Archiv der Pharmazie

Cover image for Vol. 348 Issue 4

Edited By: Holger Stark

Impact Factor: 1.396

ISI Journal Citation Reports © Ranking: 2013: 42/58 (Chemistry Medicinal); 74/148 (Chemistry Multidisciplinary); 180/256 (Pharmacology & Pharmacy)

Online ISSN: 1521-4184

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Recently Published Articles

  1. Acetylcholinesterase Inhibitory and Antioxidant Activities of Novel Symmetric Sulfamides Derived from Phenethylamines

    Kadir Aksu, Fevzi Topal, İlhami Gulcin, Ferhan Tümer and Süleyman Göksu

    Article first published online: 24 APR 2015 | DOI: 10.1002/ardp.201500035

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    A series of novel phenolic sulfamides were synthesized and evaluated for their antioxidant and acetylcholinesterase inhibitory properties. All compounds clearly showed antioxidant, antiradical, metal binding, and reducing abilities as well as acetylcholinesterase inhibition.

  2. Synthesis, Biological Activity, and Docking Study of Novel Isatin Coupled Thiazolidin-4-one Derivatives as Anticonvulsants

    Anna P. Nikalje, Altamash Ansari, Sanjay Bari and Vinod Ugale

    Article first published online: 22 APR 2015 | DOI: 10.1002/ardp.201500020

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    A series of novel 2-(substituted-phenyl)-3-(2-oxoindolin-3-ylidene)amino)-thiazolidin-4-one derivatives were synthesized and evaluated for their anticonvulsant and CNS depressant activities on mice. All the derivatives showed good CNS depressant activity and protection in the MES test. In addition, the designed compounds were docked into the NMDA and AMPA receptors, revealing binding interactions.

  3. Design, Synthesis, and Biological Evaluation of Thiazolidine-2,4-dione Conjugates as PPAR-γ Agonists

    Syed Nazreen, Mohammad Sarwar Alam, Hinna Hamid, Mohammad Shahar Yar, Abhijeet Dhulap, Perwez Alam, Mohammad Abdul Qadar Pasha, Sameena Bano, Mohammad Mahboob Alam, Saqlain Haider, Chetna Kharbanda, Yakub Ali and Kolakappi Pillai

    Article first published online: 21 APR 2015 | DOI: 10.1002/ardp.201400280

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    A new series of 2,4-thiazolidinedione analogues (5am) was synthesized, showing potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation and significant blood glucose lowering effects comparable to the standard drugs pioglitazone and rosiglitazone. Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.

  4. Toward Labeled Argininamide-Type NPY Y1 Receptor Antagonists: Identification of a Favorable Propionylation Site in BIBO3304

    Max Keller, Lisa Schindler, Günther Bernhardt and Armin Buschauer

    Article first published online: 17 APR 2015 | DOI: 10.1002/ardp.201400427

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    (R)-N-[4-(Aminocarbonylaminomethyl)benzyl]-Nα-diphenylacetylargininamide (BIBO3304) was modified to obtain propionylated derivatives with high neuropeptide Y (NPY) Y1 receptor affinity and selectivity. The new compounds are promising candidates for radiolabeling by [3H]propionylation.

  5. Design, Synthesis, and Anti-Thrombotic Evaluation of Some Novel Fluorinated Thrombin Inhibitor Derivatives

    Haifeng Chen and Yujie Ren

    Article first published online: 16 APR 2015 | DOI: 10.1002/ardp.201400460

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    With the help of computer-aided simulation, a series of fluoride groups were introduced into thrombin inhibitory drugs, and the resulting thrombin inhibitory activity was demonstrated in vitro. The most potent compound was found to be 3-(2-(((4-carbamimidoylphenyl)amino)methyl)-1-ethyl-N-(2-fluorophenyl)-1H-benzo[d]imidazole-5-carboxamido)propanoic acid 12a, with an IC50 value of 3.53 nmol/L.