Archiv der Pharmazie

Cover image for Vol. 347 Issue 10

Edited By: Holger Stark

Impact Factor: 1.396

ISI Journal Citation Reports © Ranking: 2013: 42/58 (Chemistry Medicinal); 74/148 (Chemistry Multidisciplinary); 180/254 (Pharmacology & Pharmacy)

Online ISSN: 1521-4184

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Recently Published Articles

  1. New CYP17 Hydroxylase Inhibitors: Synthesis, Biological Evaluation, QSAR, and Molecular Docking Study of New Pregnenolone Analogs

    Najim A. Al-Masoudi, Dawood S. Ali, Bahjat Saeed, Rolf W. Hartmann, Matthias Engel, Sajid Rashid and Aamer Saeed

    Article first published online: 24 SEP 2014 | DOI: 10.1002/ardp.201400255

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    New imine, acyl, and tosylate analogs of pregnenolone were synthesized and evaluated for their CYP17 hydroxylase and HIV inhibition activities. The 5-aryl-1,3,4-thiadiazol-2-yl)-imino-pregnenolone derivatives turned out to be more active than the sulfonate and ester analogs. Molecular docking studies demonstrated similar binding patterns of all new pregnenolone derivatives.

  2. Design, Synthesis, and Biological Evaluation of Hydrazone Incorporated 1,2,4-Triazines as Anticonvulsant Agents

    Mohammed Amir, Israr Ali, Mohd. Zaheen Hassan and Naveen Mulakayala

    Article first published online: 24 SEP 2014 | DOI: 10.1002/ardp.201400045

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    New hydrazone incorporated triazines were designed and evaluated for their anticonvulsant activity. 4-[{2-(5-(3-Chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6k (MES ED50 54.31, scPTZ ED50 92.01) and 4-[{2-(5-(4-chlorobenzyl)-3-phenyl-1,2,4-triazine-6-yl)hydrazono}methyl]-N,N-dimethylaniline 6r (MES ED50 46.05, scPTZ ED50 83.90) emerged as the most active anticonvulsant agents with GABAergic effects.

  3. Mitochondria as a Target in the Therapeutic Properties of Curcumin

    Joyce Trujillo, Luis Fernando Granados-Castro, Cecilia Zazueta, Ana Cristina Andérica-Romero, Yolanda Irasema Chirino and José Pedraza-Chaverrí

    Article first published online: 22 SEP 2014 | DOI: 10.1002/ardp.201400266

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    Curcumin is a phenolic compound extracted from Curcuma longa. It is able to induce cytoprotective enzymes, anti-apoptotic signaling, and mitochondrial respiration and to diminish reactive oxygen spices. This review focuses on some of the most recent findings that suggest a close relationship of the antioxidant activity of curcumin with the mitochondrial function.

  4. Synthesis and Biological Evaluation of Benzothiazole Derivatives Bearing the ortho-Hydroxy-N-acylhydrazone Moiety as Potent Antitumor Agents

    Junjie Ma, Guangyan Zhang, Xiaoqi Han, Guanglong Bao, Lihui Wang, Xin Zhai and Ping Gong

    Article first published online: 17 SEP 2014 | DOI: 10.1002/ardp.201400230

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    Novel benzothiazole derivatives bearing the ortho-hydroxy-N-acylhydrazone moiety were synthesized and evaluated for their procaspase-3 kinase activation activities and antiproliferative activities. The most promising compound 18e (procaspase-3 EC50 = 0.31 µM) with IC50 values ranging from 0.24 to 0.92 µM against all tested cell lines was 4.24–12.2 times more active than PAC-1 (procaspase-3 EC50 = 0.41 µM).

  5. Synthesis and Carbonic Anhydrase Inhibitory Effects of Novel Sulfamides Derived from 1-Aminoindanes and Anilines

    Yusuf Akbaba, Enes Bastem, Fevzi Topal, İlhami Gülçin, Ahmet Maraş and Süleyman Göksu

    Article first published online: 16 SEP 2014 | DOI: 10.1002/ardp.201400257

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    Seven novel sulfamides were synthesized and their inhibitory properties against the human carbonic anhydrase isoenzymes I and II (hCA I and hCA II) were evaluated. Carbamate 17 showed the most potent inhibitory effect against hCA I (Ki: 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (Ki: 117.80 nM).