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Recently Published Articles
- Synthesis and Carbonic Anhydrase Isoenzymes Inhibitory Effects of Brominated Diphenylmethanone and Its Derivatives
Yasin Çetinkaya, Hülya Göçer, İlhami Gülçin and Abdullah Menzek
Article first published online: 6 MAR 2014 | DOI: 10.1002/ardp.201300349
Known and novel derivatives and the corresponding benzylic alcohols of (3,4-dimethoxyphenyl)(2,3,4-dimethoxyphenyl)methanone were synthesized and their inhibitory effects on the carbonic anhydrase (CA) isoenzymes I and II were investigated. Compound 10 had the highest inhibitory activity on human CA I (IC50 = 3.48 µM, Ki = 2.19 µM) whereas compound 5 was found to be the best inhibitor for human CA II (IC50 = 1.33 µM, Ki = 2.09 µM).
- Synthesis and Biological Evaluation of Substituted N-[3-(1H-Pyrrol-1-yl)methyl]-1,2,5,6-tetrahydropyridin-1-yl]benzamide/benzene Sulfonamides as Anti-Inflammatory Agents
Madhavi Gangapuram, Elizabeth Mazzio, Suresh Eyunni, Karam F. A. Soliman and Kinfe K. Redda
Article first published online: 2 MAR 2014 | DOI: 10.1002/ardp.201300379
The anti-inflammatory activities of 12 new substituted N-[3-(1H-pyrrol-1-yl)methyl]-1,2,5,6-tetrahydrobenzamide/benzene sulfonamides (9a–l) were investigated in murine BV-2 microglial cells. Only SO2-substituted tetrahydropyridine derivatives were effective at sub-lethal concentrations (IC50 values of 12.92–19.63 µM for 9i–k). Compound 9i also blocked the lipopolysaccharide-inducible nitric oxide synthase and attenuated the release of IL-1α, IL-10, and IL-6.
- Synthesis and Antitumor Activities of Some New N1-(Flavon-6-yl)amidrazone Derivatives
Almeqdad Y. Habashneh, Mustafa M. El-Abadelah, Malek A. Zihlif, Amer Imraish and Mutasem O. Taha
Article first published online: 24 FEB 2014 | DOI: 10.1002/ardp.201300326
A new series of N1-(flavon-6-yl)amidrazones were synthesized by reacting the hydrazonoyl chloride derived from 6-aminoflavone with the appropriate sec-cyclic amines. The N-morpholine derivative was the most active against two cancer cell lines. Docking studies revealed that this derivative fits and blocks the oncogenic tyrosine kinases bcr/abl and EGFR similar to the anticancer agent imatinib.
- Synthesis and Antitumor Activity of Some Substituted Indazole Derivatives
Najat Abbassi, El Mostapha Rakib, Hakima Chicha, Latifa Bouissane, Abdellah Hannioui, Cinzia Aiello, Rosaria Gangemi, Patrizio Castagnola, Camillo Rosano and Maurizio Viale
Article first published online: 19 FEB 2014 | DOI: 10.1002/ardp.201300390
Some new N-[6-indazolyl]arylsulfonamides were synthesized and screened against two human tumor cell lines, A2780 and A549. Most of the new compounds, and especially compounds 4 and 9, showed promising anticancer activities against both cell lines.
- Potent Biphalin Analogs with µ/δ Mixed Opioid Activity: In Vivo and In Vitro Biological Evaluation
Roberto Costante, Francesco Pinnen, Azzurra Stefanucci and Adriano Mollica
Article first published online: 19 FEB 2014 | DOI: 10.1002/ardp.201300380
Two non-hydrazine analogs of the potent opioid octapeptide biphalin were synthesized and their antinociceptive activities were evaluated through in vitro and in vivo bioassays. Compound 10 exhibited remarkable analgesic activity in the tail-flick test following i.t. administration in rats.