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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96条记录   Carbonic anhydrase inhibitors: Thioxolone versus sulfonamides for obtaining isozyme-selective inhibitors? [作者：Innocenti, A; Maresca, A; Scozzafava, A; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3938-3941 , 文章类型： Article，,卷期：2008年18-14] Inhibition of 13 mammalian isoforms of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), CA I-XV, with thioxolone (6-hydroxy-1,3-benzoxathiol-2-one) and two sulfonamides was investigated. Thioxolone was inefficient ... Identification of novel inhibitors of methionyl-tRNA synthetase (MetRS) by virtual screening [作者：Finn, J; Stidham, M; Hilgers, M; Kedar, GC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3932-3937 , 文章类型： Article，,卷期：2008年18-14] Multiple inhibitors of the antibacterial target, Staphylococcus aureus MetRS, were identified by virtual screening. The process consisted of building a Catalyst (R) pharmacophore from a ligand-S. aureus MetRS structure a... Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase [作者：Menear, KA; Adcock, C; Alonso, FC; Blackburn, K; Copsey, L; Drzewiecki, J; Fundo, A; Le Gall, A; Gomez, S; Javaid, H; Lence, CF; Martin, NMB; Mydlowski, C; Smith, GCM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3942-3945 , 文章类型： Article，,卷期：2008年18-14] We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed ... Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A(2A) receptor antagonists [作者：Shah, U; Lankin, CM; Boyle, CD; Chackalamannil, S; Greenlee, WJ; Neustadt, BR; Cohen-Williams, ME; Higgins, GA; Ng, K; Varty, GB; Zhang, HT; Lachowicz, JE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4204-4209 , 文章类型： Article，,卷期：2008年18-14] SCH 58261 is a reported adenosine A(2A) receptor antagonist which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A(1) receptor and does not demo... Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors [作者：Verissimo, E; Berry, N; Gibbons, P; Cristiano, MLS; Rosenthal, PJ; Gut, J; Ward, SA; O'Neill, PM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4210-4214 , 文章类型： Article，,卷期：2008年18-14] The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Mic... Synthesis and screening of small molecule inhibitors of anthrax edema factor [作者：Jimenez, ME; Bush, K; Pawlik, J; Sower, L; Peterson, JW; Gilbertson, SR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4215-4218 , 文章类型： Article，,卷期：2008年18-14] The synthesis and development of a novel class of molecules that inhibit anthrax edema factor, an adenylyl cyclase, is reported. These molecules are derived from the initial discovery that histidine and imidazole adducts... Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034 [作者：Bogen, S; Arasappan, A; Pan, W; Ruan, S; Padilla, A; Saksena, AK; Girijavallabhan, V; Njoroge, FG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4219-4223 , 文章类型： Article，,卷期：2008年18-14] Substitutions on the P-1 cyclobutyl side chain of SCH 503034 were studied by introduction of hydroxyl and fluoro substituents. Additionally, effects of. uoro substitution on other P1 moieties were evaluated. (C) 2008 Els... Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI) [作者：Wu, DP; Pontillo, J; Ching, B; Hudson, S; Gao, YH; Fleck, BA; Gogas, K; Wade, WS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4224-4227 , 文章类型： Article，,卷期：2008年18-14] The design, synthesis, and SAR of a series of ring-constrained norepinephrine reuptake inhibitors are described. A substantially rigid inhibitor with potent functional activity at the transporter (IC50 = 8 nM) was used t... Urotensin-II receptor antagonists: Synthesis and SAR of N-cyclic azaalkyl benzamides [作者：Jin, J; An, M; Sapienza, A; Aiyar, N; Naselsky, D; Sarau, HM; Foley, JJ; Salyers, KL; Knight, SD; Keenan, RM; Rivero, RA; Dhanak, D; Douglas, SA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3950-3954 , 文章类型： Article，,卷期：2008年18-14] SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with ... Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent [作者：Zhu, GD; Gandhi, VB; Gong, JC; Thomas, S; Luo, Y; Liu, XS; Shi, Y; Klinghofer, V; Johnson, EF; Frost, D; Donawho, C; Jarvis, K; Bouska, J; Marsh, KC; Rosenberg, SH; Giranda, VL; Penning, TD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3955-3958 , 文章类型： Article，,卷期：2008年18-14] Poly(ADP-ribose) polymerases (PARPs) play significant roles in various cellular functions including DNA repair and control of RNA transcription. PARP inhibitors have been demonstrated to potentiate the effect of cytotoxi... Discovery of selective and nonpeptidic cathepsin S inhibitors [作者：Irie, O; Ehara, T; Iwasaki, A; Yokokawa, F; Sakaki, J; Hirao, H; Kanazawa, T; Teno, N; Horiuchi, M; Umemura, I; Gunji, H; Masuya, K; Hitomi, Y; Iwasaki, G; Nonomura, K; Tanabe, K; Fukaya, H; Kosaka, T; Snell, CR; Hallett, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3959-3962 , 文章类型： Article，,卷期：2008年18-14] Nonpeptidic, selective, and potent cathepsin S inhibitors were derived from an in-house pyrrolopyrimidine cathepsin K inhibitor by modi. cation of the P2 and P3 moieties. The pyrrolopyrimidine-based inhibitors show nanom... Natural products in parallel synthesis: Triazole libraries of nonactic acid [作者：Luesse, SB; Wells, G; Nayek, A; Smith, AE; Kusche, BR; Bergmeier, SC; McMills, MC; Priestley, ND; Wright, DL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3946-3949 , 文章类型： Article，,卷期：2008年18-14] The synthesis of a library of nonactic acid-derived triazoloamide derivatives and their evaluation as antimicrobial agents is described. (C) 2008 Elsevier Ltd. All rights reserved. Discovery of a novel series of Notch-sparing gamma-secretase inhibitors [作者：Kreft, A; Harrison, B; Aschmies, S; Atchison, K; Casebier, D; Cole, DC; Diamantidis, G; Ellingboe, J; Hauze, D; Hu, Y; Huryn, D; Jin, M; Kubrak, D; Lu, PM; Lundquist, J; Mann, C; Martone, R; Moore, W; Oganesian, A; Porte, A; Riddell, DR; Sonnenberg-Reines, J; Stock, JR; Sun, SC; Wagner, E; Woller, K; Xu, Z; Zhou, H; Jacobsen, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4232-4236 , 文章类型： Article，,卷期：2008年18-14] Using a cell-based assay, we have identified a new series of Notch-sparing gamma-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved gamma-se... Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors [作者：Hamblin, JN; Angell, TDR; Ballantine, SP; Cook, CM; Cooper, AWJ; Dawson, J; Delves, CJ; Jones, PS; Lindvall, M; Lucas, FS; Mitchell, CJ; Neu, MY; Ranshaw, LE; Solanke, YE; Somers, DO; Wiseman, JO,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4237-4241 , 文章类型： Article，,卷期：2008年18-14] Optimisation of a high-throughput screening hit resulted in the discovery of 4-(substituted amino)-1-alkyl-pyrazolo[3,4-b]pyridine-5-carboxamides as potent and selective inhibitors of Phosphodiesterase 4 (PDE4). Herein, ... Spiroleptosphol isolated from Leptosphaeria doliolum [作者：Hashimoto, M; Tsushima, T; Murakami, T; Nomiya, M; Takada, N; Tanaka, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4228-4231 , 文章类型： Article，,卷期：2008年18-14] A novel gamma-methylidene-spirobutanolide spirolephtoshol (1) was isolated from ascomycetous fungus Leptosphaeria doliolum as a cytotoxic compound. The relative structure was established by the NMR analysis involving the... Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors [作者：Janetka, JW; Almeida, L; Ashwell, S; Brassil, PJ; Daly, K; Deng, C; Gero, T; Glynn, RE; Horn, CL; Ioannidis, S; Lyne, P; Newcombe, NJ; Oza, VB; Pass, M; Springer, SK; Su, M; Toader, D; Vasbinder, MM; Yu, DW; Yu, Y; Zabludoff, SD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4242-4248 , 文章类型： Article，,卷期：2008年18-14] Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this...