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Medizinische Chemie - Neueste Forschungsartikel der Fachverlage

 
Aktuelle Fachartikel zur Medizinischen Chemie, sortiert nach Erscheinungsdatum.

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Journal of Medicinal Chemistry Journal of Medicinal Chemistry, Volume 51 Issue 17 (September 11, 2008) is now available Quelle: Journal of Medicinal Chemistry | 11 Sep 2008 | 6:00 am CEST

Genome-Wide Computational and Expression Analyses Reveal G-Quadruplex DNA Motifs as Conserved cis-Regulatory Elements in Human and Related Species Anjali Verma, Kangkan Halder, Rashi Halder, Vinod Kumar Yadav, Pooja Rawal, Ram Krishna Thakur, Farhan Mohd, Abhay Sharma, and Shantanu Chowdhury Web Release Date: Thu, 4 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800448a Quelle: Journal of Medicinal Chemistry | 4 Sep 2008 | 6:00 am CEST

Book Review of Annual Review of Pharmacology and Toxicology. Volume 48 Michael LaFontaine Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800677x Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Discovery and Evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an Orally Efficacious Inhibitor of Insulin-like Growth Factor-1 Receptor Kinase with Broad Spectrum in Vivo Antitumor Activity Upender Velaparthi, Mark Wittman, Peiying Liu, Joan M. Carboni, Francis Y. Lee, Ricardo Attar, Praveen Balimane, Wendy Clarke, Michael W. Sinz, Warren Hurlburt, Karishma Patel, Lorell Discenza, Sean Kim, Marco Gottardis, Ann Greer, Aixin Li, Mark Saulnier, Zheng Yang, Kurt Zimmermann, George Trainor, and Dolatrai Vyas Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800832q Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection Vincenzo Summa, Alessia Petrocchi, Fabio Bonelli, Benedetta Crescenzi, Monica Donghi, Marco Ferrara, Fabrizio Fiore, Cristina Gardelli, Odalys Gonzalez Paz, Daria J. Hazuda, Philip Jones, Olaf Kinzel, Ralph Laufer, Edith Monteagudo, Ester Muraglia, Emanuela Nizi, Federica Orvieto, Paola Pace, Giovanna Pescatore, Rita Scarpelli, Kara Stillmock, Marc V. Witmer, and Michael Rowley Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800245z Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Design, Synthesis, and Biological Evaluation of Potent c-Met Inhibitors Noel D. D’Angelo, Steven F. Bellon, Shon K. Booker, Yuan Cheng, Angela Coxon, Celia Dominguez, Ingrid Fellows, Douglas Hoffman, Randall Hungate, Paula Kaplan-Lefko, Matthew R. Lee, Chun Li, Longbin Liu, Elizabeth Rainbeau, Paul J. Reider, Karen Rex, Aaron Siegmund, Yaxiong Sun, Andrew S. Tasker, Ning Xi, Shimin Xu, Yajing Yang, Yihong Zhang, Teresa L. Burgess, Isabelle Dussault, and Tae-Seong Kim Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8006189 Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Targeting the Ribose and Phosphate Binding Site of p38 Mitogen-Activated Protein (MAP) Kinase: Synthesis and Biological Testing of 2-Alkylsulfanyl-, 4(5)-Aryl-, 5(4)-Heteroaryl-Substituted Imidazoles Pierre Koch, Christiane Bäuerlein, Hartmut Jank, and Stefan Laufer Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800373t Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Book Review of Biopharmaceutical Drug Design and Development. Second Edition Aliasger K. Salem Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm8009734 Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Novel Aldosterone Synthase Inhibitors with Extended Carbocyclic Skeleton by a Combined Ligand-Based and Structure-Based Drug Design Approach Simon Lucas, Ralf Heim, Matthias Negri, Iris Antes, Christina Ries, Katarzyna E. Schewe, Alessandra Bisi, Silvia Gobbi, and Rolf W. Hartmann Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800683c Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Synthesis and Antitumor Activity of Mechercharmycin A Analogues Delia Hernández, Marta Altuna, Carmen Cuevas, Rosa Aligué, Fernando Albericio, and Mercedes Álvarez Web Release Date: Wed, 3 Sep 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800513w Quelle: Journal of Medicinal Chemistry | 3 Sep 2008 | 6:00 am CEST

