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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   Dual binding site inhibitors of B-RAF kinase [作者：Wolin, RL; Bembenek, SD; Wei, J; Crawford, S; Lundeen, K; Brunmark, A; Karlsson, L; Edwards, JP; Blevitt, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2825-2829 , 文章类型： Article，,卷期：2008年18-9] Computer aided modeling guided the design of a series of diarylimidazole compounds (11-22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the func... Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands [作者：Worm, K; Zhou, QJ; Saeui, CT; Green, RC; Cassel, JA; Stabley, GJ; DeHaven, RN; Conway-James, N; LaBuda, CJ; Koblish, M; Little, PJ; Dolle, RE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2830-2835 , 文章类型： Article，,卷期：2008年18-9] Sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Starting from a screening hit 8 that had modest affinity for the cannabinoid CB2 receptor, a parallel synthesis approach and initial... The isolation, structure determination and cytotoxicity of the new fungal metabolite, trichodermamide C [作者：Davis, RA; Longden, J; Avery, VM; Healy, PC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2836-2839 , 文章类型： Article，,卷期：2008年18-9] Chemical investigations of a culture broth from the endophytic fungus Eupenicillium sp. afforded the new modified dipeptide trichodermamide C 1. The structure of 1 was established following the analysis of NMR, UV, IR, M... Discovery of a novel submicromolar inhibitor of the lymphoid specific tyrosine phosphatase [作者：Xie, YL; Liu, YD; Gong, GL; Rinderspacher, A; Deng, SX; Smith, DH; Toebben, U; Tzilianos, E; Branden, L; Vidovic, D; Chung, C; Schurer, S; Tautz, L; Landry, DW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2840-2844 , 文章类型： Article，,卷期：2008年18-9] We report here a class of thiazolidine-2,4-diones and 2-thioxothiazolidin-4-ones as potent inhibitors of the lymphoid specific tyrosine phosphatase (Lyp) identified from high throughput screens. Chemical modi. cation by ... Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties [作者：Corte, JR; Fang, T; Pinto, DJP; Han, W; Hu, ZL; Jiang, XJ; Li, YL; Gauuan, JF; Hadden, M; Orton, D; Rendina, AR; Luettgen, JM; Wong, PC; He, K; Morin, PE; Chang, CH; Cheney, DL; Knabb, RM; Wexler, RR; Lam, PYS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2845-2849 , 文章类型： Article，,卷期：2008年18-9] Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable e... Synthesis and PKC theta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles [作者：Boschelli, DH; Wu, BQ; Sosa, ACB; Chen, J; Asselin, M; Cole, DC; Lee, J; Yang, XK; Chaudhary, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2850-2853 , 文章类型： Article，,卷期：2008年18-9] The thieno[2,3-b]pyridine-5-carbonitrile with a 5-indolylamine at C-4 and a phenyl group at C-2 had a moderate activity against PKC theta. Optimization of the groups at C-4 and C-2 led to analog 29, which has an IC50 val... QSAR study of mosquito repellents from terpenoid with a six-member-ring [作者：Wang, ZD; Song, J; Chen, JZ; Song, ZQ; Shang, SB; Jiang, ZK; Han, ZJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2854-2859 , 文章类型： Article，,卷期：2008年18-9] A new class of low-toxicity mosquito repellents is synthesized from alpha- and beta-pinene in terpenoid compounds and preliminary biological tests show promising mosquito repellency. Statistical modeling is built using C... 2-aminomethyl piperidines as novel urotensin-II receptor antagonists [作者：Jin, J; Wang, YH; Wang, F; Shi, DC; Erhard, KF; Wu, ZN; Guida, BF; Lawrence, SK; Behm, DJ; Disa, J; Vaidya, KS; Evans, C; McMillan, LJ; Rivero, RA; Neeb, MJ; Douglas, SA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2860-2864 , 文章类型： Article，,卷期：2008年18-9] A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the iden... Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif [作者：Kreutter, KD; Lu, TB; Lee, L; Giardino, EC; Patel, S; Huang, H; Xu, GZ; Fitzgerald, M; Haertlein, BJ; Mohan, V; Crysler, C; Eisennagel, S; Dasgupta, M; McMillan, M; Spurlino, JC; Huebert, ND; Maryanoff, BE; Tomczuk, BE; Damiano, BP; Player, MR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2865-2870 , 文章类型： Article，,卷期：2008年18-9] 2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated in 14, which is a potent thrombin inhibitor (K-i = 1.2 nM) th... Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides [作者：Moreno-Diaz, H; Villalobos-Molina, R; Ortiz-Andrade, R; Diaz-Coutino, D; Medina-Franco, JL; Webster, SP; Binnie, M; Estrada-Soto, S; Ibarra-Barajas, M; Leon-Rivera, I; Navarrete-Vazquez, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2871-2877 , 文章类型： Article，,卷期：2008年18-9] N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1-8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds s... Farnesyl pyrophosphate synthase enantiospecificity with a chiral risedronate analog, [6,7-dihydro-5H-cyclopenta[c]pyridin-7yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501): Synthetic, structural, and modeling studies [作者：Deprele, S; Kashemirov, BA; Hogan, JM; Ebetino, FH; Barnett, BL; Evdokimov, A; McKenna, CE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2878-2882 , 文章类型： Article，,卷期：2008年18-9] The complex formed from crystallization of human farnesyl pyrophosphate synthase (hFPPS) from a solution of racemic [ 6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501,8), a chiral... Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB [作者：Mallari, JP; Shelat, A; Kosinski, A; Caffrey, CR; Connelly, M; Zhu, FY; McKerrow, JH; Guy, RK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2883-2885 , 文章类型： Article，,卷期：2008年18-9] Human African trypanosomiasis ( HAT) is caused by the protozoan parasite Trypanosoma brucei. The cysteine proteases of T. brucei have been shown to be crucial for parasite replication and represent an attractive point fo... Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin [作者：Tomishima, M; Ohki, H; Yamada, A; Maki, K; Ikeda, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2886-2890 , 文章类型： Article，,卷期：2008年18-9] Further optimization of the potent antifungal activity of side chain analogs of the natural product FR901379 led to the discovery of compound 8 with an excellent, well-balanced pro. le. Potent compounds with reduced hemo... A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series [作者：De Luca, L; Barreca, ML; Ferro, S; Iraci, N; Michiels, M; Christ, F; Debyser, Z; Witvrouw, M; Chimirri, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2891-2895 , 文章类型： Article，,卷期：2008年18-9] We report herein the development of a new three-dimensional pharmacophore model for HIV-1 integrase inhibitors which led to the discovery of some 4-[1-(4-fluorobenzyl)-1H-indol-3-yl]-2-hydroxy-4-oxobut-2-enoic acids that... Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity [作者：Whitlock, GA; Fish, PV; Fray, MJ; Stobie, A; Wakenhut, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2896-2899 , 文章类型： Article，,卷期：2008年18-9] A novel series of pyridyl-phenyl ethers are disclosed, which possess dual 5-HT and NA reuptake pharmacology with good selectivity over dopamine reuptake inhibition. An analysis of the relationship between lipophilicity a... Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives [作者：Park, H; Min, K; Kwak, HS; Koo, KD; Lim, D; Seo, SW; Choi, JU; Platt, B; Choi, DY,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2900-2904 , 文章类型： Article，,卷期：2008年18-9] We describe synthesis and evaluation of a series of cyclic urea derivatives with hydroxylethylamine isostere. Modi. cation of P3, P1, and P2' and combination of SAR display a > 100-fold increase in potency with good cell...