Archiv der Pharmazie

Cover image for Archiv der Pharmazie

January 2013

Volume 346, Issue 1

Pages 7–82

  1. Contents

    1. Top of page
    2. Contents
    3. Full Paper
    4. Short Communication
    5. Full Papers
    1. You have free access to this content
      Archiv der Pharmazie 1/2013

      Version of Record online: 11 JAN 2013 | DOI: 10.1002/ardp.201390000

  2. Full Paper

    1. Top of page
    2. Contents
    3. Full Paper
    4. Short Communication
    5. Full Papers
    1. Design and Synthesis of Aza-Flavones as a New Class of Xanthine Oxidase Inhibitors (pages 7–16)

      Rajni Dhiman, Sahil Sharma, Gagandip Singh, Kunal Nepali and Preet Mohinder Singh Bedi

      Version of Record online: 18 OCT 2012 | DOI: 10.1002/ardp.201200296

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      To develop non-purine-based xanthine oxidase inhibitors, the flavone framework was used as lead structure for further optimization. By means of structure-based classical bioisosterism, quinolone was used as an isoster for chromone. This type of replacement does not alter the shape and structural features required for xanthine oxidase inhibition. The rationally designed and synthesized series of 2-aryl/heteroaryl-4-quinolones (aza analogs of flavones) was evaluated for in vitro xanthine oxidase inhibitory activity.

  3. Short Communication

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    4. Short Communication
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    1. Synthesis and Selective Human Monoamine Oxidase B Inhibition of Heterocyclic Hybrids Based on Hydrazine and Thiazole Scaffolds (pages 17–22)

      Simone Carradori, Melissa D'Ascenzio, Celeste De Monte, Daniela Secci and Matilde Yáñez

      Version of Record online: 15 OCT 2012 | DOI: 10.1002/ardp.201200318

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      The hydrazothiazole scaffold has been designed combining the hydrazide moiety of iproniazid and the thiazole nucleus of glitazones, a class of peroxisome proliferator-activated receptor γ agonists recently co-crystallized with human monoamine oxidase B (hMAO-B). The resulting derivatives were assayed to evaluate their in vitro inhibitory activity against both the A and B isoforms of hMAO. All compounds were shown to be selective and potent hMAO-B inhibitors in the low micromolar/high nanomolar range.

  4. Full Papers

    1. Top of page
    2. Contents
    3. Full Paper
    4. Short Communication
    5. Full Papers
    1. Design of Novel β-Carboline Derivatives with Pendant 5-Bromothienyl and Their Evaluation as Phosphodiesterase-5 Inhibitors (pages 23–33)

      Dalia S. El-Gamil, Nermin S. Ahmed, Bernard D. Gary, Gary A. Piazza, Matthias Engel, Rolf W. Hartmann and Ashraf H. Abadi

      Version of Record online: 19 OCT 2012 | DOI: 10.1002/ardp.201200334

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      New derivatives with the tetrahydro-β-carboline-imidazolidinedione and tetrahydro-β-carboline-piperazinedione scaffolds and a pendant bromothienyl moiety at C-5/C-6 were synthesized and tested for their ability to inhibit PDE5 in vitro. Of these, 13 derivatives showed PDE5 inhibitory activity with IC50 values in the range of 0.16–5.4 µm and with compound 8 being the most active derivative. The tetracyclic scaffold was shown to be essential for PDE5 inhibition.

    2. Synthesis and Biological Evaluation of New Bischromone Derivatives with Antiproliferative Activity (pages 34–43)

      Agata Szulawska-Mroczek, Marta Szumilak, Malgorzata Szczesio, Andrzej Olczak, Ryszard B. Nazarski, Wieslawa Lewgowd, Malgorzata Czyz and Andrzej Stanczak

      Version of Record online: 26 OCT 2012 | DOI: 10.1002/ardp.201200220

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      New bischromone derivatives resulting in two different product groups (compounds 4ac and 5ac) are described as potential anticancer drugs. N,N′-[(Methylimino)dipropane-3,1-diyl]bis(4-oxo-4H-chromene-3-carboxamide) 4a and (3,3′)-3,3′-{(methylimino)bis[propane-3,1-diyliminomethylylidene]}bis(2H-chromene-2,4(3H)-dione) 5a were evaluated in vitro in the highly aggressive melanoma cell line A375, with 5a showing higher potency in the induction of apoptosis and cell cycle arrest. Compound 5a was also more active in diminishing the adhesive potential of melanoma cells.

    3. Novel Dithiocarbamic Acid Esters Derived from 6-Aminomethyl-4-anilinoquinazolines and 6-Aminomethyl-4-anilino-3-cyanoquinolines as Potent EGFR Inhibitors (pages 44–52)

      Xin Zhang, Ridong Li, Kang Qiao, Zemei Ge, Liangren Zhang, Tieming Cheng and Runtao Li

      Version of Record online: 25 NOV 2012 | DOI: 10.1002/ardp.201200267

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      Two series of dithiocarbamic acid esters were designed and synthesized. Compound 14d was found to have higher biological activity than lapatinib. Some useful structure–activity relationships were revealed.

    4. Synthesis and Pharmacological Screening of Novel meso-Substituted Porphyrin Analogs (pages 53–61)

      Ahmed A. Fadda, Rasha E. El-Mekawy, Ahmed I. El-Shafei and Harold Freeman

      Version of Record online: 22 NOV 2012 | DOI: 10.1002/ardp.201200313

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      A newly synthesized series of mesotetrakis[aryl]-21H,23H-porphyrin derivatives 2aj was considered as a model to study the free radical-induced damage of biological membranes and the protective effects of these porphyrins. Compounds 2c and 2d bearing a sulfur atom, a nitro group, and a chlorine atom exhibited markedly higher antihemolysis activity than the other analogs. Compounds 2a, 2c, 2d, and 2j showed the highest protection activity against DNA damage.

    5. Biological Evaluation of Androstene Derivatives (pages 62–70)

      Mariana Garrido, Eugene Bratoeff, Mario García-Lorenzana, Yvonne Heuze, Juan Soriano, Norma Valencia, Francisco Cortes and Marisa Cabeza

      Version of Record online: 4 DEC 2012 | DOI: 10.1002/ardp.201200335

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      The binding of several new dihydroepiandrosterone ester derivatives A2A6 to the progesterone receptor (PR) was evaluated. A1 binds to the PR and inhibits the ovulation in female cycling mice stimulated with luteinizing hormone-releasing hormone. A6 binds to the PR with the highest affinity and induces a synergistic activity with progesterone. Furthermore, A6 inhibits ovulation in the same manner as A1. These results suggest that A1 and A6 block gonadotropin secretion.

    6. Synthesis and Anticonvulsant Properties of New N-Mannich Bases Derived from 3,3-Diphenyl- and 3-Ethyl-3-methyl-pyrrolidine-2,5-diones. Part III (pages 71–82)

      Jolanta Obniska, Iwona Chlebek, Krzysztof Kamiński and Janina Karolak-Wojciechowska

      Version of Record online: 25 NOV 2012 | DOI: 10.1002/ardp.201200265

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      Twenty-four new N-[(4-phenylpiperazin-1-yl)-methyl] derivatives of 3,3-diphenyl- (718) and 3-ethyl-3-methyl-pyrrolidine-2,5-dione (1930) were synthesized and evaluated for their anticonvulsant activity in the maximum electroshock (MES) and subcutaneous pentylenetetrazole seizure tests. Several of the compounds showed activity in the MES test, which is an animal model of human generalized tonic–clonic seizures. These molecules act as potent NaV1.2 sodium channel current blockers.

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