ChemMedChem

Cover image for Vol. 11 Issue 14

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

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 76/253 (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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July 24, 2016

Drugs to Fight Bugs

Drugs to Fight BugsTwo recent reports in ChemMedChem are making waves in antimicrobial research. In the early July issue (13), professors William Wuest (Temple University), Kevin Minbiole (Villanova University), and co-workers report branched tetracationic quaternary ammonium compounds (QACs) as the most potent QACs reported so far against methicillin-resistant S. aureus. Their work is a significant breakthrough in the field of antiseptics and anti-biofilm agents.

In the current issue (14), Prof. R. D. Süssmuth and colleagues at the Technische Universität Berlin report their study of highly potent albicidin derivatives which will aid in the development of more drug-like structures of this class of antibiotic.

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Recently Published Articles

  1. Dioxonaphthoimidazoliums are Potent and Selective Rogue Stem Cell Clearing Agents with SOX2-Suppressing Properties

    Dr. Si-Han Sherman Ho, Dr. Azhar Ali, Yi-Cheng Ng, Dr. Kuen-Kuen Millie Lam, Prof. Shu Wang, Prof. Woon-Khiong Chan, Dr. Tan-Min Chin and Prof. Mei-Lin Go

    Version of Record online: 22 JUL 2016 | DOI: 10.1002/cmdc.201600262

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    Removing the rogues: The safety of stem cell therapy depends on the removal of undifferentiated rogue cells, which would otherwise transform into a malignant phenotype. The potent and selective stemotoxic properties of dioxonaphthoimidazoliums highlight their potential as stem cell clearing agents that could be deployed for this purpose.

  2. Synthesis of Albicidin Derivatives: Assessing the Role of N-terminal Acylation on the Antibacterial Activity

    Dennis Kerwat, Stefan Grätz, Dr. Julian Kretz, Maria Seidel, Maria Kunert, Dr. John B. Weston and Prof. Dr. Roderich D. Süssmuth

    Version of Record online: 21 JUL 2016 | DOI: 10.1002/cmdc.201600231

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    Advantages of acylated albicidin: The peptide antibiotic albicidin represents the most prominent member of a new class of antibacterial gyrase inhibitors. It shows remarkable antibacterial activities against Gram-positive and Gram-negative microorganisms. 14 newly synthesized albicidin derivatives with structural variations at the N-terminus are reported here. Gyrase inhibition and determination of minimal inhibitorial concentrations were assessed in parallel to show activities in a nm range and the necessity of N-acylation.

  3. A Double Prodrug with Improved Membrane Permeability over the Parent Chelator HBED Provides Superior Cytoprotection against Hydrogen Peroxide

    Dr. Nikki A. Thiele and Dr. Kenneth B. Sloan

    Version of Record online: 21 JUL 2016 | DOI: 10.1002/cmdc.201600197

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    Double your prodrug, double your fun! N,N′-bis(2-hydroxybenzyl)ethylenediamine-N,N′-diacetic acid (HBED), an iron chelator, has poor oral bioavailability that limits its clinical use. Here, double prodrugs of HBED that are activated by hydrolysis and oxidation were studied. Solubility, diffusivity, and cytoprotection studies all suggest that the double prodrugs may have improved membrane permeability over HBED that could lead to better delivery in vivo.

  4. Hedgehog Proteins Consume Steroidal CYP17A1 Antagonists: Potential Therapeutic Significance in Advanced Prostate Cancer

    Brandon M. Bordeau, Daniel A. Ciulla and Prof. Brian P. Callahan

    Version of Record online: 20 JUL 2016 | DOI: 10.1002/cmdc.201600238

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    Wrong way! Biochemical experiments indicate that steroidal anti-androgens, abiraterone and galeterone, undergo off-target covalent reactions with hedgehog proteins to produce hedgehog–drug conjugates. Cell-based assays indicate that these conjugates stimulate hedgehog signaling in the low nanomolar range.

  5. Fragment Screening of RORγt Using Cocktail Crystallography: Identification of Simultaneous Binding of Multiple Fragments

    Dr. Yafeng Xue, Hongwei Guo and Dr. Per Hillertz

    Version of Record online: 19 JUL 2016 | DOI: 10.1002/cmdc.201600242

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    Cocktail hour: A fragment screening using cocktail crystallography for the orphan nuclear receptor RORγt has enabled an experimental mapping of the ligand binding pocket and the identification of five distinct binding hotspots. This work also led to the observation of significant induced-fit, simultaneous binding of multiple fragments, as well as a surface binding site away from the ligand binding pocket (an initial hint to explore alternative ways to modulate RORγt through protein–protein interactions).

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