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Recently Published Articles
- Ultrasound-Assisted Synthesis, Anticonvulsant Activity, and Docking Study of Indole-Appended Thiazolidin-4-ones
Anna Pratima G. Nikalje, Sameer I. Shaikh, Abhineet Mulay, Firoz A. K. Khan, Jaiprakash N. Sangshetti and Shoaib Shaikh
Article first published online: 24 JUL 2014 | DOI: 10.1002/ardp.201400148
Novel indolyl thiazolidin-4-ones were designed and evaluated for their anticonvulsant and behavioral activities. Molecular docking studies, distance mapping, and prediction of the ADME properties were performed. 3-(2-Hydroxyphenyl)-2-(1H-indol-3-yl)thiazolidin-4-one at 100 mg/kg showed protection in the MES and sc-PTZ models and was found to decrease the behavioral activity in mice when compared to diazepam.
- Novel Ametantrone–Amsacrine Related Hybrids as Topoisomerase IIβ Poisons and Cytotoxic Agents
Giuseppe Zagotto, Alessandra Gianoncelli, Claudia Sissi, Cristina Marzano, Valentina Gandin, Riccardo Pasquale, Giovanni Capranico, Giovanni Ribaudo and Manlio Palumbo
Article first published online: 17 JUL 2014 | DOI: 10.1002/ardp.201400111
The structural requirements for cleavable complex stabilization by topoisomerase II poisons are still poorly understood. To better define a pharmacophoric pattern, several conjugates were prepared combining the chemical features of two well-known topoisomerase II poisons, amsacrine and ametantrone. Neither the planar chromophore nor the side chains alone are able to direct the strength of the interaction between the small molecule and the macromolecular complex.
- Vanillin Analog – Vanillyl Mandelic Acid, a Novel Specific Inhibitor of Snake Venom 5′-Nucleotidase
Raghaven Arun, Abdul Salam Syed Yasir Arafat, Cletus J. M. D'Souza, Venkatabalasubramanian Sivaramakrishnan and Bhadrapura Lakkappa Dhananjaya
Article first published online: 15 JUL 2014 | DOI: 10.1002/ardp.201400069
For the first time, vanillin mandelic acid (VMA), an analog of vanillin, is reported to potentially, selectively, and specifically inhibit the activity of snake venom 5′-nucleotidase (sv5′NUC). VMA can be used as a molecular tool to evaluate the role of 5′NUC in snake envenomation and to develop prototypes and lead compounds with potential therapeutic applications against snake bites.
- Gypsogenin Derivatives: An Unexpected Class of Inhibitors of Cholinesterases
Lucie Heller, Stefan Schwarz, Björn A. Weber and René Csuk
Article first published online: 8 JUL 2014 | DOI: 10.1002/ardp.201400103
Gypsogenin (1) is a highly functionalized molecule. Several derivatives of 1 were prepared and investigated for their potential as cholinesterase inhibitors. (3β,4α) 3-O-Acetyl-olean-12-ene-23,28-dinitrile (11) was shown to be a potent, non-cytotoxic triterpenoid acetylcholinesterase inhibitor, with a Ki value of 2.67 ± 0.59 μM.
- Synthesis, Cytotoxicity, Docking Study, and Tubulin Polymerization Inhibitory Activity of Novel 1-(3,4-Dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxanilides
Omar M. Aly, Eman A. Beshr, Raed M. Maklad, Muhamad Mustafa and Amira M. Gamal-Eldeen
Article first published online: 3 JUL 2014 | DOI: 10.1002/ardp.201400096
Novel 1-(3,4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-1,2,4-triazole-3-carboxylic acid derivatives (4a–n) were synthesized. With IC50 values of 7.79, 10.79, and 13.20 µM, the anilides of m-anisidine 4e, o-anisidine 4f, and 3,5-difluoroaniline 4l showed best cytotoxic activity on MCF-7 cells. In docking studies, compounds 4d, 4e, 4f, and 4l interacted with several amino acids in the colchicine binding site of β-tubulin.