Adamantyl-Substituted Retinoid-Derived Molecules That Interact with the Orphan Nuclear Receptor Small Heterodimer Partner: Effects of Replacing the 1-Adamantyl or Hydroxyl Group on Inhibition of Cancer Cell Growth, Induction of Cancer Cell Apoptosis, and Inhibition of Src Homology 2 Domain-Containing Protein Tyrosine Phosphatase-2 Activity Marcia I. Dawson, Zebin Xia, Tao Jiang, Mao Ye, Joseph A. Fontana, Lulu Farhana, Bhaumik Patel, Li Ping Xue, Mohammad Bhuiyan, Roberto Pellicciari, Antonio Macchiarulo, Roberto Nuti, Xiao-Kun Zhang, Young-Hoon Han, Lutz Tautz, Peter D. Hobbs, Ling Jong, Nahid Waleh, Wan-ru Chao, Gen-Sheng Feng, Yuhong Pang, and Ying Su Web Release Date: Sat, 30 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800456k Quelle: Journal of Medicinal Chemistry | 30 Aug 2008 | 6:00 am CEST

Book Review of Drug-like Properties: Concepts, Structure Design, and Methods Thomas E. Prisinzano Web Release Date: Sat, 30 Aug 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm8009348 Quelle: Journal of Medicinal Chemistry | 30 Aug 2008 | 6:00 am CEST

The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer Adrian J. Folkes, Khatereh Ahmadi, Wendy K. Alderton, Sonia Alix, Stewart J. Baker, Gary Box, Irina S. Chuckowree, Paul A. Clarke, Paul Depledge, Suzanne A. Eccles, Lori S. Friedman, Angela Hayes, Timothy C. Hancox, Arumugam Kugendradas, Letitia Lensun, Pauline Moore, Alan G. Olivero, Jodie Pang, Sonal Patel, Giles H. Pergl-Wilson, Florence I. Raynaud, Anthony Robson, Nahid Saghir, Laurent Salphati, Sukhjit Sohal, Mark H. Ultsch, Melanie Valenti, Heidi J.A. Wallweber, Nan Chi Wan, Christian Wiesmann, Paul Workman, Alexander Zhyvoloup, Marketa J. Zvelebil, and Stephen J. Shuttleworth Web Release Date: Fri, 29 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800295d Quelle: Journal of Medicinal Chemistry | 29 Aug 2008 | 6:00 am CEST

Discovery of Orally Bioavailable Cathepsin S Inhibitors for the Reversal of Neuropathic Pain Osamu Irie, Takatoshi Kosaka, Takeru Ehara, Fumiaki Yokokawa, Takanori Kanazawa, Hajime Hirao, Astuko Iwasaki, Junichi Sakaki, Naoki Teno, Yuko Hitomi, Genji Iwasaki, Hiroaki Fukaya, Kazuhiko Nonomura, Keiko Tanabe, Shinichi Koizumi, Noriko Uchiyama, Stuart J. Bevan, Marzia Malcangio, Clive Gentry, Alyson J. Fox, Mohammed Yaqoob, Andrew J. Culshaw, and Allan Hallett Web Release Date: Fri, 29 Aug 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800839j Quelle: Journal of Medicinal Chemistry | 29 Aug 2008 | 6:00 am CEST

Oversulfated Chondroitin Sulfate: Impact of a Heparin Impurity, Associated with Adverse Clinical Events, on Low-Molecular-Weight Heparin Preparation Zhenqing Zhang, Michel Weïwer, Boyangzi Li, Melissa M. Kemp, Tyler H. Daman, and Robert J. Linhardt Web Release Date: Fri, 29 Aug 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800785t Quelle: Journal of Medicinal Chemistry | 29 Aug 2008 | 6:00 am CEST

Lipid-Lowering (Hetero)Aromatic Tetrahydro-1,4-Oxazine Derivatives with Antioxidant and Squalene Synthase Inhibitory Activity Angeliki P. Kourounakis, Christos Charitos, Eleni A. Rekka, and Panos N. Kourounakis Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800663w Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) Forms an Irreversible Bond To the Active Site of the GluR2 AMPA Receptor Leslie A. Cruz, Eva Estébanez-Perpiñá, Sam Pfaff, Sabine Borngraeber, Ning Bao, Justin Blethrow, Robert J. Fletterick, and Pamela M. England Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm701517b Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

