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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85条记录   Novel CXCR3 antagonists with a piperazinyl-piperidine core [作者：McGuinness, BF; Carroll, CD; Zawacki, LG; Dong, GZ; Yang, CM; Hobbs, DW; Jacob-Samuel, B; Hall, JW; Jenh, CH; Kozlowski, JA; Anilkumar, GN; Rosenblum, SB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5205-5208 , 文章类型： Article，,卷期：2009年19-17] High-throughput screening of an encoded combinatorial aryl piperazine library led to the identification of a novel series of potent piperazinyl-piperidine based CXCR3 antagonists. Analogs of the initial hit were synthesi... Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: Discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one [作者：Hughes, RO; Walker, JK; Rogier, DJ; Heasley, SE; Blevis-Bal, RM; Benson, AG; Jacobsen, EJ; Cubbage, JW; Fobian, YM; Owen, DR; Freskos, JN; Molyneaux, JM; Brown, DL; Acker, BA; Maddux, TM; Tollefson, MB; Moon, JB; Mischke, BV; Rumsey, JM; Zheng, Y; MacInnes, A; Bond, BR; Yu, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5209-5213 , 文章类型： Article，,卷期：2009年19-17] We describe efforts to improve the pharmacokinetic profile of the aminopyridopyrazinone class of PDE5 inhibitors. These efforts led to the discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-... Thiazole analog as stearoyl-CoA desaturase 1 inhibitor [作者：Li, CS; Belair, L; Guay, J; Murgasva, R; Sturkenboom, W; Ramtohul, YK; Zhang, L; Huang, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5214-5217 , 文章类型： Article，,卷期：2009年19-17] SCD1 inhibition may represent a novel treatment for obesity, type-2 diabetes and related metabolic disorders. A prototype thiazole amide analog 13 (MF-152) was identified as an excellent tool in the study of SCD biology ... Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists [作者：Zhu, ZN; Sun, ZY; Ye, YZ; McKittrick, B; Greenlee, W; Czarniecki, M; Fawzi, A; Zhang, HT; Lachowicz, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5218-5221 , 文章类型： Article，,卷期：2009年19-17] A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an ... Protein-DNA photo-crosslinking with a genetically encoded benzophenone-containing amino acid [作者：Lee, HS; Dimla, RD; Schultz, PG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5222-5224 , 文章类型： Article，,卷期：2009年19-17] The photo-crosslinking amino acid, p-benzoyl-L-phenylalanine (pBpa), was genetically incorporated into Escherichia coli catabolite activator protein (CAP) in bacteria in response to an amber nonsense codon using an ortho... Benzo[c][2,7]naphthyridines as inhibitors of PDK-1 [作者：Kim, KH; Wissner, A; Floyd, MB; Fraser, HL; Wang, YD; Dushin, RG; Hu, YB; Olland, A; Guo, B; Arndt, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5225-5228 , 文章类型： Article，,卷期：2009年19-17] A series of substituted benzo[c][2,7]-naphthyridines were prepared and showed good potency in inhibiting PDK-1. The synthesis and SAR of this series of compounds are presented as well as the X-ray crystal structure of on... Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition [作者：Ryu, YB; Curtis-Long, MJ; Lee, JW; Ryu, HW; Kim, JY; Lee, WS; Park, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4912-4915 , 文章类型： Article，,卷期：2009年19-17] The structural characteristics of. avonoids (1-3 and 6-8) from the root of Cudrania tricuspidata required for neuraminidase inhibition were studied and compared with commercially available. avonoids (4, 5, and 9-12). Alk... 2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2 ',3 ':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists [作者：Wang, YH; Duraiswami, C; Madauss, KP; Tran, TB; Williams, SP; Deng, SJ; Graybill, TL; Hammond, M; Jones, DG; Grygielko, ET; Bray, JD; Thompson, SK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4916-4919 , 文章类型： Article，,卷期：2009年19-17] High throughput screening of the corporate compound collection led to the identification of a novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as ... Substituted 3-(4-(1,3,5-triazin-2-yl)-phenyl)-2-aminopropanoic acids as novel tryptophan hydroxylase inhibitors [作者：Jin, HH; Cianchetta, G; Devasagayaraj, A; Gu, KJ; Marinelli, B; Samal, L; Scott, S; Stouch, T; Tunoori, A; Wang, Y; Zang, Y; Zhang, CM; Kimball, SD; Main, AJ; Ding, ZM; Sun, WM; Yang, Q; Yu, XQ; Powell, DR; Wilson, A; Liu, Q; Shi, ZC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5229-5232 , 文章类型： Article，,卷期：2009年19-17] Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. As a neurotransmitter, serotonin plays important physiological roles both peripherally and centrally. Here we describe the discovery of substitu... N-substituted bis-C-alkyloxadiazolones as dual effectors: Efficient intermediates to amidoximes or amidines and prodrug candidates of potent antimalarials [作者：Degardin, M; Wein, S; Durand, T; Escale, R; Vial, H; Vo-Hoang, Y,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5233-5236 , 文章类型： Article，,卷期：2009年19-17] A convenient route to N-substituted bis-C-alkylamidines possessing antiplasmodial activity and their oxadiazolone and amidoxime prodrug candidates, is described. These three families of compounds were available after a k... Studies towards topical selective beta(2)-adrenoceptor agonists with a long duration of action [作者：Bouyssou, T; Rudolf, K; Hoenke, C; Lustenberger, P; Schnapp, A; Konetzki, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5237-5240 , 文章类型： Article，,卷期：2009年19-17] beta(2)-Adrenoceptor agonists with basic and acidic groups attached via an alkyl linker to the phenyl ethanolamine core were prepared and investigated in vitro and in vivo. The compounds exhibited a high potency in a fun... Click chemistry based rapid one-pot synthesis and evaluation for protease inhibition of new tetracyclic triazole fused benzodiazepine derivatives [作者：Mohapatra, DK; Maity, PK; Shabab, M; Khan, MI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5241-5245 , 文章类型： Article，,卷期：2009年19-17] We describe herein a one-pot synthesis of novel tetracyclic scaffolds that incorporate a fusion of a proline, 1,2,3-triazole ring with [1,4]-benzodiazepin-8(4H)-one ring systems following click chemistry. The expected pe... Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors [作者：Truong, AP; Aubele, DL; Probst, GD; Neitzel, ML; Semko, CM; Bowers, S; Dressen, D; Hom, RK; Konradi, AW; Sham, HL; Garofalo, AW; Keim, PS; Wu, J; Dappen, MS; Wong, K; Goldbach, E; Quinn, KP; Sauer, JM; Brigham, EF; Wallace, W; Nguyen, L; Hemphill, SS; Bova, MP; Basi, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4920-4923 , 文章类型： Article，,卷期：2009年19-17] In this Letter, we report our strategy to design potent and metabolically stable gamma-secretase inhibitors that are efficacious in reducing the cortical A beta x-40 levels in FVB mice via a single PO dose. (C) 2009 Else... Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells [作者：Allen, JG; Lee, MR; Han, CYE; Scherrer, J; Flynn, S; Boucher, C; Zhao, HL; O'Connor, AB; Roveto, P; Bauer, D; Graceffa, R; Richards, WG; Babij, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4924-4928 , 文章类型： Article，,卷期：2009年19-17] A screening campaign of a diverse collection of similar to 250,000 small molecule compounds was performed to identify inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with potential osteogenic activity in osteoblast c... Carbonic anhydrase inhibitors. Inhibition of the Rv1284 and Rv3273 beta-carbonic anhydrases from Mycobacterium tuberculosis with diazenylbenzenesulfonamides [作者：Maresca, A; Carta, F; Vullo, D; Scozzafava, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4929-4932 , 文章类型： Article，,卷期：2009年19-17] A series of diazenylbenzenesulfonamides obtained from sulfanilamide or metanilamide by diazotization followed by coupling with phenols or amines, was tested for the inhibition of the beta-carbonic anhydrases (CAs, EC 4.2... Synthesis and antibacterial activity of 7-(1,2,3,4-tetrahydropyrrolo[1,2-a]-pyrazin-7-yl) quinolones [作者：Zhu, B; Marinelli, BA; Goldschmidt, R; Foleno, BD; Hilliard, JJ; Bush, K; Macielag, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4933-4936 , 文章类型： Article，,卷期：2009年19-17] A novel series of 7-(1,2,3,4-tetrahydropyrrolo[1,2-a]-pyrazin-7-yl) quinolones has been designed and synthesized in which the heterocyclic side chain is attached to the quinolone core through a carbon-carbon linkage. The...