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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32条记录   Design, Synthesis, and Biological Evaluation of 3,4-Dihydroquinolin-2(1H)-one and 1,2,3,4-Tetrahydroquinoline-Based Selective Human Neuronal Nitric Oxide Synthase (nNOS) Inhibitors [作者：RAMNAUTH JAILALL; SPEED JOANNE; MADDAFORD SHAWN P; DOVE PETER; ANNEDI SUBHASH C; RENTON PAUL; RAKHIT SUMAN; ANDREWS JOHN; SILVERMAN SARAH; MLADENOVA GABRIELA; ZINGHINI SALVATORE; NAIR SHEELA; CATALANO CONCETTINA; LEE DAVID K H; DE FELICE MILENA; PORRECA FRANK,期刊：Journal of Medicinal Chemistry, 页码：5562-5575 , 文章类型： Article，,卷期：2011年54-15] Neuronal nitric oxide synthase (nNOS) inhibitors are effective in preclinical models of many neurological disorders. In this study, two related series of compounds, 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroqui... In Vivo PET Imaging of Histone Deacetylases by (18)F-Suberoylanilide Hydroxamic Acid ((18)F-SAHA) [作者：HENDRICKS J ADAM; KELIHER EDMUND J; MARINELLI BRETT; REINER THOMAS; WEISSLEDER RALPH; MAZITSCHEK RALPH,期刊：Journal of Medicinal Chemistry, 页码：5576-5582 , 文章类型： Article，,卷期：2011年54-15] Histone deacetylases (HDACs) are a group of enzymes that modulate gene expression and cell state by deacetylation of both histone and non-histone proteins. A variety of HDAC inhibitors (HDACi) have already undergone clin... Novel Benzoxazine and Benzothiazine Derivatives as Multifunctional Antihyperlipidemic Agents [作者：MATRALIS ALEXIOS N; KATSELOU MARIA G; NIKITAKIS ANASTASIOS; KOUROUNAKIS ANGELIKI P,期刊：Journal of Medicinal Chemistry, 页码：5583-5591 , 文章类型： Article，,卷期：2011年54-15] Atherosclerosis is a multifactorial disease with several mechanisms participating in its manifestation. To address this disorder, we applied a strategy involving the design of a single chemical compound able to simultane... Fragment-Based Drug Design and Drug Repositioning Using Multiple Ligand Simultaneous Docking (MLSD): Identifying Celecoxib and Template Compounds as Novel Inhibitors of Signal Transducer and Activator of Transcription 3 (STAT3) [作者：LI HUAMENG; LIU AIGUO; ZHAO ZHENJIANG; XU YUFANG; LIN JIAYUH; JOU DAVID; LI CHENGLONG,期刊：Journal of Medicinal Chemistry, 页码：5592-5596 , 文章类型： Article，,卷期：2011年54-15] We describe a novel method of drug discovery using MLSD and drug repositioning with cancer target STAT3 being used as a test case. Multiple drug scaffolds were simultaneously docked into hot spots of STAT3 by MLSD, follo... Preliminary Finding on a New Calcium Channel Entry Blocker Chemotype: 5,6-Diamino-4-hydroxy-2-mercaptopyrimidine Derivatives [作者：COSIMELLI BARBARA; SEVERI ELDA; NOVELLINO ETTORE; CAVACCINI ANNA; CATALDI MAURO; BUDRIESI ROBERTA; MICUCCI MATTEO; CHIARINI ALBERTO; IOAN PIERFRANCO,期刊：Journal of Medicinal Chemistry, 页码：5597-5601 , 文章类型： Article，,卷期：2011年54-15] We report the preliminary in vitro characterization of a series of pyrimidines as a new chemotype that modulates cardiovascular parameters and relaxes ileum smooth muscle according to classical calcium entry blockers. Te... Important Role of Oxidative Stress Biomarkers in Huntington's Disease [作者：TUNEZ ISAAC; SANCHEZLOPEZ FERNANDO; AGUEERA EDUARDO; FERNANDEZBOLANOS RICARDO; MANUEL SANCHEZ FRANCISCO; TASSETCUEVAN INMACULADA,期刊：Journal of Medicinal Chemistry, 页码：5602-5606 , 文章类型： Article，,卷期：2011年54-15] This study examined global oxidative stress (GOS) and antioxidant system and their correlation with disease stage in 19 patients with HD. The results revealed an increase in oxidative stress biomarkers and a reduction in... Utilization of Halogen Bond in Lead Optimization: A Case Study of Rational Design of Potent Phosphodiesterase Type 5 (PDE5) Inhibitors [作者：XU ZHIJIAN; LIU ZHENG; CHEN TONG; CHEN TIANTIAN; WANG ZHEN; TIAN GUANGHUI; SHI JING; WANG XUELAN; LU YUNXIANG; YAN XIUHUA; WANG GUAN; JIANG HUALIANG; CHEN KAIXIAN; WANG SHUDONG; XU YECHUN; SHEN JINGSHAN; ZHU WEILIANG,期刊：Journal of Medicinal Chemistry, 页码：5607-5611 , 文章类型： Article，,卷期：2011年54-15] For proof-of-concept of halogen bonding in drug design, a series of halogenated compounds were designed based on a lead structure as new inhibitors of phosphodiesterase type S. Bioassay results revealed a good correlatio... The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: Addressing the "Core Issue" in the Design of Estrogen Receptor Ligands [作者：KATZENELLENBOGEN JOHN A,期刊：Journal of Medicinal Chemistry, 页码：5271-5282 , 文章类型： Article，,卷期：2011年54-15] Synthesis