Discovery of Novel and Cardioselective Diltiazem-like Calcium Channel Blockers via Virtual Screening Emanuele Carosati, Roberta Budriesi, Pierfranco Ioan, Maria P. Ugenti, Maria Frosini, Fabio Fusi, Gaetano Corda, Barbara Cosimelli, Domenico Spinelli, Alberto Chiarini, and Gabriele Cruciani Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800151n Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

Aminoacyl−Anthraquinone Conjugates as Telomerase Inhibitors: Synthesis, Biophysical and Biological Evaluation Giuseppe Zagotto, Claudia Sissi, Lorena Lucatello, Claudia Pivetta, Sergio A. Cadamuro, Keith R. Fox, Stephen Neidle, and Manlio Palumbo Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800160v Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

Discovery and Labeling of High-Affinity 3,4-Diarylpyrazolines as Candidate Radioligands for In Vivo Imaging of Cannabinoid Subtype-1 (CB1) Receptors Sean R. Donohue, Victor W. Pike, Sjoerd J. Finnema, Phong Truong, Jan Andersson, Balázs Gulyás, and Christer Halldin Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800329z Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

Molecular Engineering of Conotoxins: The Importance of Loop Size to α-Conotoxin Structure and Function Ai-Hua Jin, Norelle L. Daly, Simon T. Nevin, Ching-I A. Wang, Sebastien Dutertre, Richard J. Lewis, David J. Adams, David J. Craik, and Paul F. Alewood Web Release Date: Thu, 28 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800278k Quelle: Journal of Medicinal Chemistry | 28 Aug 2008 | 6:00 am CEST

3,4-Dihydro-2H-1,4-benzoxazine Derivatives Combining Thrombin Inhibitory and Glycoprotein IIb/IIIa Receptor Antagonistic Activity as a Novel Class of Antithrombotic Compounds with Dual Function Janez Ilaš, Žiga Jakopin, Tina Borštnar, Mojca Stegnar, and Danijel Kikelj Web Release Date: Wed, 27 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8003448 Quelle: Journal of Medicinal Chemistry | 27 Aug 2008 | 6:00 am CEST

Residues in the 11 Å Channel of Histone Deacetylase 1 Promote Catalytic Activity: Implications for Designing Isoform-Selective Histone Deacetylase Inhibitors Sujith V. W. Weerasinghe, Guillermina Estiu, Olaf Wiest, and Mary Kay H. Pflum Web Release Date: Wed, 27 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800081j Quelle: Journal of Medicinal Chemistry | 27 Aug 2008 | 6:00 am CEST

Potent Cationic Inhibitors of West Nile Virus NS2B/NS3 Protease With Serum Stability, Cell Permeability and Antiviral Activity Martin J. Stoermer, Keith J. Chappell, Susann Liebscher, Christina M. Jensen, Chun H. Gan, Praveer K. Gupta, Wei-Jun Xu, Paul R. Young, and David P. Fairlie Web Release Date: Tue, 26 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800503y Quelle: Journal of Medicinal Chemistry | 26 Aug 2008 | 6:00 am CEST

Anxiolytic-like Effects of N,N-Dialkyl-2-phenylindol-3-ylglyoxylamides by Modulation of Translocator Protein Promoting Neurosteroid Biosynthesis Federico Da Settimo, Francesca Simorini, Sabrina Taliani, Concettina La Motta, Anna Maria Marini, Silvia Salerno, Marusca Bellandi, Ettore Novellino, Giovanni Greco, Barbara Cosimelli, Eleonora Da Pozzo, Barbara Costa, Nicola Simola, Micaela Morelli, and Claudia Martini Web Release Date: Tue, 26 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8003224 Quelle: Journal of Medicinal Chemistry | 26 Aug 2008 | 6:00 am CEST

Inactivation of NF-κB Components by Covalent Binding of (−)-Dehydroxymethylepoxyquinomicin to Specific Cysteine Residues Mizuki Yamamoto, Ryouichi Horie, Masatoshi Takeiri, Ikuko Kozawa, and Kazuo Umezawa Web Release Date: Tue, 26 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8006245 Quelle: Journal of Medicinal Chemistry | 26 Aug 2008 | 6:00 am CEST

