Archiv der Pharmazie

Cover image for Archiv der Pharmazie

September 2012

Volume 345, Issue 9

Pages 677–752

  1. Contents

    1. Top of page
    2. Contents
    3. Full Papers
    1. Archiv der Pharmazie 9/2012

      Version of Record online: 10 SEP 2012 | DOI: 10.1002/ardp.201290009

  2. Full Papers

    1. Top of page
    2. Contents
    3. Full Papers
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      1,2,4-Trisubstituted Cyclopentanes as Platforms for Diversity (pages 677–686)

      Yousheng Guan, Caterina Bissantz, Donald E. Bergstrom and Andreas Link

      Version of Record online: 4 JUL 2012 | DOI: 10.1002/ardp.201200101

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      Towards the systematic exploration of chemical space: A series of trisubstituted cyclopentane derivatives were synthesized and are suggested as platforms for diversity. Positioning of substituents on the ring enables the efficient construction of libraries of natural product mimetics and drug-like compounds.

    2. Ligand-Based Design, Synthesis, and Pharmacological Evaluation of 3-Methoxyquinoxalin-2-carboxamides as Structurally Novel Serotonin Type-3 Receptor Antagonists (pages 687–694)

      Radhakrishnan Mahesh, Thangaraj Devadoss, Arghya Kusum Dhar, Sudali Muthu Venkatesh, Sourabh Mundra, Dilip Kumar Pandey, Shvetank Bhatt and Ankur Kumar Jindal

      Version of Record online: 6 JUN 2012 | DOI: 10.1002/ardp.201200038

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      The design, synthesis, and 5-HT3 receptor antagonistic activities of 3-methoxyquinoxalin-2-carboxamides are described. Compounds 6a (pA2 7.2), 6e (pA2 7.0), 6f (pA2 7.5), 6g (pA2 7.5), 6n (pA2 7.0), and 6o (pA2 7.2) exhibited increased antagonism compared to that of the standard 5-HT3 antagonist, ondansetron (pA2 6.9).

    3. Synthesis and Evaluation of Human Monoamine Oxidase Inhibitory Activities of Some 3,5-Diaryl-N-substituted-4,5-dihydro-1H-pyrazole-1-carbothioamide Derivatives (pages 695–702)

      Kerem Şentürk, Oya Unsal Tan, Samiye Yabanoğlu Çiftçi, Gülberk Uçar and Erhan Palaska

      Version of Record online: 5 JUN 2012 | DOI: 10.1002/ardp.201100448

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      A series of novel 3-aryl-5-(4-fluorophenyl)-N-substituted-4,5-dihydro-1H-pyrazole-1-carbothioamide derivatives was designed and synthesized. 5-(4-Fluorophenyl)-3-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide was found to be the most potent and selective monoamine oxidase inhibitor.

    4. Synthesis of Some Azoles Incorporating a Sulfonamide Moiety as Anticonvulsant Agents (pages 703–712)

      Awatef A. Farag, Safaa N. Abd-Alrahman, Gihan F. Ahmed, Ramy M. Ammar, Yousry A. Ammar and Samir Y. Abbas

      Version of Record online: 14 JUN 2012 | DOI: 10.1002/ardp.201200014

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      Many heterocyclic compounds containing a sulfonamide thiazole moiety were synthesized. For 15 of these compounds, the anticonvulsant activity was evaluated and 6 compounds showed protection against picrotoxin-induced convulsion. 4-(6-Amino-3,5-dicyano-4-(4-methoxyphenyl)-2-oxopyridin-1(2H)-yl)-N-(thiazol-2-yl)benzenesulfonamide (11b) exhibited significant anticonvulsive effects and abolished the tonic extensor phase, offering 100% protection.

    5. Synthesis and Anticonvulsant Properties of New Mannich Bases Derived from 3,3-Disubstituted Pyrrolidine-2,5-diones. Part IV (pages 713–722)

      Jolanta Obniska, Iwona Chlebek and Krzysztof Kamiński

      Version of Record online: 6 JUN 2012 | DOI: 10.1002/ardp.201200092

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      The majority of compounds showed high activity in the maximal electroshock (MES) test, which is an animal model of human generalized tonic–clonic seizures. Several compounds were also effective in the 6-Hz screen known as a model of human partial and therapy resistant epilepsy.

    6. The MIA-QSAR Method for the Prediction of Bioactivities of Possible Acetylcholinesterase Inhibitors (pages 723–728)

      Michelle Bitencourt, Matheus P. Freitas and Roberto Rittner

      Version of Record online: 6 JUN 2012 | DOI: 10.1002/ardp.201200079

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      MIA-QSAR methodology, a method capable of relating chemical structures with their biological activities, was used to study a class of acetylcholinesterase inhibitors. Three new compounds exhibiting high estimated pIC50 values were found, which may be promising inhibitors in the treatment of Alzheimer's disease.

    7. New Pyrimidinone and Fused Pyrimidinone Derivatives as Potential Anticancer Chemotherapeutics (pages 729–738)

      Aymn E. Rashad, Ahmed H. Shamroukh, Nabil M. Yousif, Mowafia A. Salama, Hatem S. Ali, Mamdouh M. Ali, Abeer E. Mahmoud and Mahmoud El-Shahat

      Version of Record online: 6 JUN 2012 | DOI: 10.1002/ardp.201200119

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      A series of novel substituted pyrimidinones and fused pyrimidinones were synthesized starting with oxiranylmethanone 2. Most of the tested compounds showed potent cytotoxic activity against the MCF-7 cell line, comparable to the activity of the anticancer drug cisplatin. In the MCF-7 cells treated with the tested compounds, the activity of superoxide dismutase and the level of hydrogen peroxide were significantly increased, while the activities of catalase and glutathione peroxidase and the levels of reduced glutathione were significantly lowered. Derivatives 11 and 16 revealed the highest anticancer activity.

    8. Antimycobacterial Activity of Pyrimido[4,5-b]diazepine Derivatives (pages 739–744)

      Braulio Insuasty, Angélica García, Juan Bueno, Jairo Quiroga, Rodrigo Abonia and Alejandro Ortiz

      Version of Record online: 25 JUN 2012 | DOI: 10.1002/ardp.201100433

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      Three series of novel 8,9-dihydro-7H-pyrimido[5,4-b][1,4]diazepines, 4ad, 5ad, and 7ad, were obtained in good yields using simple reaction methodologies. The new pyrimidodiazepines were evaluated against 15 Mycobacterium spp. strains. Moderate inhibitory activity on 13 microorganisms was obtained for compounds 4a, 5a, 5c, and 5d.

    9. Synthesis and Antioxidant Activity of a New Class of Bis and Tris Heterocycles (pages 745–752)

      Venkatapuram Padmavathi, Bhumireddy Chinnachennaiahgari Venkatesh, Akkarapalli Muralikrishna and Adivireddy Padmaja

      Version of Record online: 16 MAY 2012 | DOI: 10.1002/ardp.201100361

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      A series of novel heterocycles, bisbenzoxazolyl/benzothiazolyl/benzimidazolyl pyrazoles/isoxazoles/pyrimidines, were synthesized and evaluated for their antioxidant activity. The bisbenzoxazolylisoxazole 10 exhibited good antioxidant activity when compared with the standard ascorbic acid.