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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44条记录   Carbamate Derivatives of Indolines as Cholinesterase Inhibitors and Antioxidants for the Treatment of Alzheimer's Disease [作者：YANOVSKY INESSA; FINKINGRONER EFRAT; ZAIKIN ANDREY; LERMAN LENA; SHALOM HILA; ZEELI SHANI; WEILL TEHILLA; GINSBURG ISAAC; NUDELMAN ABRAHAM; WEINSTOCK MARTA,期刊：Journal of Medicinal Chemistry, 页码：10700-10715 , 文章类型： Article，,卷期：2012年55-23] The cascade of events that occurs in Alzheimer's disease involving oxidative stress and the reduction in cholinergic transmission can be better addressed by multifunctional drugs than cholinesterase inhibitors alone. For... Investigating the Role of T-7 and T-12 Residues on the Biological Properties of Thrombin-Binding Aptamer: Enhancement of Anticoagulant Activity by a Single Nucleobase Modification [作者：BORBONE NICOLA; BUCCI MARIAROSARIA; OLIVIERO GIORGIA; MORELLI ELENA; AMATO JUSSARA; DATRI VALENTINA; DERRICO STEFANO; VELLECCO VALENTINA; CIRINO GIUSEPPE; PICCIALLI GENNARO; FATTORUSSO CATERINA; VARRA MICHELA; MAYOL LUCIANO; PERSICO MARCO; SCUOTTO MARIA,期刊：Journal of Medicinal Chemistry, 页码：10716-10728 , 文章类型： Article，,卷期：2012年55-23] An acyclic pyrimidine analogue, containing a five-member cycle fused on the pyrimidine ring, was synthesized and introduced at position 7 or 12 of the 15-mer oligodeoxynucleotide GGTTGGTGTGGTTGG, known as thrombin-bindin... Design of a Novel Cyclotide-Based CXCR4 Antagonist with Anti-Human Immunodeficiency Virus (HIV)-1 Activity [作者：ABOYE TESHOME L; HA HELEN; MAJUMDER SUBHABRATA; CHRIST FRAUKE; DEBYSER ZEGER; SHEKHTMAN ALEXANDER; NEAMATI NOURI; CAMARERO JULIO A,期刊：Journal of Medicinal Chemistry, 页码：10729-10734 , 文章类型： Article，,卷期：2012年55-23] Herein, we report for the first time the design and synthesis of a novel cyclotide able to efficiently inhibit HIV-1 viral replication by selectively targeting cytokine receptor CXCR4. This was accomplished by grafting a... An Anthraquinone Scaffold for Putative, Two-Face Bim BH3 alpha-Helix Mimic [作者：ZHANG ZHICHAO; LI XIANGQIAN; SONG TING; ZHAO YAN; FENG YINGANG,期刊：Journal of Medicinal Chemistry, 页码：10735-10741 , 文章类型： Article，,卷期：2012年55-23] Bim BH3 peptide features an alpha-helix with hotspot residues on multiple faces. Compound 5 (6-bromo-2,3-dihydroxyanthracene-9,10-dione), which adopts a rigid-plan amphipathic conformation, was designed and evaluated as ... DNA Cloning, Characterization, and Inhibition Studies of an alpha-Carbonic Anhydrase from the Pathogenic Bacterium Vibrio cholerae [作者：DEL PRETE SONIA; ISIK SEMRA; VULLO DANIELA; DE LUCA VIVIANA; CARGINALE VINCENZO; SCOZZAFAVA ANDREA; SUPURAN CLAUDIU T; CAPASSO CLEMENTE,期刊：Journal of Medicinal Chemistry, 页码：10742-10748 , 文章类型： Article，,卷期：2012年55-23] We have cloned, purified, and characterized an alpha-carbonic anhydrase (CA, EC 4.2.1.1) from the human pathogenic bacterium Vibrio cholerae, VchCA. The new enzyme has significant catalytic activity, and an inhibition st... Cyanobacterial Peptides as a Prototype for the Design of Potent beta-Secretase Inhibitors and the Development of Selective Chemical Probes for Other Aspartic Proteases [作者：LIU YANXIA; ZHANG WEI; LI LI; SALVADOR LILIBETH A; CHEN TIANTIAN; CHEN WUYAN; FELSENSTEIN KEVIN M; LADD THOMAS B; PRICE ASHLEIGH R; GOLDE TODD E; HE JIANHUA; XU YECHUN; LI YINGXIA; LUESCH HENDRIK,期刊：Journal of Medicinal Chemistry, 页码：10749-10765 , 