Synthesis and Biological Evaluation of 2-Amino-3-(4-Chlorobenzoyl)-4-[N-(Substituted) Piperazin-1-yl]Thiophenes as Potent Allosteric Enhancers of the A1 Adenosine Receptor Romeo Romagnoli, Pier Giovanni Baraldi, Maria Dora Carrion, Carlota Lopez Cara, Olga Cruz-Lopez, Maria Antonietta Iaconinoto, Delia Preti, John C. Shryock, Allan R. Moorman, Fabrizio Vincenzi, Katia Varani, and Pier Andrea Borea Web Release Date: Tue, 26 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800586p Quelle: Journal of Medicinal Chemistry | 26 Aug 2008 | 6:00 am CEST

Structure-Guided Design of N-Phenyl Tertiary Amines as Transrepression-Selective Liver X Receptor Modulators with Anti-Inflammatory Activity Esther Y. Chao, Justin A. Caravella, Mike A. Watson, Nino Campobasso, Serena Ghisletti, Andrew N. Billin, Cristin Galardi, Ping Wang, Bryan A. Laffitte, Marie A. Iannone, Bryan J. Goodwin, Jason A. Nichols, Derek J. Parks, Eugene Stewart, Robert W. Wiethe, Shawn P. Williams, Angela Smallwood, Kenneth H. Pearce, Christopher K. Glass, Timothy M. Willson, William J. Zuercher, and Jon L. Collins Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800612u Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Discovery of Potent and Selective Small-Molecule PAR-2 Agonists Jimmi Gerner Seitzberg, Anne Eeg Knapp, Birgitte Winther Lund, Sine Mandrup Bertozzi, Erika A. Currier, Jian-Nong Ma, Vladimir Sherbukhin, Ethan S. Burstein, and Roger Olsson Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm800754r Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Hunter−Killer Peptide (HKP) for Targeted Therapy H. Michael Ellerby, Dale E. Bredesen, Satoshi Fujimura, and Varghese John Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Perspective) DOI: 10.1021/jm800495u Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Potent Dual Thymidylate Synthase and Dihydrofolate Reductase Inhibitors: Classical and Nonclassical 2-Amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine Antifolates Aleem Gangjee, Yibin Qiu, Wei Li, and Roy L. Kisliuk Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8006933 Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

