Cover image for Vol. 11 Issue 20

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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October 19, 2016

ACT-451840: An Antimalarial Drug with a Novel Mechanism of Action

ACT-451840: An Antimalarial Drug with a Novel Mechanism of Action

Malaria remains one of the most significant health burdens in poorer parts of the world. With the recent emergence of initial signs of parasites resistant to artemisinine combination therapy, and in the absence of effective malaria vaccines, the quest for antimalarials with different mechanisms of action has gained increased importance.

Industry–university collaborative efforts led by Christoph Boss (Actelion Pharamceuticals Ltd.) and Sergio Wittlin (Swiss Tropical and Public Health Institute) toward the identification of an antimalarial drug with a novel mechanism of action resulted in the identification of ACT-451840, which was investigated in clinical trials.

Read the recent Actelion press release as well as our news article; the full paper can be found here: 10.1002/cmdc.201600298.

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Recently Published Articles

  1. Using Chemical Probes to Assess the Feasibility of Targeting SecA for Developing Antimicrobial Agents against Gram-Negative Bacteria

    Dr. Jinshan Jin, Dr. Ying-Hsin Hsieh, Dr. Jianmei Cui, Dr. Krishna Damera, Dr. Chaofeng Dai, Dr. Arpana S. Chaudhary, Dr. Hao Zhang, Dr. Hsiuchin Yang, Nannan Cao, Prof. Chun Jiang, Prof. Martti Vaara, Prof. Binghe Wang and Prof. Phang C. Tai

    Version of Record online: 18 OCT 2016 | DOI: 10.1002/cmdc.201600421

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    Broad-spectrum antimicrobials? SecA inhibitors are potent antimicrobials against Gram-positive bacteria. Whether SecA is a valid target against Gram-negative bacteria is an unanswered question. By probing the membrane permeability issue, we found that indeed inhibition of SecA leads to bacteriostatic and bactericidal effects against Gram-negative bacteria. Such effects are not attenuated by the presence of efflux pumps, which are responsible for multidrug resistance. Therefore, SecA is an excellent target for developing broad-spectrum antimicrobials against drug-resistant bacteria.

  2. Acryloylphenylcarboxamides: A New Class of Breast Cancer Resistance Protein (ABCG2) Modulators

    Stefanie Kraege, Sebastian C. Köhler and Prof. Dr. Michael Wiese

    Version of Record online: 13 OCT 2016 | DOI: 10.1002/cmdc.201600341

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    Busted! Acryloylphenylcarboxamides represent a new class of ABCG2 inhibitors. We combined the chalcone moiety with an additional aromatic residue by an amide linker. The position of the aromatic residue as well as that of the dimethoxy substituent on ring B have a large impact on activity. The most promising compound shows high potency and no cytotoxicity.

  3. Designing Simple Lipidated Lysines: Bifurcation Imparts Selective Antibacterial Activity

    Chandradhish Ghosh, Mohini Mohan Konai, Paramita Sarkar, Dr. Sandip Samaddar and Prof. Dr. Jayanta Haldar

    Version of Record online: 12 OCT 2016 | DOI: 10.1002/cmdc.201600400

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    How simple but selective antibacterial membrane-active agents can be designed is presented herein. Bifurcation of long alkyl chains into two short chains leads to selective antibacterial activity. A representative bifurcated compound exhibits broad-spectrum bactericidal activity and disrupts biofilms. It also treats burn wounds in mice infected with Acinetobacter baumannii. This principle could be applied to further designs of membrane-active agents.

  4. Structure–Activity Relationships of 2-Sufonylpyrimidines as Quorum-Sensing Inhibitors to Tackle Biofilm Formation and eDNA Release of Pseudomonas aeruginosa

    Andreas Thomann, Christian Brengel, Dr. Carsten Börger, Dr. Dagmar Kail, Dr. Anke Steinbach, Dr. Martin Empting and Prof. Dr. Rolf W. Hartmann

    Version of Record online: 12 OCT 2016 | DOI: 10.1002/cmdc.201600419

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    Dual-target SAR: a challenging task! With the use of flexible alignment and Hansch analysis, drug-like dual inhibitors of the Pseudomonas quinolone signal (PQS) synthase (PqsD) and the PQS receptor (PqsR) were developed. These compounds have high ligand efficiencies and can be used to combat extracellular DNA and biofilm formation by the drug-resistant and pathogenic bacteria Pseudomonas aeruginosa.

  5. Increasing Thyromimetic Potency through Halogen Substitution

    Dr. Jordan Devereaux, Dr. Skylar J. Ferrara, Tania Banerji, Dr. Andrew T. Placzek and Prof. Thomas S. Scanlan

    Version of Record online: 12 OCT 2016 | DOI: 10.1002/cmdc.201600408

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    Modifying the structure of the potent TRβ-selective thyroid hormone analogue sobetirome by replacing the 3,5-dimethyl groups with chlorine or bromine to exploit halogen bonding interactions within the TR ligand binding domain gives compounds with significantly increased potency in vitro and in vivo while retaining distribution to the CNS. These improved characteristics make the new compounds attractive candidates for treating CNS demyelination diseases influenced by thyroid hormone stimulation.