文章类型： Article，,卷期：2012年55-23] Inspired by marine cyanobacterial natural products, we synthesized modified peptides with a central statine-core unit, characteristic for aspartic protease inhibition. A series of tasiamide B analogues inhibited BACE1, a... Property-Based Optimization of Hydroxamate-Based gamma-Lactam HDAC Inhibitors to Improve Their Metabolic Stability and Pharmacokinetic Profiles [作者：CHOI EUNHYUN; LEE CHULHO; CHO MISUN; SEO JEONG JEA; YANG JEE SUN; OH SOO JIN; LEE KIHO; PARK SONGKYU; KIM HWAN MOOK; KWON HO JEONG; HAN GYOONHEE,期刊：Journal of Medicinal Chemistry, 页码：10766-10770 , 文章类型： Article，,卷期：2012年55-23] Hydroxamate-based HDAC inhibitors have promising anticancer activities but metabolic instability and poor pharmacokinetics leading to poor in vivo results. QSAR and PK studies of HDAC inhibitors showed that a gamma-lacta... Design and Synthesis of Dual Modulators of Soluble Epoxide Hydrolase and Peroxisome Proliferator-Activated Receptors [作者：BUSCATO ESTELLA; BLOECHER RENE; LAMERS CHRISTINA; KLINGLER FRANCAMARIA; HAHN STEFFEN; STEINHILBER DIETER; SCHUBERTZSILAVECZ MANFRED; PROSCHAK EWGENIJ,期刊：Journal of Medicinal Chemistry, 页码：10771-10775 , 文章类型： Article，,卷期：2012年55-23] Metabolic syndrome is a complex condition which often requires the use of multiple medications as a treatment. The resulting problems of polypharmacy are increase in side effects, drug-drug interactions, and its high eco... Investigating the Effects of a Hydrolytically Stable Hapten and a Th1 Adjuvant on Heroin Vaccine Performance [作者：BREMER PAUL T; JANDA KIM D,期刊：Journal of Medicinal Chemistry, 页码：10776-10780 , 文章类型： Article，,卷期：2012年55-23] We challenged the performance of our previous heroin vaccine with a similar vaccine containing a more hydrolytically stable hapten analogue and a Th1 adjuvant (CpG ODN). Our results indicate that the elements of our prev... Bacterial Reduction as Means for Colonic Drug Delivery: Can Other Chemical Groups Provide an Alternative to the Azo Bond? [作者：SAPHIER SIGAL; HAFT AVITAL; MARGEL SHLOMO,期刊：Journal of Medicinal Chemistry, 页码：10781-10785 , 文章类型： Article，,卷期：2012年55-23] We compared the rate of colonic bacterial reduction of disulfide and nitro bonds to that of an azo counterpart. The disulfide and nitro reduction rates are comparable to that of azo having a similar molecular structure. ... Rapid Protein-Ligand Costructures from Sparse NOE Data [作者：SHAH DIPEN M; AB EISO; DIERCKS TAMMO; HASS MATHIAS A S; VAN NULAND NICO A J; SIEGAL GREGG,期刊：Journal of Medicinal Chemistry, 页码：10786-10790 , 文章类型： Article，,卷期：2012年55-23] An efficient way to rapidly generate protein-ligand costructures based on solution-NMR using sparse NOE data combined with selective isotope labeling is presented. A docked model of the 27 kDa N-terminal ATPase domain of... Phenyltetrahydroisoquinoline-Pyridinaldoxime Conjugates as Efficient Uncharged Reactivators for the Dephosphylation of Inhibited Human Acetylcholinesterase [作者：MERCEY GUILLAUME; RENOU JULIEN; VERDELET TRISTAN; KIACHYNA MARIA; BAATI RACHID; GILOR EMILIE; ARBOLEAS MELANIE; LOIODICE MELANIE; NACHON FLORIAN; JEAN LUDOVIC; RENARD PIERREYVES,期刊：Journal of Medicinal Chemistry, 页码：10791-10795 , 文章类型： Article，,卷期：2012年55-23] Pyridinium and bis-pyridinium aldoximes are used as antidotes to reactivate acetylcholinesterase (AChE) inhibited by organophosphorus nerve agents. Herein, we described a series of nine nonquaternary phenyltetrahydroisoq...