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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22条记录   Macrocyclic Peptoid-Peptide Hybrids as Inhibitors of Class I Histone Deacetylases [作者：OLSEN CHRISTIAN A; MONTERO ANA; LEMAN LUKE J; GHADIRI M REZA,期刊：ACS Medicinal Chemistry Letters, 页码：749-753 , 文章类型： Article，,卷期：2012年3-9] We report the design, synthesis, and biological evaluation of the first macrocyclic peptoid-containing histone deacetylase (HDAC) inhibitors. The compounds selectively inhibit human class I HDAC isoforms in vitro, with n... Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor [作者：NAKAMURA YUJI; FUJIMOTO TEPPEI; OGAWA YASUYUKI; SUGITA CHIE; MIYAZAKI SHOJIRO; TAMAKI KAZUHIKO; TAKAHASHI MIZUKI; MATSUI YUMI; NAGAYAMA TAKAHIRO; MANABE KENICHI; MIZUNO MAKOTO; MASUBUCHI NORIKO; CHIBA KATSUYOSHI; NISHI TAKAHIDE,期刊：ACS Medicinal Chemistry Letters, 页码：754-758 , 文章类型： Article，,卷期：2012年3-9] A novel orally bioavailable renin inhibitor, DS-8108b (5), showing potent renin inhibitory activity and excellent in vivo efficacy is described. We report herein the synthesis and pharmacological effects of 5 including r... Substrate-Selective Inhibition of Cyclooxygenase-2: Development and Evaluation of Achiral Profen Probes [作者：WINDSOR MATTHEW A; HERMANSON DANIEL J; KINGSLEY PHILIP J; XU SHU; CREWS BRENDA C; HO WINNIE; KEENAN CATHERINE M; BANERJEE SURAJIT; SHARKEY KEITH A; MARNETT LAWRENCE J,期刊：ACS Medicinal Chemistry Letters, 页码：759-763 , 文章类型： Article，,卷期：2012年3-9] Cyclooxygenase-2 (COX-2) oxygenates arachidonic acid and the endocannabinoids 2-arachidonoylglycerol (2-AG) and arachidonoylethanolamide (AEA). We recently reported that (R)-profens selectively inhibit endocannabinoid ox... Identification of an Adamantyl Azaquinolone JNK Selective Inhibitor [作者：HAYNES NANCYELLEN; SCOTT NATHAN R; CHEN LI C; JANSON CHERYL A; LI JIA KUI; LUKACS CHRISTINE M; RAILKAR ARUNA; TOZZO EFFIE; WHITTARD TONI; BROWN NICHOLAS F; CHEUNG ADRIAN WAIHING,期刊：ACS Medicinal Chemistry Letters, 页码：764-768 , 文章类型： Article，,卷期：2012年3-9] 3-[4-((1S,2S,3R,5S,7S)-5-Hydroxyadamantan-2-ylcarbamoyl)benzyl]-4-oxo-1-phenyl-1,4-dihydro-[1,8]naphthyridine-2-carboxylic acid methyl ester (4) was identified as a novel, druglike and selective quinolone pan JNK inhibit... Symmetric Kv1.5 Blockers Discovered by Focused Screening [作者：BOSTROM JONAS,期刊：ACS Medicinal Chemistry Letters, 页码：769-773 , 文章类型： Article，,卷期：2012年3-9] Guided by computational methods, a set of 1920 compounds were selected from the AstraZeneca corporate collection and screened for Kv1.5 activity. To facilitate rapid generation of structure activity relationships, specia... Fluorescent Human EP3 Receptor Antagonists [作者：TOMASCH MIRIAM; SCHWED J STEPHAN; KUCZKA KARINA; DOS SANTOS SASCHA MEYER; HARDER SEBASTIAN; NUESING ROLF M; PAULKE ALEXANDER; STARK HOLGER,期刊：ACS Medicinal Chemistry Letters, 页码：774-779 , 文章类型： Article，,卷期：2012年3-9] Exchange of the lipophilc part of ortho-substituted cinnamic acid lead structures with different small molecule fluorophoric moieties via a dimethylene spacer resulted in hEP(3)R ligands with affinities in the nanomolar ...