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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
July 24, 2016
Drugs to Fight Bugs
Two 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.
Recently Published Articles
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Janish Desai, Dr. Yi-Liang Liu, Hongli Wei, Dr. Weidong Liu, Dr. Tzu-Ping Ko, Prof. Rey-Ting Guo and Prof. Eric Oldfield
Version of Record online: 26 JUL 2016 | DOI: 10.1002/cmdc.201600311
New drug target: Staphylococcus aureus heptaprenyl diphosphate synthase (HepPPS), involved in menaquinone biosynthesis, functions as a heterodimer and is inhibited by bisphosphonates (IC50=0.83 μm), which also inhibit S. aureus cell growth, an effect that is rescued by menaquinone. HepPPS is also partially inhibited by its substrates FPP as well as IPP, most likely due to disruption of the heterodimeric complex structure.
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Prof. Vladislav Deigin, Dr. Olga Ksenofontova, Dr. Alexey Khrushchev, Dr. Oleg Yatskin, Dr. Alexandra Goryacheva and Prof. Vadim Ivanov
Version of Record online: 26 JUL 2016 | DOI: 10.1002/cmdc.201600157
Robust and bioavailable! The low stability of peptide pharmaceuticals in non-invasive administration limits the use of these compounds in medical practice. We developed a platform based on branched piperazine-2,5-diones for creating orally stable peptidomimetics. These derivatives were attached to the N or C termini of an active linear peptide, increasing their resistance against proteolytic activity. As a result, the first orally active hemostimulatory peptides have been prepared.
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Version of Record online: 26 JUL 2016 | DOI: 10.1002/cmdc.201600244
Antibiotics by MCR: We disclose a new family of antibacterial agents derived from para-nitrophenols and indoline, prepared by a multicomponent reaction (MCR). The new alkylaminophenols show minimum inhibitory concentrations lower than 1.4 μm against selected resistant microorganisms. Cytotoxicity assays demonstrated that such compounds are viable candidates as antibacterials, as no cytotoxicity was observed at these concentrations.
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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
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.
- 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
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.