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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   Four Lessons from Global Health Drug Discovery: Medicine for an Ailing Industry? [作者：ELLIOTT RICHARD L,期刊：ACS Medicinal Chemistry Letters, 页码：688-690 , 文章类型： Editorial Material，,卷期：2012年3-9] In recent years, the pharmaceutical industry has faced many challenges to its business model, undergoing tremendous change and turmoil to survive. Are there any lessons to be drawn from drug discovery focused on Global H... Bromodomains: Are Readers Right for Epigenetic Therapy? [作者：CONWAY STUART J,期刊：ACS Medicinal Chemistry Letters, 页码：691-694 , 文章类型： Editorial Material，,卷期：2012年3-9] There is intense interest in the development of small molecule inhibitors of the acetyl-lysine-reading bromodomain protein module. These inhibitors represent a way of interfering therapeutically in epigenetic processes, ... Substituted Pyridines as Sodium Channel Blockers [作者：BLASS BENJAMIN,期刊：ACS Medicinal Chemistry Letters, 页码：695-696 , 文章类型： Editorial Material，,卷期：2012年3-9] Cyclopropyl-spiro-piperidines Useful as Sodium Channel Blockers [作者：BLASS BENJAMIN,期刊：ACS Medicinal Chemistry Letters, 页码：697-698 , 文章类型： Editorial Material，,卷期：2012年3-9] Hepatitis C Virus Protease Inhibitors [作者：ABDELMAGID AHMED F,期刊：ACS Medicinal Chemistry Letters, 页码：699-700 , 文章类型： Editorial Material，,卷期：2012年3-9] Inhibitors of LRRK2 as Treatment for Parkinson's Disease [作者：ABDELMAGID AHMED F,期刊：ACS Medicinal Chemistry Letters, 页码：701-702 , 文章类型： Editorial Material，,卷期：2012年3-9] Prostaglandin E-2 Synthase-1 Inhibitors as Potential Treatment for Osteoarthritis [作者：ABDELMAGID AHMED F,期刊：ACS Medicinal Chemistry Letters, 页码：703-704 , 文章类型： Editorial Material，,卷期：2012年3-9] Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors [作者：WANG TAO; LAMB MICHELLE L; BLOCK MICHAEL H; DAVIES AUDREY MOLINA; HAN YONGXIN; HOFFMANN ETHAN; IOANNIDIS STEPHANOS; JOSEY JOHN A; LIU ZHONGYING; LYNE PAUL D; MACINTYRE TERRY; MOHR PETER J; OMER CHARLES A; SJOGREN TOVE; THRESS KENNETH; WANG BIN; WANG HAIYUN; YU DINGWEI; ZHANGT HAIJUN,期刊：ACS Medicinal Chemistry Letters, 页码：705-709 , 文章类型： Article，,卷期：2012年3-9] Trk receptor tyrosine kinases have been implicated in cancer and pain. A crystal structure of TrkA with AZ-23 (1a) was obtained, and scaffold hopping resulted in two 5/6-bicyclic series comprising either imidazo[4,5-b]py... Design, Synthesis, and Testing of a Molecular Truck for Colonic Delivery of 5-Aminosalicylic Acid [作者：NAVATH SURYAKIRAN; RAO VENKATARAMANARAO; WOODFORD RITAMARIE T; MIDURAKIELA MONICA T; AHAD ALI M; ALLETI RAMESH; KIELA PAWEL R; MASH EUGENE A,期刊：ACS Medicinal Chemistry Letters, 页码：710-714 , 文章类型： Article，,卷期：2012年3-9] A molecular scaffold bearing eight terminal alkyne groups was synthesized from sucrose. Eight copies of an azide-terminated, azo-linked precursor to 5-aminosalicylic acid were attached to the scaffold via copper(I)-catal... Structure-Activity Relationships and Molecular Modeling of 1,2,4-Triazoles as Adenosine Receptor Antagonists [作者：CARLSSON JENS; TOSH DILIP K; PHAN KHAI; GAO ZHANGUO; JACOBSON KENNETH A,期刊：ACS Medicinal Chemistry Letters, 页码：715-720 , 文章类型： Article，,卷期：2012年3-9] The structure-activity relationship (SAR) for a novel class of 1,2,4-triazole antagonists of the human A(2A) adenosine receptor (hA(2A)AR) was