A β-Fluoroamine Inhibitor of Purine Nucleoside Phosphorylase Jennifer M. Mason, Andrew S. Murkin, Lei Li, Vern L. Schramm, Graeme J. Gainsford, and Brian W. Skelton Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800792b Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Melanocortin Tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 Modified at the Para Position of the Benzyl Side Chain (DPhe): Importance for Mouse Melanocortin-3 Receptor Agonist versus Antagonist Activity Bettina Proneth, Irina D. Pogozheva, Federico P. Portillo, Henry I. Mosberg, and Carrie Haskell-Luevano Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800291b Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor of AKT Kinase Dirk A. Heerding, Nelson Rhodes, Jack D. Leber, Tammy J. Clark, Richard M. Keenan, Louis V. Lafrance, Mei Li, Igor G. Safonov, Dennis T. Takata, Joseph W. Venslavsky, Dennis S. Yamashita, Anthony E. Choudhry, Robert A. Copeland, Zhihong Lai, Michael D. Schaber, Peter J. Tummino, Susan L. Strum, Edgar R. Wood, Derek R. Duckett, Derek Eberwein, Victoria B. Knick, Timothy J. Lansing, Randy T. McConnell, ShuYun Zhang, Elisabeth A. Minthorn, Nestor O. Concha, Gregory L. Warren, and Rakesh Kumar Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8004527 Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Enantiomeric Propanolamines as selective N-Methyl-D-aspartate 2B Receptor Antagonists Yesim A. Tahirovic, Matthew Geballe, Ewa Gruszecka-Kowalik, Scott J. Myers, Polina Lyuboslavsky, Phuong Le, Adam French, Hasan Irier, Woo-baeg Choi, Keith Easterling, Hongjie Yuan, Lawrence J. Wilson, Robert Kotloski, James O. McNamara, Raymond Dingledine, Dennis C. Liotta, Stephen F. Traynelis, and James P. Snyder Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8002153 Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Virtual Screening, Identification, and Biochemical Characterization of Novel Inhibitors of the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 Alon Herschhorn and Amnon Hizi Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800473d Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Synthesis and in Vitro Evaluation of 5-[18F]Fluoroalkyl Pyrimidine Nucleosides for Molecular Imaging of Herpes Simplex Virus Type 1 Thymidine Kinase Reporter Gene Expression Ann-Marie Chacko, Wenchao Qu, and Hank F. Kung Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800501d Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Optimizing Natural Products by Biosynthetic Engineering: Discovery of Nonquinone Hsp90 Inhibitors Ming-Qiang Zhang, Sabine Gaisser, Mohammad Nur-E-Alam, Lesley S. Sheehan, William A. Vousden, Nikolaos Gaitatzis, Gerrard Peck, Nigel J. Coates, Steven J. Moss, Markus Radzom, Teresa A. Foster, Rose M. Sheridan, Matthew A. Gregory, S. Mark Roe, Chrisostomos Prodromou, Laurence Pearl, Susan M. Boyd, Barrie Wilkinson, and Christine J. Martin Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Letter) DOI: 10.1021/jm8006068 Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Phosphoramidate Dinucleosides as Hepatitis C Virus Polymerase Inhibitors Ivan Zlatev, Hélène Dutartre, Ivan Barvik, Johan Neyts, Bruno Canard, Jean-Jacques Vasseur, Karine Alvarez, and François Morvan Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800617c Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Synthesis, Ex Vivo Evaluation, and Radiolabeling of Potent 1,5-Diphenylpyrrolidin-2-one Cannabinoid Subtype-1 Receptor Ligands as Candidates for In Vivo Imaging Sean R. Donohue, Joseph H. Krushinski, Victor W. Pike, Eyassu Chernet, Lee Phebus, Amy K. Chesterfield, Christian C. Felder, Christer Halldin, and John M. Schaus Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800416m Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Novel Opioid Peptide Derived Antagonists Containing (2S)-2-Methyl-3-(2,6-dimethyl-4-carbamoylphenyl)propanoic Acid [(2S)-Mdcp] Animesh Ghosh, Jie Luo, Chen Liu, Grazyna Weltrowska, Carole Lemieux, Nga N. Chung, Yixin Lu, and Peter W. Schiller Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm8004702 Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Structural Modifications of N-(1,2,3,4-Tetrahydronaphthalen-1-yl)-4-Aryl-1-piperazinehexanamides: Influence on Lipophilicity and 5-HT7 Receptor Activity. Part III Marcello Leopoldo, Enza Lacivita, Paola De Giorgio, Claudia Fracasso, Sara Guzzetti, Silvio Caccia, Marialessandra Contino, Nicola A. Colabufo, Francesco Berardi, and Roberto Perrone Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800615e Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Inhibition of Geranylgeranyl Diphosphate Synthase by Bisphosphonates: A Crystallographic and Computational Investigation Cammy K.-M. Chen, Michael P. Hudock, Yonghui Zhang, Rey-Ting Guo, Rong Cao, Joo Hwan No, Po-Huang Liang, Tzu-Ping Ko, Tao-Hsin Chang, Shiou-chi Chang, Yongcheng Song, Jordan Axelson, Anup Kumar, Andrew H.-J. Wang, and Eric Oldfield Web Release Date: Sat, 23 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800325y Quelle: Journal of Medicinal Chemistry | 23 Aug 2008 | 6:00 am CEST

Design, Synthesis, and Evaluation of Novel Organophosphorus Inhibitors of Bacterial Ureases Stamatia Vassiliou, Agnieszka Grabowiecka, Paulina Kosikowska, Athanasios Yiotakis, Paweł Kafarski, and Łukasz Berlicki Web Release Date: Fri, 22 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800570q Quelle: Journal of Medicinal Chemistry | 22 Aug 2008 | 6:00 am CEST

Phosphate Prodrugs Derived from N-Acetylglucosamine Have Enhanced Chondroprotective Activity in Explant Cultures and Represent a New Lead in Antiosteoarthritis Drug Discovery Christopher McGuigan, Michaela Serpi, Rita Bibbo, Helen Roberts, Clare Hughes, Bruce Caterson, Ana Torrent Gibert, and Carlos Raúl Alaez Verson Web Release Date: Thu, 21 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800594c Quelle: Journal of Medicinal Chemistry | 21 Aug 2008 | 6:00 am CEST

