Archiv der Pharmazie

Cover image for Archiv der Pharmazie

April 2012

Volume 345, Issue 4

Pages 257–334

  1. Contents

    1. Top of page
    2. Contents
    3. Full Papers
    1. Archiv der Pharmazie 4/2012

      Version of Record online: 10 APR 2012 | DOI: 10.1002/ardp.201290004

  2. Full Papers

    1. Top of page
    2. Contents
    3. Full Papers
    1. Design and Synthesis of New 1,3-Benzdiazinan-4-one Derivatives as Selective Cyclooxygenase (COX-2) Inhibitors (pages 257–264)

      Afshin Zarghi, Tannaz Zebardast, Fatemeh Hajighasemali, Eskandar Alipoor, Bahram Daraie and Mehdi Hedayati

      Version of Record online: 11 NOV 2011 | DOI: 10.1002/ardp.201100138

      Thumbnail image of graphical abstract

      A new group of regioisomeric 2,3-diaryl-1,3-benzdiazinan-4-ones, possessing a methyl sulfonyl pharmacophore, were synthesized and their biological activities were tested for cyclooxygenase-2 (COX-2) inhibitory activity. In vitro COX-1/COX-2 inhibition studies identified 3-(p-fluorophenyl)-2-(4-methylsulfonylphenyl)-1,3-benzdiazinane-4-one (2b) as a potent and highly selective (IC50 = 0.07 µM; selectivity index = 572.8) COX-2 inhibitor.

    2. Comparative Structural Analysis of α-Glucosidase Inhibitors on Difference Species: A Computational Study (pages 265–274)

      N. S. Hari Narayana Moorthy, Maria J. Ramos and Pedro A. Fernandes

      Version of Record online: 18 OCT 2011 | DOI: 10.1002/ardp.201100047

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      Structural feature analyses of chlorogenic acid derivatives with alkyl groups of varying lengths as α-glucosidase inhibitors were performed by QSAR techniques. The statistically significant models derived from the study were validated by leave-one-out, Y-randomization and test set methods. The predictive capacity of the models was assessed by their validation parameters, such as cross-validated correlation coefficients (Q2) and predictive residual analysis.

    3. Synthesis of 1-Substituted 3-Aryl-5-aryl(hetaryl)-2-pyrazolines and Study of Their Antitumor Activity (pages 275–286)

      Braulio Insuasty, Leidy Chamizo, Jhon Muñoz, Alexis Tigreros, Jairo Quiroga, Rodrigo Abonía, Manuel Nogueras and Justo Cobo

      Version of Record online: 22 NOV 2011 | DOI: 10.1002/ardp.201100170

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      Three series of novel 1,3,5-trisubstituted 2-pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. 5-(Benzo[d][1,3]dioxol-5-yl)-3-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (9a) shows remarkable activity toward leukemia, renal cancer and prostate cancer cell lines with GI50 values of 1.88, 1.91 and 1.94 µM, respectively.

    4. Synthesis and Cytotoxic Evaluation of Some New Phthalazinylpiperazine Derivatives (pages 287–293)

      Yajing Liu, Shulan Zhang, Ye Li, Jianqiang Wang, Yu Song and Ping Gong

      Version of Record online: 18 OCT 2011 | DOI: 10.1002/ardp.201100250

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      A new series of 1,4-disubstituted phthalazinylpiperazine derivatives 7a–f, 12a–f and 20a–f were designed and synthesized, and their cytotoxic activities against A549, HT-29 and MDA-MB-231 cancer cell lines in vitro were compared to that of vatalanib.

    5. Ultrasound-Assisted Synthesis of Novel α-Aminophosphonates and Their Biological Activity (pages 294–301)

      Syed Rasheed, Katla Venkataramana, Kuruva Chandrasekhar, Gemmalamadugu Fareeda and Chamarthi Naga Raju

      Version of Record online: 7 DEC 2011 | DOI: 10.1002/ardp.201100256

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      A new class of α-aminosubstituted phosphonates was synthesized and evaluated for their antimicrobial and antiviral activity.

    6. Synthesis and Antibacterial Activity of Novel Fused 1,3-Thiazoles and 1,3-Thiazines Incorporating a 2,4-Dihydroxyphenyl Residue (pages 302–313)

      Joanna Matysiak, Renata Los, Anna Malm, Monika M. Karpińska, Urszula Głaszcz, Barbara Rajtar, Małgorzata Polz-Dacewicz, Marta Trojanowska-Wesołowska and Andrzej Niewiadomy

      Version of Record online: 18 OCT 2011 | DOI: 10.1002/ardp.201100251

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      A series of benzothiazoles, 1,3-thiazolo[5,4-b]pyridines, 4H-3,1-benzothiazines, naphtho[2,3-d][1,3]thiazole-4,9-diones and other related compounds containing a 2,4-dihydroxyphenyl moiety were prepared and their MIC values towards eight reference bacterial strains were determined. 4-(6-Chloro-4H-3,1-benzothiazin-2-yl)-6-methylbenzene-1,3-diol may be regarded as a promising precursor for the development of novel antibacterial agents.

    7. Synthesis and Antimicrobial Evaluation of New Pyrano[4,3-b]pyran and Pyrano[3,2-c]chromene Derivatives Bearing a 2-Thiophenoxyquinoline Nucleus (pages 314–322)

      Jigar A. Makawana, Manish P. Patel and Ranjan G. Patel

      Version of Record online: 22 NOV 2011 | DOI: 10.1002/ardp.201100203

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      A new series of pyrano[4,3-b]pyran 4a–i and pyrano[3,2-c]chromene 6a–r derivatives bearing a 2-thiophenoxyquinoline nucleus were synthesized. All compounds were screened against three Gram-positive bacteria, three Gram-negative bacteria and two fungi. The majority of the compounds were found to be active against Bacillus subtilis, Clostridium tetani and Candida albicans as compared to standard drugs.

    8. Synthesis and Antioxidant Properties of (3,4-Dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone and Its Derivatives (pages 323–334)

      Yasin Çetinkaya, Hülya Göçer, Abdullah Menzek and İlhami Gülçin

      Version of Record online: 7 DEC 2011 | DOI: 10.1002/ardp.201100272

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      (3,4-Dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone (5) and its two derivatives with bromine were synthesized. 4-(3,4-Dihydroxybenzyl)benzene-1,2,3-triol and its dibromide derivative (16) were also synthesized. The in vitro antioxidant activities of nine new compounds were determined, showing that the synthesized bromophenols had effective antioxidant power. The phenol 5 with two phenolic rings and five phenolic hydroxyl groups was the most potent antioxidant and radical scavenger.