explored. Thirty-three analogs of a ligand that was discovered in a structure... From in Silico Discovery to Intracellular Activity: Targeting JNK-Protein Interactions with Small Molecules [作者：KAOUD TAMER S; YAN CHUNLI; MITRA SHREYA; TSENG CHUNCHIA; JOSE JINEY; TALIAFERRO JULIANA M; TUOHETAHUNTILA MAIDINA; DEVKOTA ASHWINI; SAMMONS RACHEL; PARK JIHYUN; PARK HEEKWANG; SHI YUE; HONG JIYONG; REN PENGYU; DALBY KEVIN N,期刊：ACS Medicinal Chemistry Letters, 页码：721-725 , 文章类型： Article，,卷期：2012年3-9] The JNK-JIPI interaction represents an attractive target for the selective inhibition of JNK-mediated signaling. We report a virtual screening (VS) workflow, based on a combination of three-dimensional shape and electros... Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist [作者：BROWN SEAN P; DRANSFIELD PAUL J; VIMOLRATANA MARC; JIAO XIANYUN; ZHU LIUSHENG; PATTAROPONG VATEE; SUN YING; LIU JINQIAN; LUO JIAN; ZHANG JANE; WONG SIMON; ZHUANG RUN; GUO QI; LI FRANK; MEDINA JULIO C; SWAMINATH GAYATHRI; LIN DANIEL C H; HOUZE JONATHAN B,期刊：ACS Medicinal Chemistry Letters, 页码：726-730 , 文章类型： Article，,卷期：2012年3-9] GPR40 (FFA1) is a G-protein-coupled receptor, primarily expressed in pancreatic islets, the activation of which elicits increased insulin secretion only in the presence of elevated glucose levels. A potent, orally bioava... Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease [作者：PRIME MICHAEL E; BROOKFIELD FREDERICK A; COURTNEY STEPHEN M; GAINES SIMON; MARSTON RICHARD W; ICHIHARA OSAMU; LI MARIE; VAIDYA DARSHAN; WILLIAMS HELEN; PEDRETDUNN ANNA; REED LAURA; SCHAERTL SABINE; TOLEDOSHERMAN LETICIA; BECONI MARIA; MACDONALD DOUGLAS; MUNOZSANJUAN IGNACIO; DOMINGUEZ CELIA; WITYAK JOHN,期刊：ACS Medicinal Chemistry Letters, 页码：731-735 , 文章类型： Article，,卷期：2012年3-9] A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure activity relationship of this new series and report on the transglutaminas... Quinolinyl Pyrimidines: Potent Inhibitors of NDH-2 as a Novel Class of Anti-TB Agents [作者：SHIRUDE PRAVIN S; PAUL BEENA; CHOUDHURY NILANJANA ROY; KEDARI CHAITANYA; BANDODKAR BALACHANDRA; UGARKAR BHEEMARAO G,期刊：ACS Medicinal Chemistry Letters, 页码：736-740 , 文章类型： Article，,卷期：2012年3-9] NDH-2 is an essential respiratory enzyme in Mycobacterium tuberculosis (Mtb), which plays an important role in the physiology of Mtb. Herein, we present a target-based effort to identify a new structural class of inhibit... Crystal Structure and Specific Binding Mode of Sisomicin to the Bacterial Ribosomal Decoding Site [作者：KONDO JIRO; KOGANEI MAI; KASAHARA TOMOKO,期刊：ACS Medicinal Chemistry Letters, 页码：741-744 , 文章类型： Article，,卷期：2012年3-9] Sisomicin with an unsaturated sugar ring I displays better antibacterial activity than other structurally related aminoglycosides, such as gentamicin, tobramycin, and amikacin. In the present study, we have confirmed by ... Synthesis and Biological Evaluation of a Biotinylated Paclitaxel with an Extra-Long Chain Spacer Arm [作者：LIS LEV G; SMART MARY A; LUCHNIAK ANNA; GUPTA MOHAN L JR; GURVICH VADIM J,期刊：ACS Medicinal Chemistry Letters, 页码：745-748 , 文章类型： Article，,卷期：2012年3-9] A biotinylated paclitaxel derivative with an extra-long chain (LC-LC-biotin) spacer arm was synthesized using an improved synthetic reaction sequence. The biotinylated paclitaxel analogue retained excellent microtubule s...