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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71条记录   Structure-based lead identification of ATP-competitive MK2 inhibitors [作者：Barf, T; Kaptein, A; de Wilde, S; van der Heijden, R; van Someren, R; Demont, D; Schultz-Fademrecht, C; Versteegh, J; van Zeeland, M; Seegers, N; Kazemier, B; van de Kar, B; van Hoek, M; de Roos, J; Klop, H; Smeets, R; Hofstra, C; Hornberg, J; Oubrie, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3818-3822 , 文章类型： Article，,卷期：2011年21-12] MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray crystallography and structure-based drug design. The lead ha... Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors [作者：Kaptein, A; Oubrie, A; de Zwart, E; Hoogenboom, N; de Wit, J; van de Kar, B; van Hoek, M; Vogel, G; de Kimpe, V; Schultz-Fademrecht, C; Borsboom, J; van Zeeland, M; Versteegh, J; Kazemier, B; de Roos, J; Wijnands, F; Dulos, J; Jaeger, M; Leandro-Garcia, P; Barf, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3823-3827 , 文章类型： Article，,卷期：2011年21-12] The identification of a potent, selective, and orally available MK2 inhibitor series is described. The initial absence of oral bioavailability was successfully tackled by moving the basic nitrogen of the spiro-4-piperidy... Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties [作者：Oost, T; Backfisch, G; Bhowmik, S; van Gaalen, MM; Geneste, H; Hornberger, W; Lubisch, W; Netz, A; Unger, L; Wernet, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3828-3831 , 文章类型： Article，,卷期：2011年21-12] Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole... Macrolactin W, a new antibacterial macrolide from a marine Bacillus sp. [作者：Mondol, MAM; Kim, JH; Lee, HS; Lee, YJ; Shin, HJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3832-3835 , 文章类型： Article，,卷期：2011年21-12] Bioactivity-guided isolation for the new/novel metabolites from the EtOAc extract obtained from the culture broth of a marine Bacillus sp. 09ID194 followed by chromatographic fractionations and subsequently HPLC purifica... Synthesis and in vitro antitubercular activity of ferrocene-based hydrazones (vol 21, pg 2866, 2011) [作者：Mahajan, A; Kremer, L; Louw, S; Guerardel, Y; Chibale, K; Biot, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3836-3836 , 文章类型： Correction，,卷期：2011年21-12] Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs (vol 20, pg 3737, 2010) [作者：Wagner, G; Weber, C; Nyeki, O; Nogradi, K; Bielik, A; Molnar, L; Bobok, A; Horvath, A; Kiss, B; Kolok, S; Nagy, J; Kurko, D; Gal, K; Greiner, I; Szombathelyi, Z; Keseru, GM; Domany, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3837-3838 , 文章类型： Correction，,卷期：2011年21-12] Structure-based virtual screening approach to the discovery of phosphoinositide 3-kinase alpha inhibitors (vol 21, pg 2021, 2011) [作者：Park, H; Choi, H; Hong, S; Kim, D; Oh, DS; Hong, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3839-3839 , 文章类型： Correction，,卷期：2011年21-12]