Cover image for Vol. 11 Issue 18

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. Identification and Structure–Activity Relationship Studies of Small-Molecule Inhibitors of the Methyllysine Reader Protein Spindlin1

    Dr. Dina Robaa, Dr. Tobias Wagner, Chiara Luise, Dr. Luca Carlino, Joel McMillan, Dr. Ralf Flaig, Prof. Dr. Roland Schüle, Prof. Dr. Manfred Jung and Prof. Dr. Wolfgang Sippl

    Version of Record online: 16 SEP 2016 | DOI: 10.1002/cmdc.201600362

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    Stopping the reader: An in silico screening approach coupled with in vitro testing was performed to search for inhibitors of the methyllysine reader protein Spindlin1. Among the eight identified inhibitors, 4-aminoquinazoline and quinazolinethione derivatives were recognized as promising lead structures. Subsequent chemical optimization was carried out, and a series of derivatives of both lead scaffolds were synthesized. This resulted in the discovery of Spindlin1 inhibitors and helped explore the SAR of these inhibitor series.

  2. A Triazinone Derivative Inhibits HIV-1 Replication by Interfering with Reverse Transcriptase Activity

    Dr. Emiko Urano, Dr. Kosuke Miyauchi, Dr. Yoko Kojima, Dr. Makiko Hamatake, Dr. Sherimay D. Ablan, Dr. Satoshi Fudo, Dr. Eric O. Freed, Dr. Tyuji Hoshino and Dr. Jun Komano

    Version of Record online: 16 SEP 2016 | DOI: 10.1002/cmdc.201600375

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    Resisting resistance: A novel non-nucleoside reverse transcriptase inhibitor (NNRTI, shown) was identified. Its EC50 values range from 107.9 to 145.4 nm against various primary HIV-1 clinical isolates, and is effective against HIV-1 with the K103N RT mutation, which confers substantial resistance to NNRTIs in current use. This compound has a unique drug-resistance profile and shows synergistic effects against HIV-1 in combination with other antiretroviral drugs, and could therefore serve as a lead for the development of novel NNRTIs.

  3. Chromones: A Promising Ring System for New Anti-inflammatory Drugs

    Carlos F. M. Silva, Dr. Diana C. G. A. Pinto and Prof. Artur M. S. Silva

    Version of Record online: 15 SEP 2016 | DOI: 10.1002/cmdc.201600359

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    Fact! The chromone nucleus is an important scaffold for the development of anti-inflammatory agents. Their interactions with important enzymes involved in inflammatory processes and their privileged features are not very well documented. In this minireview we discuss the structure–activity relationships of chromones as well as their mechanisms of action.

  4. Effect of Partially Fluorinated N-Alkyl-Substituted Piperidine-2-carboxamides on Pharmacologically Relevant Properties

    Raffael Vorberg, Dr. Nils Trapp, Dr. Daniel Zimmerli, Björn Wagner, Dr. Holger Fischer, Dr. Nicole A. Kratochwil, Dr. Manfred Kansy, Prof. Dr. Erick M. Carreira and Prof. Dr. Klaus Müller

    Version of Record online: 15 SEP 2016 | DOI: 10.1002/cmdc.201600325

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    Fine tuned in F sharp: Fluorinated N-alkyl-piperidine-2-carboxamides display remarkably consistent response of pharmacologically relevant properties to variations of the fluorination pattern in the alkyl group. Compared to neutral alkyl-substituted heteroaryl systems, characteristic deviations of response to fluorination are observed due to strong modulation of amine basicity affecting lipophilicity and other pharmacologically relevant properties.

  5. Theranostic Polyaminocarboxylate–Cyanine–Transferrin Conjugate for Anticancer Therapy and Near-Infrared Optical Imaging

    Dr. Chi Soo Kang, Siyuan Ren, Dr. Xiang Sun and Prof. Hyun-Soon Chong

    Version of Record online: 14 SEP 2016 | DOI: 10.1002/cmdc.201600072

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    See what you iron out: A cytotoxic and near-IR fluorescent transferrin conjugate, N-NE3TA–Tf–Cy5.5 (at left), was developed for potential theranostic use in targeted iron chelation cancer therapy and optical imaging. Microscopic observations revealed this conjugate to accumulate in cancer cells at high levels. These encouraging in vitro data suggest the potential of N-NE3TA–Tf–Cy5.5 as a novel theranostic agent for the detection and treatment of cancers.