Altmann, E; Beerli, R; Buhl, T; Endres, R; Gamse, R; Kameni-Tcheudji, J; Kneissel, M; Krawinkler, KH; Missbach, M; Schmidt, A; Seuwen, K; Weiler, S; Widler, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5161-5164 , 文章类型: Article,,卷期:2010年20-17]
- A series of novel benzimidazole derivatives has been designed via a scaffold morphing approach based on known calcilytics chemotypes. Subsequent lead optimisation led to the discovery of penta-substituted benzimidazoles ...
- Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists
[作者:Davenport, AJ; Stimson, CC; Corsi, M; Vaidya, D; Glenn, E; Jones, TD; Bailey, S; Gemkow, MJ; Fritz, U; Hallett, DJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5165-5169 , 文章类型: Article,,卷期:2010年20-17]
- A series of potent and subtype selective H3 receptor antagonists containing a novel tetrazole core and diamine motif is reported. A one-pot multi-component Ugi reaction was utilised to rapidly develop the structure-activ...
- Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors
[作者:Belanger, DB; Curran, PJ; Hruza, A; Voigt, J; Meng, ZY; Mandal, AK; Siddiqui, MA; Basso, AD; Gray, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5170-5174 , 文章类型: Article,,卷期:2010年20-17]
- The synthesis and structure-activity relationships (SAR) of novel, potent imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors are described. The X-ray crystal structure of imidazo[1,2-a]pyrazine Aurora inhibitor 1j is ...
- Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu(4) positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)
[作者:Engers, DW; Gentry, PR; Williams, R; Bolinger, JD; Weaver, CD; Menon, UN; Conn, PJ; Lindsley, CW; Niswender, CM; Hopkins, CR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5175-5178 , 文章类型: Article,,卷期:2010年20-17]
- Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel appro...
- Synthesis and evaluation of oryzalin analogs against Toxoplasma gondii
[作者:Endeshaw, MM; Li, C; de Leon, J; Yao, N; Latibeaudiere, K; Premalatha, K; Morrissette, N; Werbovetz, KA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5179-5183 , 文章类型: Article,,卷期:2010年20-17]
- The synthesis and evaluation of 20 dinitroanilines and related compounds against the obligate intracellular parasite Toxoplasma gondii is reported. Using in vitro cultures of parasites in human fibroblasts, we determined...
- Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1 beta converting enzyme (ICE or caspase 1)
[作者:Galatsis, P; Caprathe, B; Gilmore, J; Thomas, A; Linn, K; Sheehan, S; Harter, W; Kostlan, C; Lunney, E; Stankovic, C; Rubin, J; Brady, K; Allen, H; Talanian, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5184-5190 , 文章类型: Article,,卷期:2010年20-17]
- Succinic acid amides have been found to be effective P2-P3 scaffold replacements for peptidic ICE inhibitors. Heteroarylalkyl fragments occupying the P4 position provided access to compounds with nM affinities. Utilizati...
- Synthesis and in vitro antibacterial activity of novel fluoroquinolone derivatives containing substituted piperidines
[作者:Chai, Y; Liu, ML; Wang, B; You, XF; Feng, LS; Zhang, YB; Cao, J; Guo, HY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5195-5198 , 文章类型: Article,,卷期:2010年20-17]
- We report herein the synthesis of novel 7-(4-alkoxyimino-3-aminomethyl-3-methylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and correlated with ...
- Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities
[作者:Giraud, F; Marchand, P; Carbonnelle, D; Sartor, M; Lang, F; Duflos, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5203-5206 , 文章类型: Article,,卷期:2010年20-17]
- N-Aryl-3-(indol-3-yl)propanamides were synthesized and their immunosuppressive activities were evaluated. This study highlighted the promising potency of 3-[1-(4-chlorobenzyl)-1H-indol-3-yl]-N-(4-nitrophenyl) propanamide...
- Total synthesis and biological evaluation of tambjamine K and a library of unnatural analogs
[作者:Aldrich, LN; Stoops, SL; Crews, BC; Marnett, LJ; Lindsley, CW,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5207-5211 , 文章类型: Article,,卷期:2010年20-17]
- Herein we disclose the first total synthesis of tambjamine K and a library of unnatural analogs. Unnatural analogs were shown to be more potent in viability, proliferation, and invasion assays than the natural product in...
- Design and synthesis of HCV agents with sequential triple inhibitory potentials
[作者:Zhu, TM; Fawzi, MB; Flint, M; Kong, FM; Szeliga, J; Tsao, R; Howe, AYM; Pan, WT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5212-5216 , 文章类型: Article,,卷期:2010年20-17]
- The union of HCV-796, a potent selective HCV NS5B polymerase inhibitor, and Ribavirin, a molecule with activities against a wide spectrum of viruses, resulted in a class of new anti-HCV agents with a sequential triple in...
- X-ray crystal structure of JNK2 complexed with the p38 alpha inhibitor BIRB796: Insights into the rational design of DFG-out binding MAP kinase inhibitors
[作者:Kuglstatter, A; Ghate, M; Tsing, S; Villasenor, AG; Shaw, D; Barnett, JW; Browner, MF,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5217-5220 , 文章类型: Article,,卷期:2010年20-17]
- JNK2 and p38 alpha are closely related mitogen-activated protein kinases that regulate various cellular activities and are considered drug targets for inflammatory diseases. We have determined the X-ray crystal structure...
- Synthesis and SAR of (piperazin-1-yl-phenyl)-arylsulfonamides: A novel series of atypical antipsychotic agents
[作者:Park, CM; Kim, SY; Park, WK; Choi, JH; Seong, CM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:5221-5224 , 文章类型: Article,,卷期:2010年20-17]
- (Piperazin-1-yl-phenyl)-arylsulfonamides were synthesized and identified to show high affinities for both 5-HT2C and 5-HT6 receptors. Among them, naphthalene-2-sulfonic acid isopropyl-[3-(4-methyl-piperazin- 1-yl)-phenyl...
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