Cover image for Vol. 12 Issue 12

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 3.225

ISI Journal Citation Reports © Ranking: 2016: 17/60 (Chemistry Medicinal); 73/256 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

Recently Published Issues

See all

Latest News

Browse more news

June 12, 2017

VIP: Redox-Active Ruthenium(II) Polypyridyl Complexes

N. Alatrash, E. S. Narh, A. Yadav, M.-J. Kim, T. Janaratne, J. Gabriel, F. M. MacDonnell

Various ruthenium polypyridyl complexes (RPCs) have been explored as potential drugs or therapeutics for nearly a half a century now. Relatively few animal studies have been conducted with RPCs, and most of these reveal RPCs to be potent inhibitors of acetylcholine esterase (AChE) which leads to acute neurotoxicity in vivo at modest doses, severely limiting therapeutic potential. Read more...

Your Comment...

[Browse more news]

Recently Published Articles

  1. Residence Time, a New parameter to Predict Neurosteroidogenic Efficacy of Translocator Protein (TSPO) Ligands: the Case Study of N,N-Dialkyl-2-arylindol-3-ylglyoxylamides

    Prof. Barbara Costa, Prof. Sabrina Taliani, Dr. Eleonora Da Pozzo, Dr. Elisabetta Barresi, Dr. Marco Robello, Dr. Chiara Cavallini, Dr. Sandro Cosconati, Prof. Federico Da Settimo, Prof. Ettore Novellino and Prof. Claudia Martini

    Version of Record online: 22 JUN 2017 | DOI: 10.1002/cmdc.201700220

    Thumbnail image of graphical abstract

    How long can you stay? The neurosteroidogenic efficacy of translocator protein (TSPO) ligands can be predicted by evaluating the amount of time—the residence time—that a given ligand spends in the target rather than the binding affinity. This aids in the development of novel compounds with promising pharmacological properties and therapeutic potential.

  2. Thiazole-Based σ1 Receptor Ligands: Diversity by Late-Stage C−H Arylation of Thiazoles, Structure–Affinity and Selectivity Relationships, and Molecular Interactions

    Dr. Artur K. Kokornaczyk, Dr. Dirk Schepmann, Prof. Dr. Junichiro Yamaguchi, Prof. Dr. Kenichiro Itami, Dr. Erik Laurini, Dr. Maurizio Fermeglia, Prof. Dr. Sabrina Pricl and Prof. Dr. Bernhard Wünsch

    Version of Record online: 22 JUN 2017 | DOI: 10.1002/cmdc.201700166

    Thumbnail image of graphical abstract

    Bioisosteric benefits: To increase σ1 receptor ligand efficiency of spirocylic thiophenes, the thiophene ring was replaced with a thiazole, and the pyran ring was opened to afford 53 derivatives. Among these, two pyridyl-substituted thiazole derivatives were most promising, with low-nanomolar σ1 affinity, high σ12 selectivity, low lipophilicity, and very good ligand efficiency, indicating promising pharmacodynamics and pharmacokinetics.

  3. Discovery of novel wtRET and V804MRET inhibitors: from hit to lead

    luca mologni, martina dalla via, adriana chilin, manlio palumbo and Giovanni Marzaro

    Accepted manuscript online: 22 JUN 2017 02:45AM EST | DOI: 10.1002/cmdc.201700243

  4. You have full text access to this OnlineOpen article
    Nucleic Acid Templated Reactions for Chemical Biology (pages 872–882)

    Dr. Margherita Di Pisa and Prof. Dr. Oliver Seitz

    Version of Record online: 21 JUN 2017 | DOI: 10.1002/cmdc.201700266

    Thumbnail image of graphical abstract

    From sci-fi to reality: Nucleic acid templated chemical reactions are a unique asset in chemical biology, enabling specific in situ drug synthesis, release, and nucleic acid sensing. Herein we review recent and instructive examples of conditional synthesis or release of compounds for in cellulo protein interference and intracellular nucleic acid imaging.

  5. You have free access to this content
    The 52nd International Conference on Medicinal Chemistry (RICT 2016) of the French Medicinal Chemistry Society (SCT) Held in Caen (Normandy) (pages 862–871)

    Prof. Janos Sapi, Dr. Luc Van Hijfte and Prof. Patrick Dallemagne

    Version of Record online: 21 JUN 2017 | DOI: 10.1002/cmdc.201700336

    Thumbnail image of graphical abstract

    Outstanding Medchem in France: Guest editors Janos Sapi, Luc Van Hjfte, and Patrick Dallemagne look back at the 52nd International Conference on Medicinal Chemistry (RICT 2016) held in Caen, France. They discuss the history of the French Medicinal Chemistry Society (Société de Chimie Thérapeutique, SCT) and provide highlights of last year′s events, including some key presentations now collected in this Special Issue.