Archiv der Pharmazie

Cover image for Archiv der Pharmazie

October 2012

Volume 345, Issue 10

Pages 759–833

  1. Contents

    1. Top of page
    2. Contents
    3. Full Papers
    4. Short Communication
    5. Full Paper
    1. Archiv der Pharmazie 10/2012

      Article first published online: 2 OCT 2012 | DOI: 10.1002/ardp.201290010

  2. Full Papers

    1. Top of page
    2. Contents
    3. Full Papers
    4. Short Communication
    5. Full Paper
    1. Quantitative Structure–Activity Relationship Analysis of a Series of Human Renal Organic Anion Transporter Inhibitors (pages 759–766)

      Yuhui Wei, Lili Xi, Xiaojun Yao, Jiazhong Li and Xinan Wu

      Article first published online: 24 JUL 2012 | DOI: 10.1002/ardp.201200088

      Thumbnail image of graphical abstract

      Organic anion transporters (OAT) play important roles in the membrane transport of numerous potentially toxic xenobiotics, drugs, and endogenous metabolites. The relationships between 45 chemicals and the corresponding hOAT1 and hOAT3 inhibitory activities were analyzed. A quantitative structure–activity relationship model was developed by genetic algorithm and multiple linear regression method. The predictive power of the proposed model was evaluated and the applicability domain was also defined.

    2. 3-Nitro-2H-chromenes as a New Class of Inhibitors against Thioredoxin Reductase and Proliferation of Cancer Cells (pages 767–770)

      Guo-Qiang Xiao, Bao-Xia Liang, Shu-Han Chen, Tian-Miao Ou, Xian-Zhang Bu and Ming Yan

      Article first published online: 26 JUL 2012 | DOI: 10.1002/ardp.201200121

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      A series of 3-nitrochromenes were designed and synthesized. They showed good inhibitory activity against thioredoxin reductase and the proliferation of A549 cancer cells. Structure–activity relationship analysis revealed that the 3-nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. Bromo-substitutions at the 6- and 8-position of 3-nitrochromene significantly increase the inhibitory activity.

    3. Synthesis and Evaluation of Benzophenone O-Glycosides as α-Glucosidase Inhibitors (pages 771–783)

      Qingchao Liu, Tiantian Guo, Wenhong Li, Dong Li and Zili Feng

      Article first published online: 25 JUN 2012 | DOI: 10.1002/ardp.201200125

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      Facile synthesis of benzophenone O-glycosides (iriflophenone 2-O-α-L-rhamnopyranoside 1 and aquilarisinin 2) isolated from the leaves of Aquilaria sinensis and related new derivatives (3–12) was accomplished. Among these synthetic compounds, benzophenone O-glycosides 4 and 10 exhibited the most potent inhibitory activity in vitro against α-glucosidase with IC50 values of 168.7 ± 13.9 and 210.1 ± 23.9 µM, respectively.

    4. Synthesis and Antimicrobial Activities of a Novel Series of Heterocyclic α-Aminophosphonates (pages 784–789)

      Mohamed F. Abdel-Megeed, Badr E. Badr, Mohamed M. Azaam and Gamal A. El-Hiti

      Article first published online: 24 JUL 2012 | DOI: 10.1002/ardp.201200109

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      A novel series of α-aminophosphonates having heterocyclic moieties were synthesized. Their MICs indicate high antibacterial and antifungal activities at low concentrations. The synthesized compounds were proven to be safe for use as antimicrobial reagents.

    5. Effects of Varied Substituents on the Antibacterial Activity of Triazolylmethyl Oxazolidinones (pages 790–803)

      Oludotun A. Phillips, Edet E. Udo, Mohammed E. Abdel-Hamid and Reny Varghese

      Article first published online: 8 AUG 2012 | DOI: 10.1002/ardp.201100332

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      1,2,3-Triazolylmethyl piperazino oxazolidinone derivatives with varied substituents at the 4N-piperazine position were synthesized. Their antibacterial activities were evaluated against a panel of susceptible and resistant Gram-positive and selected Gram-negative bacteria. Substitution with 5-membered heteroaroyl and dinitrobenzoyl moieties potentiated the activity against staphylococcal and enterococcal strains. Compounds having dinitrobenzoyl 7n,o and 5-nitrofuroyl 7t substitutions were more potent than linezolid against M. catarrhalis. Substitution of water-solubilizing functionalities at the 4N-piperazine position resulted in compounds devoid of antibacterial activity.

