Archiv der Pharmazie

Cover image for Archiv der Pharmazie

January 2012

Volume 345, Issue 1

Pages 7–85

  1. Contents

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

      Version of Record online: 10 JAN 2012 | DOI: 10.1002/ardp.201290000

  2. Review Article

    1. Top of page
    2. Contents
    3. Review Article
    4. Full Papers
    5. Short Communication
    1. Small Molecule Inhibitors of Histone Acetyltransferases as Epigenetic Tools and Drug Candidates (pages 7–21)

      Silviya D. Furdas, Srinivasaraghavan Kannan, Wolfgang Sippl and Manfred Jung

      Version of Record online: 28 OCT 2011 | DOI: 10.1002/ardp.201100209

      Thumbnail image of graphical abstract

      Modulation of histone acetyltransferase activities as chromatin modifying enzymes involved in epigenetic regulation of transcription discloses targets for the development of novel epigenetics-derived treatment approaches. A number of natural products and synthetic compounds exhibit influence on the enzymatic activities of histone acetyltransferases due to inhibition or activation and hold therapeutical potential targeting deregulated acetylation-mediated regulatory mechanisms implicated in cancerogenesis and disease manifestation.

  3. Full Papers

    1. Top of page
    2. Contents
    3. Review Article
    4. Full Papers
    5. Short Communication
    1. Microwave-Assisted Synthesis, Hypolipidemic and Hypoglycemic Activity of Some Novel 2-(4-(2-Amino-6-(4-substituted phenyl)-pyrimidin-4-yl)-phenoxy)-2-methyl Propanoic Acid Derivatives (pages 22–27)

      Santosh N. Mokale, Rupali D. Elgire, Nikhil S. Sakle and Devanand B. Shinde

      Version of Record online: 11 NOV 2011 | DOI: 10.1002/ardp.201000229

      Thumbnail image of graphical abstract

      A novel series of aminopyrimidines containing the phenoxy isobutyric acid group as a pharmacophore was synthesized using conventional and microwave-assisted methods of synthesis. The synthesized compounds were evaluated for their hypolipidemic and hypoglycemic activities on high-fat diet-induced hyperlipidemia and hyperglycemia in male Sprague-Dawley rats.

    2. Does One Keto Group Matter? Structure-Activity Relationships of Glycyrrhetinic Acid Derivatives Modified at Position C-11 (pages 28–32)

      René Csuk, Stefan Schwarz, Ralph Kluge and Dieter Ströhl

      Version of Record online: 11 NOV 2011 | DOI: 10.1002/ardp.201000327

      Thumbnail image of graphical abstract

      It remains disputable whether the C11 keto group in glycyrrhetinic acid derivatives is the main reason for their apoptotic effect.

    3. N-(Imidazolidin-2-ylidene)-1-arylmethanamine Oxides: Synthesis, Structure and Pharmacological Evaluation (pages 33–42)

      Jarosław Saczewski, Alan Hudson, Shayna Laird, Apolonia Rybczyńska, Konrad Boblewski, Artur Lehmann, Daqing Ma, Mervyn Maze, Helena Watts and Maria Gdaniec

      Version of Record online: 14 NOV 2011 | DOI: 10.1002/ardp.201100028

      Thumbnail image of graphical abstract

      A series of N-(imidazolidin-2-ylidene)-1-arylmethanamine oxides (α-aminonitrones) was prepared and evaluated in vitro for their binding affinities to α-adrenergic and imidazoline receptors. The most potent compounds were tested in vivo for their cardiovascular and sedative-hypnotic effects in rats. The α-aminonitrone–α-iminohydroxylamine tautomerism and the structures of the products were studied using theoretical methods and single crystal X-ray crystallographic analysis

    4. Synthesis and Biological Evaluation of 4α/4β-Imidazolyl Podophyllotoxin Analogues as Antitumor Agents (pages 43–48)

      Hai Shang, Hong Chen, Dongmei Zhao, Xiaowei Tang, Yongfeng Liu, Li Pan and Maosheng Cheng

      Version of Record online: 28 SEP 2011 | DOI: 10.1002/ardp.201100094

      Thumbnail image of graphical abstract

      A series of podophyllotoxin analogues have been synthesized and evaluated for their cytotoxic activity on human cancer cell lines. Compound 12 exhibited remarkable cytotoxicity, demonstrating effects against all tumor cell lines, including the K562/ADM cell line.

    5. Synthesis and Cytotoxicity Studies of Novel 2-Hydrazonylpyrido[2,3-b]pyrazin-3(4H)-ones (pages 49–56)

      Guogang Zhang, Yajing Liu, Shuobing Wang, Chuan Zhou, Qingchang Huang and Ping Gong

      Version of Record online: 23 SEP 2011 | DOI: 10.1002/ardp.201100103

      Thumbnail image of graphical abstract

      A series of 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives was designed and synthesized. Preliminary structure–activity relationships suggested that compounds with 4-methoxyphenyl or 4-(trifluoromethoxy)phenyl groups on the N-4 position were generally more potent than those with an unsubstituted phenyl group.

    6. Design and Synthesis of Novel Diphenyl Oxalamide and Diphenyl Acetamide Derivatives as Anticonvulsants (pages 57–64)

      Anna Pratima G. Nikalje, Mangesh Ghodke and Amol Girbane

      Version of Record online: 23 SEP 2011 | DOI: 10.1002/ardp.201100108

      Thumbnail image of graphical abstract

      A series of novel N1-substituted-N2,N2-diphenyl oxalamide and 2-substituted amino-N,N-diphenyl acetamide derivatives was synthesized and evaluated for their anticonvulsant, CNS depressant activity and neurotoxicity

    7. Synthesis and In-vivo Evaluation of Carbonyl-amide Linkage Based New Benzimidazole Derivatives (pages 65–72)

      Irfan N. Shaikh, Kallappa M. Hosamani, Harisha R. Seetharamareddy and Mallinath H. Hugar

      Version of Record online: 23 SEP 2011 | DOI: 10.1002/ardp.201100068

      Thumbnail image of graphical abstract

      One-pot synthesis of carbonyl-amide linkage based new benzimidazole derivatives as potent anti-inflammatory, anti-diabetic and anticonvulsant agents.

    8. Synthesis and Anticancer Activity of Indolin-2-one Derivatives Bearing the 4-Thiazolidinone Moiety (pages 73–80)

      Shuobing Wang, Yanfang Zhao, Wufu Zhu, Ying Liu, Kaixing Guo and Ping Gong

      Version of Record online: 20 SEP 2011 | DOI: 10.1002/ardp.201100082

      Thumbnail image of graphical abstract

      A novel series of indolin-2-one derivatives containing the 4-thiazolidinone moiety (5a-5p) was synthesized and evaluated in vitro against three human cancer cell lines (HT-29, H460 and MDA-MB-231). The promising compound 5h showed remarkable cytotoxicity and selectivity against HT-29 and H460 cancer cell lines (IC50 = 0.016 µmol/L, 0.0037 µmol/L, respectively)

  4. Short Communication

    1. Top of page
    2. Contents
    3. Review Article
    4. Full Papers
    5. Short Communication
    1. An Efficient Synthesis of Aripiprazole, Buspirone and NAN-190 by the Reductive Alkylation of Amines Procedure (pages 81–85)

      Piotr Kowalski and Jolanta Jaśkowska

      Version of Record online: 5 OCT 2011 | DOI: 10.1002/ardp.201100112

      Thumbnail image of graphical abstract

      The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, buspirone 1b, and NAN-190 1c.

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