Archiv der Pharmazie

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1. Archiv der Pharmazie 12/2011
  Article first published online: 1 DEC 2011 | DOI: 10.1002/ardp.201190011
Full Papers
1. Synthesis and Histamine H3 and H4 Receptor Activity of Conformationally Restricted Cyanoguanidines Related to UR-PI376 (pages 775–785)
  Roland Geyer and Armin Buschauer
  Article first published online: 11 OCT 2011 | DOI: 10.1002/ardp.201100144
  Conformationally constrained analogues of the human histamine H₄ receptor (hH₄R) agonist UR-PI376 were synthesized and investigated for their activity (agonism, antagonism) in [³⁵S]GTPγS assays on hH₄R compared to H₃ receptors (hH₃R) expressed in Sf9 insect cells. Cis- and trans-configured imidazolylcyclohexylcyanoguanidines show different hH₄R and hH₃R selectivities.
2. Synthesis and Biological Evaluation of Antifungal Activities of Novel 1,2-trans Glycosphingolipids (pages 786–793)
  Ning Ding, Wei Zhang, Guokai Lv and Yingxia Li
  Article first published online: 11 OCT 2011 | DOI: 10.1002/ardp.201000335
  Antifungal activities of 1,2-trans glycosphingolipids (GSL) were tested against three Candida species. The results indicated that the kind of sugar moiety affected their antifungal activities and selectivities. In addition, a carbamoyl group-modified GSL (T9) displayed strong antifungal activities against all three tested organisms.
3. Synthesis and Anti-Candida Potential of Certain Novel 1-[(3-Substituted-3-phenyl)propyl]-1H-imidazoles (pages 794–801)
  Mohamed Nabil Aboul-Enein, Aida Abd El-Sattar El-Azzouny, Mohamed Ibrahim Attia, Ola Ahmed Saleh and Amany Lotfy Kansoh
  Article first published online: 11 OCT 2011 | DOI: 10.1002/ardp.201000224
  The target compounds 1-[(3-aroyloxy-3-phenyl)propyl]-1H-imidazoles 5a–f were obtained in four steps starting from acetophenone 1 whereas 1-[(3-alkyl/aralkyl/phenyl-3-phenyl)propan-3-ol]-1H-imidazoles 5g–j were synthesized in three steps. Compounds 5b and 5c showed anti-Candida activity comparable to tioconazole and were more potent than miconazole.
4. Synthesis and In-Vitro Antimycobacterial Activity of Fluoroquinolone Derivatives Containing a Coumarin Moiety (pages 802–809)
  Qiang Guo, Ming-Liang Liu, Lian-Shun Feng, Kai Lv, Yan Guan, Hui-Yuan Guo and Chun-Ling Xiao
  Article first published online: 12 OCT 2011 | DOI: 10.1002/ardp.201000256
  A series of gatifloxacin, ciprofloxacin, and 8-OCH₃ ciprofloxacin coumarin derivatives was designed, synthesized, characterized and evaluated for their in-vitro activity. The activity of one compound (6) was found to be 2–8-fold more potent than the respective parent GTFX, CPFX, and 8-OCH₃ CPFX, indicating that the lipophilicity of the tested compounds is not the sole parameter affecting antimycobacterial activity.
5. Synthesis, Molecular Modelling and Biological Evaluation of 4-Amino-2(1H)-quinazolinone and 2,4(1H,3H)-Quinazolidone Derivatives as Antitumor Agents (pages 810–820)
  Stephanie Richter and Barbara Gioffreda
  Article first published online: 11 OCT 2011 | DOI: 10.1002/ardp.201000312
  A series of 6-benzoyl-, 6-arylthio- and 6-arylsulfonyl-4-amino-2(1H)-quinazolinones and -2,4(1H,3H)-quinazolinediones were prepared. They were evaluated in vitro for their cytotoxicity against the NCI-60 cancer cell lines.
6. Efficient Regioselective Three-Component Domino Synthesis of 3-(1,2,4-Triazol-5-yl)-1,3-thiazolidin-4-ones as Potent Antifungal and Antituberculosis Agents (pages 821–829)
  Serry A. El Bialy, Maria M. Nagy and Hamdy M. Abdel-Rahman
  Article first published online: 20 SEP 2011 | DOI: 10.1002/ardp.201100001
  A series of thiazolidinone derivatives was synthesized by using the three-component domino reaction. All compounds were evaluated against various microbial agents including Candida albicans A39, Aspergillus fumigatus (strain 168.95), and Mycobacterium tuberculosis H37Rv.
7. Synthesis of New Pyrroles of Potential Anti-Inflammatory Activity (pages 830–839)
  Mosaad S. Mohamed, Rehab Kamel and Samar S. Fathallah
  Article first published online: 29 SEP 2011 | DOI: 10.1002/ardp.201100056
  A series of heterocyclic compounds as potential anti-inflammatory agents was synthesized and evaluated. Several derivatives as, e.g., 6–11 showed a promising anti-inflammatory activity compared to ibuprofen.
Short Communication
1. Short Synthesis of Ethyl 3-(3-aminophenyl)propanoate (pages 840–842)
  Ulrike Nagel, Gregor Radau and Andreas Link
  Article first published online: 12 OCT 2011 | DOI: 10.1002/ardp.200900164
  Ethyl 3-(3-aminophenyl)propanoate, an important precursor of biologically active compounds, was prepared in a two-step procedure by means of Meldrum's acid in triethylammonium formate and stannous chloride in ethanol.