and Pharmacological Characterization of Bicyclic Triple Reuptake Inhibitor 3-Aryl Octahydrocyclopenta[c]pyrrole Analogues [作者：SHAO LIMING; HEWITT MICHAEL C; MALCOLM SCOTT C; WANG FENGJIANG; MA JIANGUO; CAMPBELL UNA C; SPICER NANCY A; ENGEL SHARON R; HARDY LARRY W; JIANG ZHIDONG; SCHREIBER RUDY; SPEAR KERRY L; VARNEY MARK A,期刊：Journal of Medicinal Chemistry, 页码：5283-5295 , 文章类型： Article，,卷期：2011年54-15] The present work expands the chemical space known to offer potent inhibition of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) and discloses novel bicyclic octahydrocyc... Antimalarial Activity of Natural and Synthetic Prodiginines [作者：PAPIREDDY KANCHARLA; SMILKSTEIN MARTIN; KELLY JANE XU; SHWETA; SALEM SHAIMAA M; ALHAMADSHEH MAMOUN; HAYNES STUART W; CHALLIS GREGORY L; REYNOLDS KEVIN A,期刊：Journal of Medicinal Chemistry, 页码：5296-5306 , 文章类型： Article，,卷期：2011年54-15] Prodiginines are a family of linear and cyclic oligopyrrole red-pigmented compounds. Herein we describe the in vitro antimalarial activity of four natural (IC(50) = 1.7-8.0 nM) and three sets of synthetic prodiginines ag... Conformationally Constrained Peptides from CD2 To Modulate Protein-Protein Interactions between CD2 and CD58 [作者：GOKHALE AMEYA; WELDEGHIORGHIS THOMAS K; TANEJA VEENA; SATYANARAYANAJOIS SEETHARAMA D,期刊：Journal of Medicinal Chemistry, 页码：5307-5319 , 文章类型： Article，,卷期：2011年54-15] Cell adhesion molecule CD2 and its ligand CDS8 provide good examples of protein protein interactions in cells that participate in the immune response. To modulate the cell adhesion interaction, peptides were designed fro... Tryptophan 2,3-Dioxygenase (TDO) Inhibitors. 3-(2-(Pyridyl)ethenyl)indoles as Potential Anticancer Immunomodulators [作者：DOLUSIC EDUARD; LARRIEU PIERRE; MOINEAUX LAURENCE; STROOBANT VINCENT; PILOTTE LUC; COLAU DIDIER; POCHET LIONEL; VAN DEN EYNDE BENOIT; MASEREEL BERNARD; WOUTERS JOHAN; FREDERICK RAPHAEL,期刊：Journal of Medicinal Chemistry, 页码：5320-5334 , 文章类型： Article，,卷期：2011年54-15] Tryptophan catabolism mediated by indoleamine 2,3-dioxygenase (IDO) is an important mechanism of peripheral immune tolerance contributing to tumoral immune resistance. IDO inhibition is thus an active area of research in... Targeting HIV Entry through Interaction with Envelope Glycoprotein 120 (gp120): Synthesis and Antiviral Evaluation of 1,3,5-Triazines with Aromatic Amino Acids [作者：LOZANO VIRGINIA; AGUADO LEIRE; HOORELBEKE BART; RENDERS MARLEEN; CAMARASA MARIAJOSE; SCHOLS DOMINIQUE; BALZARINI JAN; SANFELIX ANA; PEREZPEREZ MARIAJESUS,期刊：Journal of Medicinal Chemistry, 页码：5335-5348 , 文章类型： Article，,卷期：2011年54-15] On the basis of the interesting inhibitory properties that lectins show against HIV-replication through their interaction with glycoprotein 120 (gp120), we here describe the design, synthesis, and anti-HIV evaluation of ... Modulation of GABA(A)-Receptors by Honokiol and Derivatives: Subtype Selectivity and Structure-Activity Relationship [作者：TAFERNER BARBARA; SCHUEHLY WOLFGANG; HUEFNER ANTJE; BABURIN IGOR; WIESNER KATHARINA; ECKER GERHARD F; HERING STEFFEN,期刊：Journal of Medicinal Chemistry, 页码：5349-5361 , 文章类型： Article，,卷期：2011年54-15] A series of 31 analogues of the neolignan honokiol (a major constituent of Magnolia officinalis) was synthesized, and their effects on GABA(A) receptors expressed in Xenopus oocytes were investigated. Honokiol enhanced c... Synthesis and in Vitro Biological Evaluation of Carbonyl Group-Containing Analogues for sigma(1) Receptors [作者：WANG WEI; CUI JINQUAN; LU XIAOXIA; PADAKANTI PRASHANTH K; XU JINBIN; PARSONS STANLEY M; LUEDTKE ROBERT R; RATH NIGAM P; TU ZHUDE,期刊：Journal of Medicinal Chemistry, 页码：5362-5372 , 文章类型： Article，,卷期：2011年54-15] To identify the ligands for sigma(1) receptors that are potent and selective, analogues of prezamicol and trozamicol scaffolds of carbonyl-containing vesicular acetylcholine transporter (VAChT) inhibitors were explored. ... Polysulfated Xanthones: Multipathway Development of a New Generation of Dual Anticoagulant/Antiplatelet Agents [作者：CORREIADASILVA MARTA; SOUSA EMILIA; DUARTE BARBARA; MARQUES FRANKLIM; CARVALHO FELIX; CUNHARIBEIRO LUIS M; PINTO MADALENA M M,期刊：Journal of Medicinal Chemistry, 页码：5373-5384 , 文章类型： Article，,卷期：2011年54-15] A multipathway strategy was used to evaluate the in vitro and in vivo antithrombotic effects of a new synthetic family of sulfated small molecules. Polysulfated xanthonosides showed highly effective anticoagulation effec...