Archiv der Pharmazie

Cover image for Vol. 348 Issue 11

Edited By: Holger Stark

Impact Factor: 1.531

ISI Journal Citation Reports © Ranking: 2014: 41/59 (Chemistry Medicinal); 75/157 (Chemistry Multidisciplinary); 180/255 (Pharmacology & Pharmacy)

Online ISSN: 1521-4184

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  1. Monoamine Oxidase Inhibitory Activity of Ferulic Acid Amides: Curcumin-Based Design and Synthesis

    Vishnu N. Badavath, İpek Baysal, Gülberk Uçar, Susanta K. Mondal, Barij N. Sinha and Venkatesan Jayaprakash

    Article first published online: 23 NOV 2015 | DOI: 10.1002/ardp.201500317

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    A series of ferulic acid amides 6a–m were designed and tested for their inhibitory activity on human monoamine oxidase (hMAO) isoforms. All the compounds were found to have inhibitory activity, with a gradual shift from hMAO-B selectivity (6a,b) to non-selectivity (6c–f). Molecular docking simulation showed that compound 6k is a competitive and reversible inhibitor of hMAO-B.

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    Design, Synthesis, and Antiviral Activity of Novel Ribonucleosides of 1,2,3-Triazolylbenzyl-aminophosphonates

    Abdelaaziz Ouahrouch, Moha Taourirte, Dominique Schols, Robert Snoeck, Graciela Andrei, Joachim W. Engels and Hassan B. Lazrek

    Article first published online: 17 NOV 2015 | DOI: 10.1002/ardp.201500292

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    Ribonucleosides of 1,2,3-triazolylbenzyl-aminophosphonate analogs were synthesized through the Kabachnik–Fields reaction and copper-catalyzed cycloaddition of the azide–alkyne reaction. All compounds were tested against various strains of DNA and RNA viruses. Compounds 4b and 4c showed modest inhibitory activity against respiratory syncytial virus while compound 4h displayed modest inhibitory activity against Coxsackie virus B4.

  3. Evaluation of Novel Chalcone Oximes as Inhibitors of Tyrosinase and Melanin Formation in B16 Cells

    Sini K. Radhakrishnan, Ronald G. Shimmon, Costa Conn and Anthony T. Baker

    Article first published online: 17 NOV 2015 | DOI: 10.1002/ardp.201500298

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    A series of hydroxy-substituted chalcone oxime derivatives were synthesized and evaluated for their inhibitory activities on tyrosinase and melanogenesis in murine B16F10 melanoma cells. Two of the compounds exhibited much higher tyrosinase inhibitory activities than kojic acid. The active inhibitors were shown to strongly interact with the tyrosinase residues of Agaricus bisporus.

  4. Mechanochemical Synthesis and Antioxidant Activity of Curcumin-Templated Azoles

    Daisy R. Sherin and Kallikat N. Rajasekharan

    Article first published online: 10 NOV 2015 | DOI: 10.1002/ardp.201500305

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    3,5-Bis(4-hydroxy-3-methoxystyryl)pyrazoles 2a–f and 3,5-bis(4-hydroxy-3-methoxystyryl)isoxazole 2g were rapidly prepared mechanochemically from curcumin 1 and hydrazines or hydroxylamine. Several of these compounds exhibit better antioxidant activity than curcumin. For example, the EC50 values based on the percentage of DPPH inhibition by 1, 2a, and 2g are 40, 14, and 8 µmol, respectively.

  5. 1,8-Naphthyridine Derivatives: A Review of Multiple Biological Activities

    Alka Madaan, Ritu Verma, Vivek Kumar, Anu T. Singh, Swatantra K. Jain and Manu Jaggi

    Article first published online: 9 NOV 2015 | DOI: 10.1002/ardp.201500237

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    The 1,8-naphthyridine (C8H6N2) scaffold is one of the six isomeric forms of diazanaphthalenes or pyridopyridines. Nalidixic acid (1-ethyl-7-methyl-4-oxo-[1,8]naphthyridine-3-carboxylic acid) was the first of the synthetic quinolone antibiotics. This comprehensive review summarizes the diverse biological activities of the 1,8-naphthyridine derivatives reported so far.