Novel Insight in Structure−Activity Relationship and Bioanalysis of P-Glycoprotein Targeting Highly Potent Tetrakishydroxymethyl Substituted 3,9-Diazatetraasteranes Claudius Coburger, Jörg Wollmann, Christiane Baumert, Martin Krug, Josef Molnár, Hermann Lage, and Andreas Hilgeroth Web Release Date: Thu, 21 Aug 2008 00:00:00 EDT (Brief Article) DOI: 10.1021/jm800480y Quelle: Journal of Medicinal Chemistry | 21 Aug 2008 | 6:00 am CEST

Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models Robert L. Hudkins, James L. Diebold, Ming Tao, Kurt A. Josef, Chung Ho Park, Thelma S. Angeles, Lisa D. Aimone, Jean Husten, Mark A. Ator, Sheryl L. Meyer, Beverly P. Holskin, John T. Durkin, Alexander A. Fedorov, Elena V. Fedorov, Steven C. Almo, Joanne R. Mathiasen, Donna Bozyczko-Coyne, Michael S. Saporito, Richard W. Scott, and John P. Mallamo Web Release Date: Thu, 21 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm8005838 Quelle: Journal of Medicinal Chemistry | 21 Aug 2008 | 6:00 am CEST

Discovery of Antimycobacterial Spiro-piperidin-4-ones: An Atom Economic, Stereoselective Synthesis, and Biological Intervention Raju Ranjith Kumar, Subbu Perumal, Palaniappan Senthilkumar, Perumal Yogeeswari, and Dharmarajan Sriram Web Release Date: Thu, 21 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800545k Quelle: Journal of Medicinal Chemistry | 21 Aug 2008 | 6:00 am CEST

Discovery of Novel Cdc25 Phosphatase Inhibitors with Micromolar Activity Based on the Structure-Based Virtual Screening Hwangseo Park, Young Jae Bahn, Suk-Kyeong Jung, Dae Gwin Jeong, Sang-Hyeup Lee, Il Seo, Tae-Sung Yoon, Seung Jun Kim, and Seong Eon Ryu Web Release Date: Thu, 21 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm701157g Quelle: Journal of Medicinal Chemistry | 21 Aug 2008 | 6:00 am CEST

4′′-Benzoylureido-TSAO Derivatives as Potent and Selective Non-Nucleoside HCMV Inhibitors. Structure−Activity Relationship and Mechanism of Antiviral Action Sonia de Castro, M. Teresa Peromingo, Lieve Naesens, Graciela Andrei, Robert Snoeck, Jan Balzarini, Sonsoles Velázquez, and María-José Camarasa Web Release Date: Sat, 16 Aug 2008 00:00:00 EDT (Article) DOI: 10.1021/jm800050t Quelle: Journal of Medicinal Chemistry | 16 Aug 2008 | 6:00 am CEST

Recent Advances on Phosphodiesterase 4 Inhibitors for the Treatment of Asthma and Chronic Obstructive Pulmonary Disease Arumugam Kodimuthali, S. Sugin Lal Jabaris, and Manojit Pal Web Release Date: Fri, 8 Aug 2008 00:00:00 EDT (Perspective) DOI: 10.1021/jm800582j Quelle: Journal of Medicinal Chemistry | 8 Aug 2008 | 6:00 am CEST

Book Review of Molecular Modeling: Basic Principles and Applications. Third Edition Salvatore Profeta Jr. Web Release Date: Thu, 7 Aug 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800757u Quelle: Journal of Medicinal Chemistry | 7 Aug 2008 | 6:00 am CEST

Book Review of Carbohydrate Chemistry and Biochemistry. Structure and Mechanism D. Eric Walters Web Release Date: Fri, 1 Aug 2008 00:00:00 EDT (Book Review) DOI: 10.1021/jm800822h Quelle: Journal of Medicinal Chemistry | 1 Aug 2008 | 6:00 am CEST

