Archiv der Pharmazie

Cover image for Vol. 348 Issue 7

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 Evaluation of a Series of Oleanolic Acid Saponins as α-Glucosidase and α-Amylase Inhibitors

    Tiantian Guo, Shaoping Wu, Sen Guo, Lu Bai, Qingchao Liu and Naisheng Bai

    Article first published online: 24 JUL 2015 | DOI: 10.1002/ardp.201500179

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    A series of naturally occurring oleanane-type triterpenoid saponins and non-natural oleanolic acid saponins were synthesized, and their inhibitory activities against α-glucosidase and α-amylase were evaluated in vitro. With an IC50 value of 87.3 μM, 28-O-monoglucoside 8 exhibited fivefold stronger inhibitory activity against α-glucosidase than the antidiabetic acarbose.

  2. In Vitro Inhibition of Human Placental Glutathione S-Transferase by 3-Arylcoumarin Derivatives

    Mustafa Muhlis Alparslan and Özkan Danış

    Article first published online: 22 JUL 2015 | DOI: 10.1002/ardp.201500151

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    A series of 3-aryl-2H-chromen-2-one derivatives (4a–d, 5a–d, and 6a,b) are assessed for their inhibitory activity on human GSTP1-1. The most active compound (6a, IC50 = 13.5 µM) shows mixed inhibition with respect to glutathion and non-competitive inhibition against 1-chloro-2,4-dinitrobenzene, and may serve as a lead for developing new glutathione S-transferase inhibitors.

  3. Synthesis and Evaluation of Chroman-4-One Linked to N-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors

    Saman Arab, Seyed-Esmail Sadat-Ebrahimi, Maryam Mohammadi-Khanaposhtani, Alireza Moradi, Hamid Nadri, Mohammad Mahdavi, Setareh Moghimi, Mehdi Asadi, Loghman Firoozpour, Morteza Pirali-Hamedani, Abbas Shafiee and Alireza Foroumadi

    Article first published online: 20 JUL 2015 | DOI: 10.1002/ardp.201500149

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    A novel series of chroman-4-one derivatives bearing N-benzyl pyridinium derivatives (8a–l) were synthesized and evaluated in vitro for their acetylcholinesterase inhibitory activities. The most promising compound, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide 8l, showed an IC50 value of 0.048 µM.

  4. Thiomorpholine Derivatives with Hypolipidemic and Antioxidant Activity

    Kyriaki-Konstantina Tooulia, Panagiotis Theodosis-Nobelos and Eleni A. Rekka

    Article first published online: 20 JUL 2015 | DOI: 10.1002/ardp.201500147

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    Based on the already known lipid-lowering and antioxidant action of morpholine derivatives, a series of substituted thiomorpholines were designed, further incorporating an antioxidant moiety as the N-substituent. The new derivatives show considerable antioxidant potential with hypolipidemic activity and may also have combined squalene synthase inhibitory activity.

  5. Pulmonary Delivery of siRNA via Polymeric Vectors as Therapies of Asthma

    Yuran Xie and Olivia M. Merkel

    Article first published online: 7 JUL 2015 | DOI: 10.1002/ardp.201500120

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    RNA interference (RNAi) may be a promising treatment of asthma, but so far difficulties regarding the delivery of small interference RNA (siRNA), the key factor in RNAi, to target cells/tissues have limited its clinical application. This review summarizes the cytokines, chemokines, transcription factors, tyrosine kinases, and costimulatory factors reported as targets of siRNA-mediated treatment in experimental asthma.

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