Cover image for Vol. 9 Issue 12

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (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

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November 22, 2014

The Most Accessed Are More Accessible

The Most Accessed Are More AccessibleChemMedChem's top-24 most-accessed articles of the last 12 months are now free to access! The diverse topics covered by these articles reflect the broad scope of the journal. Read more...

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  1. Carborane-Derived Local Anesthetics are Isomer Dependent

    Dr. George R. Kracke, Dr. Monika R. VanGordon, Dr. Yulia V. Sevryugina, Dr. Peter J. Kueffer, Dr. Kuanysh Kabytaev, Dr. Satish S. Jalisatgi and Dr. M. Frederick Hawthorne

    Article first published online: 24 NOV 2014 | DOI: 10.1002/cmdc.201402369

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    Cage anesthetics: In a new local anesthetic, ortho-boronicaine, the phenyl ring of lidocaine was replaced with a highly symmetric, ortho-carborane cage. Hindlimb plantar injections in mice resulted in longer analgesic effects compared with lidocaine. ortho-Boronicaine exhibited greater analgesic efficacy compared with lidocaine or the meta- and para-carborane or adamantane derivatives.

  2. Design, Synthesis, and Biological Evaluation of Unconventional Aminopyrimidine, Aminopurine, and Amino-1,3,5-triazine Methyloxynucleosides

    Gloria Fernández-Cureses, Sonia de Castro, María-Luisa Jimeno, Jan Balzarini and Prof. María-José Camarasa

    Article first published online: 24 NOV 2014 | DOI: 10.1002/cmdc.201402465

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    Bucking convention: Herein we describe unconventional nucleosides that combine methyloxy-bound pyrimidines or purines with D-allitolyl, D-altritolyl groups as unusual ribofuranosyl mimics or 2,5-bis-hydroxymethyltetrahydrofuran as their dideoxy analogues. The pyrimidine nucleotides act as adenine nucleotide mimics. This class of unconventional nucleosides represents a new family of potential antiproliferative agents.

  3. The Discovery of a Highly Selective 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 Inhibitor that is Neuroprotective in an in vitro Parkinson’s Disease Model

    Dr. Paolo Di Fruscia, Emmanouil Zacharioudakis, Chang Liu, Dr. Sébastien Moniot, Sasiwan Laohasinnarong, Mattaka Khongkow, Ian F. Harrison, Konstantina Koltsida, Dr. Christopher R. Reynolds, Karin Schmidtkunz, Prof. Dr. Manfred Jung, Dr. Kathryn L. Chapman, Prof. Dr. Clemens Steegborn, Prof. David T. Dexter, Prof. Michael J. E. Sternberg, Prof. Eric W.-F. Lam and Dr. Matthew J. Fuchter

    Article first published online: 13 NOV 2014 | DOI: 10.1002/cmdc.201402431

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    Hit discovery: Through ligand-based virtual screening validation, ICL-SIRT078, a cell-active substrate-competitive SIRT2 inhibitor with a Ki value of 0.62±0.15 μM and more than 50-fold selectivity against SIRT1, 3 and 5 was identified. In addition, ICL-SIRT078 shows a significant neuroprotective effect in a lactacystin-induced model of Parkinsonian neuronal cell death in the N27 cell line. ICL-SIRT078, or an optimised derivative thereof, warrants further investigation as a neuroprotective agent in in vivo models of Parkinson’s disease.

  4. From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy

    Dr. Yves P. Auberson, Dr. Thomas Troxler, Dr. Xuechun Zhang, Dr. Charles R. Yang, Dr. Dominik Feuerbach, Dr. Yu-Chih Liu, Dr. Bharat Lagu, Dr. Mark Perrone, Dr. Lijun Lei, Dr. Xiaoxia Shen, Dr. Dushan Zhang, Dr. Chunxiu Wang, Dr. Tie-Lin Wang, Dr. Karin Briner and Dr. Mark G. Bock

    Article first published online: 12 NOV 2014 | DOI: 10.1002/cmdc.201402418

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    Better than caffeine! Simplification of the ergoline scaffold of the H3 receptor antagonist 1 led to a series of indoles with improved pharmacological properties and better chemical accessibility. A combined pharmacodynamic, pharmacokinetic, and receptor occupancy evaluation led to the selection of 15 m, the wakefulness-enhancing properties of which were demonstrated by EEG measurements in rats.

  5. Oxidation Potentials of N-Modified Derivatives of the Analgesic Flupirtine Linked to Potassium KV7 Channel Opening Activity But Not Hepatocyte Toxicity

    Christian J. Lemmerhirt, Mirko Rombach, Dr. Anja Bodtke, Prof. Dr. Patrick J. Bednarski and Prof. Dr. Andreas Link

    Article first published online: 12 NOV 2014 | DOI: 10.1002/cmdc.201402442

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    Oxidation–activation–toxicity? The connection between activity, toxicity, and oxidation potential of the pain killer flupirtine was investigated. N-Modified analogues of flupirtine displayed varying oxidation potentials that appeared to be linked to potassium channel opening activity but not to in vitro hepatotoxicity. These data suggest that oxidative metabolites of flupirtine contribute to the mechanism of action, but not to liver toxicity.