Nominations Sought for the 2006 American Chemical Society Division of Medicinal Chemistry Award null Web Release Date: Wed, 21 Sep 2005 00:00:00 EDT (Editorial) DOI: 10.1021/jm058265h Quelle: Journal of Medicinal Chemistry | 21 Sep 2005 | 6:00 am CEST

null null Web Release Date: Wed, 12 May 2004 00:00:00 EDT (null) DOI: 10.1021/jm0400855 Quelle: Journal of Medicinal Chemistry | 12 May 2004 | 6:00 am CEST

Three-dimensional quantitative structure-activity relationship (CoMFA and CoMSIA) studies on galardin derivatives as gelatinase A (matrix metalloproteinase 2) inhibitors Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis and antinociceptive-antimicrobial activities of some new amide derivatives of 3,5-di/-and 1,3,5-trimethylpyrazoles Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis and antimicrobial studies of novel 1-benzhydryl-piperazine sulfonamide and carboxamide derivatives Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Studies on hydrazone derivatives as antifungal agents Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis of azatricyclodiones & octahydro-benzo[f]isoindoles and their antimicrobial evaluation Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Inhibition of mammalian aspartate transcarbamylase by quinazolinone derivatives Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

In-vitro antibacterial, antifungal activity of some transition metal complexes of thiosemicarbazone Schiff base (HL) derived from N 4 -(7'-chloroquinolin-4'-ylamino) thiosemicarbazide Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Mononuclear and dinuclear peroxotungsten complexes with co-ordinated dipeptides as potent inhibitors of alkaline phosphatase activity Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Inactivation of jack bean urease by N -ethylmaleimide: pH dependence, reversibility and thiols influence Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Differentiation of EDTA-sensitive from EDTA-insensitive human serum esterases hydrolysing phenylacetate Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Effects of hydroxybenzyl alcohols on melanogenesis in melanocyte-keratinocyte co-culture and monolayer culture of melanocytes Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Mono- (Ag, Hg) and di- (Cu, Hg) valent metal ions effects on the activity of jack bean urease. Probing the modes of metal binding to the enzyme Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Anti-inflammatory activity of a new triterpenoid saponin from carthamus tinctorius linn Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Simple inhibitors of histone deacetylase activity that combine features of short-chain fatty acid and hydroxamic acid inhibitors Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Structure-activity study of phosphoramido acid esters as acetylcholinesterasf inhibitors Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Inhibition of AChE by malathion and some structurally similar compounds Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Evaluation of natural substances from Evolvulus alsinoides L. with the purpose of determining their antioxidant potency Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Differential in vitro inhibition effects of some antibiotics on tumor associated carbonic anhydrase isozymes of hCA-IX and hCA-XII Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

In vitro aldose reductase inhibitory activity of some flavonyl-2,4-thiazolidinediones Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Design, synthesis and preliminary screening of novel 3-(2- N , N -dimethylaminoethylthio) indole derivatives as potential 5-HT 6 receptor ligands Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Butyrylcholinesterase, lipoxygenase inhibiting and antifungal alkaloids from isatis tinctoria Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Xanthine dehydrogenase processes retinol to retinoic acid in human mammary epithelial cells Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Effect of mesoionic 4-phenyl-5-(cinnamoyl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative salts on the activities of the nitric oxide synthase and arginase of Leishmania amazonensis Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Synthesis and evaluation of N-substituted indole-3-carboxamide derivatives as inhibitors of lipid peroxidation and superoxide anion formation Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Microbial and xanthine dehydrogenase inhibitory activity of some flavones Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Design, synthesis, characterization, antibacterial and antifungal activities of a novel class of 5,7-diaryl-4,4-dimethyl-4,5,6,7-tetrahydropyridino[3,4-d]-1,2,3-selenadiazoles Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Novel peptide-based pepsin inhibitors containing an epoxide group Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Brucella suis histidinol dehydrogenase: Synthesis and inhibition studies of substituted N-L-histidinylphenylsulfonyl hydrazide Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Antimicrobial effect by extracts of rhizome of Alpinia officinarum Hance may relate to its inhibition of β-ketoacyl-ACP reductase Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Structural elucidation and biological significance of 2-hydroxy-1-naphthaldehyde derived sulfonamides and their first row d-transition metal chelates Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Some kinetic properties of polyphenol oxidase obtained from dill ( Anethum graveolens ) Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Urease inhibitor from Datisca cannabina linn Quelle: Journal of Enzyme Inhibition and Medicinal Chemistry: Articles recently published in |

Modulation of Anopheles gambiae Epsilon glutat