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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50条记录   Antagonists of the human adenosine A(2A) receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives [作者：Gillespie, RJ; Cliffe, IA; Dawson, CE; Dourish, CT; Gaur, S; Giles, PR; Jordan, AM; Knight, AR; Lawrence, A; Lerpiniere, J; Misra, A; Pratt, RM; Todd, RS; Upton, R; Weiss, SM; Williamson, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2920-2923 , 文章类型： Article，,卷期：2008年18-9] We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the hum... Antagonists of the human adenosine A(2A) receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d] pyrimidines and 6-arylpurines [作者：Gillespie, RJ; Cliffe, IA; Dawson, CE; Dourish, CT; Gaur, S; Jordan, AM; Knight, AR; Lerpiniere, J; Misra, A; Pratt, RM; Roffey, J; Stratton, GC; Upton, R; Weiss, SM; Williamson, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2924-2929 , 文章类型： Article，,卷期：2008年18-9] A series of pyrazolo[3,4-d]pyrimidine, pyrrolo[2,3-d]pyrimidine and 6-arylpurine adenosine A(2A) antagonists is described. Many examples were highly selective against the human A(1) receptor sub-type and were active in a... Antagonists of the human adenosine A(2A) receptor. Part 1: Discovery and synthesis of thieno[3,2-d] pyrimidine-4-methanone derivatives [作者：Gillespie, RJ; Adams, DR; Bebbington, D; Benwell, K; Cliffe, IA; Dawson, CE; Dourish, CT; Fletcher, A; Gaur, S; Giles, PR; Jordan, AM; Knight, AR; Knutsen, LJS; Lawrence, A; Lerpiniere, J; Misra, A; Porter, RHP; Pratt, RM; Shepherd, R; Upton, R; Ward, SE; Weiss, SM; Williamson, DS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2916-2919 , 文章类型： Article，,卷期：2008年18-9] The (-)-(11R,2'S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A(2A) receptor antagonist. Further investigation of this compound has led to th... Novel 2-imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists [作者：Whitlock, GA; Conlon, K; McMurray, G; Roberts, LR; Stobie, A; Thurlow, RJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2930-2934 , 文章类型： Article，,卷期：2008年18-9] Novel 2-imidazoles have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Sulfonamide 23 possessed attr... Discovery of amino-acetonitrile derivatives, a new class of synthetic anthelmintic compounds [作者：Ducray, P; Gauvry, N; Pautrat, F; Goebel, T; Fruechtel, J; Desaules, Y; Weber, SS; Bouvier, J; Wagner, T; Froelich, O; Kaminsky, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2935-2938 , 文章类型： Article，,卷期：2008年18-9] A new series of amino-acetonitrile derivatives (AAD) have been discovered that exhibit high anthelmintic activity against parasitic nematode species such as Haemonchus contortus and Trichostrongylus colubriformis. Signif... Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity [作者：Honda, T; Tajima, H; Kaneko, Y; Ban, M; Inaba, T; Takeno, Y; Okamoto, K; Aono, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2939-2943 , 文章类型： Article，,卷期：2008年18-9] We found 4-pyridylmethylthio derivative 1 to be very effective in using antiangiogenesis activity to prevent proliferation of HUVECs (Human Umbilical Vein Endothelial Cells), which was induced by vascular endothelial gro... N-acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines [作者：Amorelli, B; Yang, CH; Rempel, B; Withers, SG; Knapp, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2944-2947 , 文章类型： Article，,卷期：2008年18-9] Several C-1 homologated GlcNAc-and GalNAc-thiazolines, as well as a related GalNAc-thiazole, have been prepared. The compounds are analogues of GlcNAc-thiazoline, a potent transition-state-mimicking inhibitor of retainin... Design, synthesis and evaluation of 2-phenyl-1H-benzo[d]imidazole-4,7-diones as vascular smooth muscle cell proliferation inhibitors [作者：Ryu, CK; Lee, RY; Lee, SY; Chung, HJ; Lee, SK; Chung, KH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2948-2951 , 文章类型： Article，,卷期：2008年18-9] A series of 2-phenyl-1H-benzo[d]imidazole-4,7-diones were synthesized and tested for their inhibitory activity on the PDGF-stimulated proliferation of rat aortic vascular smooth muscle cells. Among the tested compounds, ... New targeting system for antimycotic drugs: beta-Glucosidase sensitive Amphotericin B-star poly(ethylene glycol) conjugate [作者：Sedlak, M; Drabina, P; Bilkova, E; Simunek, P; Buchta, V,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2952-2956 , 文章类型： Article，,卷期：2008年18-9] A new targeting potentially intravenous conjugate Amphotericin B (AMB)-star poly(ethylene glycol) (sPEG) (M = 25,160) has been synthesized and characterized. It contains a beta-D-glucopyranoside molecular switch which is... Synthesis of gemcitabine triphosphate (dFdCTP) as a tris(triethylammonium) salt [作者：Risbood, PA; Kane, CT; Hossain, MT; Vadapalli, S; Chadda, SK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2957-2958 , 文章类型： Article，,卷期：2008年18-9] First synthesis of gemcitabine triphosphate (dFdCTP) as a tris(triethylammonium) salt is reported. Published by Elsevier Ltd. The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations [作者：Tucker, TJ; Saggar, S; Sisko, JT; Tynebor, RM; Williams, TM; Felock, PJ; Flynn, JA; Lai, MT; Liang, YX; McGaughey, G; Liu, MQ; Miller, M; Moyer, G; Munshi, V; Perlow-Poehnelt, R; Prasad, S; Sanchez, R; Torrent, M; Vacca, JP; Wan, BL; Yan, YW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2959-2966 , 文章类型： Article，,卷期：2008年18-9] Using a combination of traditional Medicinal Chemistry/SAR analysis, crystallography, and molecular modeling, we have designed and synthesized a series of novel, highly potent NNRTIs that possess broad antiviral activity... Selective androgen receptor modulators based on a series of 7H-[1,4] oxazino[3,2-g]quinolin-7-ones with improved in vivo activity [作者：Long, YO; Higuchi, RI; Caferro, TR; Lau, TLS; Wu, M; Cummings, ML; Martinborough, EA; Marschke, KB; Chang, WY; Lopez, FJ; Karanewsky, DS; Zhi, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2967-2971 , 文章类型： Article，,卷期：2008年18-9] Modification on a lead series of [1,4] oxazino[3,2-g] quinolin-7-ones at the 2-position led to selective androgen receptor modulators with improved in vivo activity. The most potent analog (-)-33a exhibited full maintena... Diphenidol-related diamines as novel muscarinic M-4 receptor antagonists [作者：Varoli, L; Andreani, A; Burnelli, S; Granaiola, M; Leoni, A; Locatelli, A; Morigi, R; Rambaldi, M; Bedini, A; Fazio, N; Spampinato, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2972-2976 , 文章类型： Article，,卷期：2008年18-9] A series of hydrochloride derivatives 2a-9a and quaternary ammonium derivatives 3b-9b of diphenidol have been synthesized and characterized in receptor binding and cellular functional assays versus human muscarinic M-1-M... A novel pyrene-guanidiniocarbonyl-pyrrole cation efficiently differentiates between ds-DNA and ds-RNA by two independent, sensitive spectroscopic methods [作者：Hernandez-Folgado, L; Schmuck, C; Tomic, S; Piantanida, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2977-2981 , 文章类型： Article，,卷期：2008年18-9] At micromolar concentrations and equimolar conditions in respect to basepairs, a novel pyrene-guanidiniocarbonyl-pyrrole cation 1 exhibited a strong ICD signal at about lambda = 300 nm specifically upon the interaction w... Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[ 2,3-b] pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor [作者：Ruel, R; Thibeault, C; L'Heureux, A; Martel, A; Cai, ZW; Wei, D; Qian, LG; Barrish, JC; Mathur, A; D'Arienzo, C; Hunt, JT; Kamath, A; Marathe, P; Zhang, YP; Derbin, G; Wautlet, B; Mortillo, S; Jeyaseelan, R; Henley, B; Tejwani, R; Bhide, RS; Trainor, GL; Fargnoli, J; Lombardo, LJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2985-2989 , 文章类型： Article，,卷期：2008年18-9] We report herein a series of substituted N-(1H-pyrrolo[2,3-b] pyridin-5-yl) pyrrolo[2,1-f][1,2,4] triazin-4-amines as inhibitors of vascular endothelial growth factor receptor-2 tyrosine kinase. Through structure-activit... Fragment-based discovery of hepatitis C virus NS5b RNA polymerase inhibitors [作者：Antonysamy, SS; Aubol, B; Blaney, J; Browner, MF; Giannetti, AM; Harris, SF; Hebert, N; Hendle, J; Hopkins, S; Jefferson, E; Kissinger, C; Leveque, V; Marciano, D; McGee, E; Najera, I; Nolan, B; Tomimoto, M; Torres, E; Wright, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2990-2995 , 文章类型： Article，,卷期：2008年18-9] Non-nucleoside inhibitors of HCV NS5b RNA polymerase were discovered by a fragment-based lead discovery approach, beginning with crystallographic fragment screening. The NS5b binding affinity and biochemical activity of ...