    6. Novel Pyrazole and Indazole Derivatives: Synthesis and Evaluation of Their Anti-Proliferative and Anti-Angiogenic Activities (pages 804–811)

      Evangelia Tzanetou, Sandra Liekens, Konstantinos M. Kasiotis, Nikolas Fokialakis and Serkos A. Haroutounian

      Article first published online: 18 JUN 2012 | DOI: 10.1002/ardp.201200057

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      The synthesis of several novel pyrazole and indazole derivatives from ketonic substrates is reported. The novel compounds containing the indazole structural framework exhibit potent cytostatic properties against all cell lines tested, exemplified by compound 13 with an IC50 value of 1.5 ± 0.4 µM against MCF-7 cells. In addition, the indazole derivative 16 was assessed as a potent inhibitor of endothelial tube formation at 30 µM.

    7. Synthesis and Biological Evaluation of Novel 6-Hydrazinyl-2,4-bismorpholino pyrimidine and 1,3,5-Triazine Derivatives as Potential Antitumor Agents (pages 812–821)

      Wufu Zhu, Yajing Liu, Yanfang Zhao, Haiyan Wang, Li Tan, Weijie Fan and Ping Gong

      Article first published online: 18 JUN 2012 | DOI: 10.1002/ardp.201200074

      Thumbnail image of graphical abstract

      A series of 6-hydrazinyl-2,4-bismorpholino pyrimidine and 1,3,5-triazine derivatives were synthesized and evaluated for their biological activity. The most promising compound 5j showed strong antiproliferative activity against H460, HT-29, and MDA-MB-231 cell lines with IC50 values of 0.05, 6.31, and 6.50 µM, which were 4.6- to 190.4-fold more active than reference compound 1, respectively. However, compound 5j exhibited weaker potency against mTOR than compound 1. Further studies on the mechanism of action are in progress.

  3. Short Communication

    1. Top of page
    2. Contents
    3. Full Papers
    4. Short Communication
    5. Full Paper
    1. A Novel Approach to the Pyridoacridine Ring System: Synthesis of the Topoisomerase Inhibitor 13-Deazaascididemin (pages 822–826)

      Stephan Raeder and Franz Bracher

      Article first published online: 4 JUL 2012 | DOI: 10.1002/ardp.201200019

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      Starting from 3-cyano-4-methylquinoline, a sequence of homolytic benzoylation, annulation of a bromopyridine ring, and radical cyclization opens a new approach to AK37, a deaza analogue of the marine pyridoacridine alkaloid ascididemin.

  4. Full Paper

    1. Top of page
    2. Contents
    3. Full Papers
    4. Short Communication
    5. Full Paper
    1. Synthesis and Pharmacological Investigation of 2-(4-Dimethylaminophenyl)-3,5-disubstituted thiazolidin-4-ones as Anticonvulsants (pages 827–833)

      Manavalan Senthilraja and Veerachamy Alagarsamy

      Article first published online: 26 JUL 2012 | DOI: 10.1002/ardp.201200126

      Thumbnail image of graphical abstract

      A new series of 2-(4-dimethylaminophenyl)-3-substituted thiazolidin-4-one-5-yl-acetyl acetamides/benzamides were synthesized starting from 3-substituted-2-(4-dimethylaminophenyl)-thiazolidin-4-one-5-yl-acetylchloride. The title compounds were investigated for their anticonvulsant activities. Compound 2-(4-dimethylaminophenyl)-3-phenylamino-thiazolidine-4-one-5-yl-acetylbenzamide (14) emerged as the most active compound of the series and as moderately more potent than the reference standard diazepam.

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