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Recently Published Articles
- Difluorophenylglycinols as New Modulators of Proteolytic Processing of Amyloid Precursor Proteins
Chia-Yu Chen, Yung-Feng Liao, Ming-Yun Chang and Ming-Kuan Hu
Article first published online: 11 DEC 2013 | DOI: 10.1002/ardp.201300283
A range of N-substituted (R)- and (S)-difluorophenylglycinols, structured on the amino alcohol framework, were explored by incorporating the arylsulfonyl moieties and various N-substituents. Compounds with effects on γ-secretase inhibition and ERK-mediated signaling pathways were evaluated on cell-based assays. The N-cyclopropylmethyl derivatives R-12c and R-13c showed modest γ-secretase inhibition and ERK-dependent activation.
- Synthesis and Biological Screening of Novel Indolalkyl Arenes Targeting the Serotonine Transporter
Claudia Ojeda-Gómez, Hernán Pessoa-Mahana, Patricio Iturriaga-Vásquez, Carlos David Pessoa-Mahana, Gonzalo Recabarren-Gajardo and Claudio Méndez-Rojas
Article first published online: 11 DEC 2013 | DOI: 10.1002/ardp.201300321
The affinities for the serotonin transporter of a new series of functionalized indolylalkylarenes 3–16(a and b) were investigated in vitro. With Ki values of 33.0, 48.0, and 17 nM, compounds 3b, 4b, and 5b, respectively, showed good binding affinities. The other synthesized compounds showed moderate or no affinity in the binding studies.
- Urantide Conformation and Interaction with the Urotensin-II Receptor
Diego Brancaccio, Antonio Limatola, Pietro Campiglia, Isabel Gomez-Monterrey, Ettore Novellino, Paolo Grieco and Alfonso Carotenuto
Article first published online: 4 DEC 2013 | DOI: 10.1002/ardp.201300269
Urantide, a human urotensin II antagonist, may have potential clinical value in the treatment of atherosclerosis. Here, the conformational preferences of urantide in DPC micelles were studied and a urantide/UT receptor (UTR) interaction model was developed, which can help the design of novel peptide and small-molecule UTR antagonists.
- Steroidomimetic Aminomethyl Spiroacetals as Novel Inhibitors of the Enzyme Δ8,7-Sterol Isomerase in Cholesterol Biosynthesis
Melanie Krojer, Christoph Müller and Franz Bracher
Article first published online: 4 DEC 2013 | DOI: 10.1002/ardp.201300296
Aminomethyl spiroacetals derived from Grundmann's ketone were identified as a new chemotype of inhibitors of human Δ8,7-sterol isomerase. In a second step, an equipotent but not cytotoxic tetraline analog was developed as potent inhibitor of cholesterol biosynthesis.
- Synthesis of Some Heterofunctionalized Penicillanic Acid Derivatives and Investigation of Their Biological Activities
Serpil Demirci, Ahmet Demirbas, Serdar Ulker, Sengul Alpay-Karaoglu and Neslihan Demirbas
Article first published online: 2 DEC 2013 | DOI: 10.1002/ardp.201300280
Synthesis of some penicillanic acid derivatives including several heterocyclic rings was performed and the biological activities of the synthesized compounds were investigated. Some of them were found to possess antimicrobial, anti-β-lactamase, antiurease, and/or antilipase activity.