Cover image for Vol. 10 Issue 5

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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April 29, 2015

Editor's Picks: Issue 05/2015

Editor's Picks: Issue 05/2015Editor's picks for issue 05: This month, two Full Papers by Dennis C. Waalboer et al. and David Böhme and Annette G. Beck-Sickinger describe methods of targeted drug delivery using molecular conjugation. Read more...

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  1. Design, Synthesis, and Biological Evaluation of Novel Nonsteroidal Farnesoid X Receptor (FXR) Antagonists: Molecular Basis of FXR Antagonism

    Huang Huang, Pei Si, Lei Wang, Yong Xu, Xin Xu, Prof. Jin Zhu, Prof. Hualiang Jiang, Prof. Weihua Li, Prof. Lili Chen and Prof. Jian Li

    Article first published online: 15 MAY 2015 | DOI: 10.1002/cmdc.201500136

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    X marks the spot: 39 trisubstituted isoxazoles were designed and synthesized, leading to compounds with pharmacological profiles ranging from agonist to antagonist at the farnesoid X receptor (FXR). By using the most potent antagonist as a probe, the essential molecular basis of FXR antagonism is proposed, and E467 on H12 can be regarded as a hot-spot residue for the future design of nonsteroidal antagonists of FXR.

  2. A Phytochemical–Halogenated Quinoline Combination Therapy Strategy for the Treatment of Pathogenic Bacteria

    Yasmeen Abouelhassan, Aaron T. Garrison, Dr. Fang Bai, Verrill M. Norwood IV, Minh Thu Nguyen, Prof. Shouguang Jin and Prof. Robert W. Huigens III

    Article first published online: 15 MAY 2015 | DOI: 10.1002/cmdc.201500179

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    Quite the combo! Halogenated quinolines and select phytochemicals, in particular gallic acid (GA), possess unique antibacterial synergy against several pathogenic bacteria, including: Staphylococcus aureus, S. epidermidis, Acinetobacter baumannii and Klebsiella pneumoniae. Here, GA is shown to potentiate the growth inhibitory properties of 1 (>10 000-fold) against S. aureus while also potentiating biofilm eradication activities against a methicillin-resistant S. aureus (MRSA) clinical isolate (fourfold).

  3. Novel Furin Inhibitors with Potent Anti-infectious Activity

    Dr. Kornelia Hardes, Dr. Gero L. Becker, Dr. Yinghui Lu, Dr. Sven O. Dahms, Susanne Köhler, Dr. Wolfgang Beyer, Prof. Kirsten Sandvig, Dr. Hiroyuki Yamamoto, Prof. Iris Lindberg, Lisa Walz, Dr. Veronika von Messling, Dr. Manuel E. Than, Prof. Wolfgang Garten and Prof. Torsten Steinmetzer

    Article first published online: 14 MAY 2015 | DOI: 10.1002/cmdc.201500103

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    Anti-infectious furin inhibitors: New peptidomimetic furin inhibitors with unnatural amino acid residues in the P3 position have been synthesized. The most potent compound, 4-guanidinomethylphenylacteyl-Arg-Tle-Arg-4-amidinobenzylamide (MI-1148), inhibits furin with a Ki value of 5.5 pM. The results confirm that the inhibition of furin is a promising strategy for a short-term treatment of acute infectious diseases.

  4. Potent, Metabolically Stable 2-Alkyl-8-(2H-1,2,3-triazol-2-yl)-9H-adenines as Adenosine A2A Receptor Ligands

    Dr. Silvia Pace, Dr. Giandomenico Brogin, Dr. Maria Antonietta Stasi, Dr. Teresa Riccioni, Franco Borsini, Dr. Francesca Capocasa, Dr. Francesco Manera, Carlo Tallarico, Dr. Pietro Grossi, Dr. Federica Vacondio, Dr. Michele Bassi, Dr. Francesca Bartoccini, Dr. Simone Lucarini, Dr. Giovanni Piersanti, Prof. Giorgio Tarzia, Walter Cabri and Dr. Patrizia Minetti

    Article first published online: 7 MAY 2015 | DOI: 10.1002/cmdc.201500113

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    The search for stability: Three, new ST1535 analogues were designed and synthesized to investigate their affinity for the A2A receptor, a validated target in the treatment of Parkinson’s disease. The aim was to improve the metabolic stability of ST1535 by blocking the ω-1 position of the butyl side chain. The new derivatives exhibited nanomolar affinity for the A2A receptor and significantly improved stability in human liver microsomes.

  5. Multitarget-Directed Tricyclic Pyridazinones as G Protein-Coupled Receptor Ligands and Cholinesterase Inhibitors

    Prof. Amedeo Pau, Dr. Marco Catto, Dr. Giovanni Pinna, Dr. Simona Frau, Dr. Gabriele Murineddu, Dr. Battistina Asproni, Prof. Maria M. Curzu, Dr. Leonardo Pisani, Dr. Francesco Leonetti, Prof. Maria Isabel Loza, Dr. José Brea, Prof. Gérard A. Pinna and Prof. Angelo Carotti

    Article first published online: 29 APR 2015 | DOI: 10.1002/cmdc.201500124

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    So many targets, so little time: Following a multitarget ligand design approach, 47 pyridazinone-based tricyclic compounds were prepared and tested as ligands of selected GPCRs (5-HT1A, α1A, and D2) and as cholinesterase inhibitors. Several compounds showed nanomolar affinity for the GPCRs tested, acting preferentially as dual antagonist ligands of α1A and 5-HT1A receptors, as well as good cholinesterase inhibitory activities.