Archiv der Pharmazie

Cover image for Vol. 348 Issue 10

Edited By: Holger Stark

Impact Factor: 1.531

ISI Journal Citation Reports © Ranking: 2014: 41/59 (Chemistry Medicinal); 75/157 (Chemistry Multidisciplinary); 179/254 (Pharmacology & Pharmacy)

Online ISSN: 1521-4184

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Recently Published Articles

  1. Synthesis and Anti-Hepatitis B Virus Evaluation of 7-Methoxy-3-heterocyclic quinolin-6-ols

    Yajing Liu, Guobing Feng, Zonghui Ma, Chen Xu, Zhuang Guo, Ping Gong and Liying Xu

    Article first published online: 5 OCT 2015 | DOI: 10.1002/ardp.201500238

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    A series of novel 7-methoxy-3-heterocyclic quinolin-6-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus activities and cytotoxicities in the HepG2.2.15 cell line. Five compounds displayed excellent potency and selectivity toward the hepatitis B virus, with IC50 values of less than 5.0 μM and selectivity index values of 11.0–71.5.

  2. Design and Synthesis of Novel 1,2,3-Triazole- and 2-Isoxazoline-Based Bis-Heterocycles as Immune Potentiators

    Tabasum Ismail, Syed Shafi, Irfan Hyder, Tabasum Sidiq, Anamika Khajuria, Sarvar M. Alam and M. Sampath Kumar Halmuthur

    Article first published online: 23 SEP 2015 | DOI: 10.1002/ardp.201400398

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    A series of bis-heterocycles bearing triazole and isooxazoline are synthesized and subjected to in vitro lymphocyte proliferation assays, followed by in vivo studies of the more active compounds, 8g and 8h. Based on both the in vitro and in vivo studies, compounds 8g and 8h possess excellent immunopotentiating activity.

  3. Design, Synthesis, and Molecular Docking of Novel Pyrrolooxazepinediol Derivatives with Anti-Influenza Neuraminidase Activity

    Ahmed O. H. El-Nezhawy, Ahmad F. Eweas, Ibrahim A. Maghrabi, Ahmed S. Edalo and Sayed F. Abdelwahab

    Article first published online: 17 SEP 2015 | DOI: 10.1002/ardp.201500209

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    Novel pyrrolo[2,1-b][1,3]oxazepine-8,9-diol derivatives 12–15 were synthesized starting from l-tartaric acid. Molecular docking studies demonstrated that all tested compounds bind to the active site of neuraminidase. Compound 12 exhibited the highest anti-influenza (H5N1) activity (EC50 = 0.016 µg/mL) comparable to that of oseltamivir (EC50 = 0.012 µg/mL).

  4. Synthesis and Identification of Pregnenolone Derivatives as Inhibitors of Isozymes of 5α-Reductase

    Alejandra Chávez-Riveros, Eugene Bratoeff, Yvonne Heuze, Juan Soriano, Isabel Moreno, Araceli Sánchez-Márquez and Marisa Cabeza

    Article first published online: 17 SEP 2015 | DOI: 10.1002/ardp.201500220

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    Inhibition of 5α-reductase (5α-R) in the prostate may be a promising therapy in cases of hyperplasia of the prostate gland and prostate cancer. Five different 21-esters of pregnenolone derivatives were synthesized and tested as inhibitors of 5α-R types 1 and 2 in vivo and in vitro. The 21(p-fluoro)benzoyloxypregna-4,16-diene-3,6,20-trione derivative shows the best molecular conformation to inhibit the in vitro activity of both 5α-R isotypes.

  5. Targeting Human Poly(ADP-Ribose) Polymerase-1 with Natural Medicines and Its Potential Applications in Ovarian Cancer Therapeutics

    Min Song, Jun-Lan Li, Xiao-Ping Li and Shi-Feng Kan

    Article first published online: 7 SEP 2015 | DOI: 10.1002/ardp.201500183

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    An integrated procedure is described to discover novel potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors by screening against a large library of natural products. Several hits are identified to have high or moderate potency against PARP-1 with inhibitory activity at the nanomolar level.