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- Volume 2, Issue 3, 2005
Current Drug Discovery Technologies - Volume 2, Issue 3, 2005
Volume 2, Issue 3, 2005
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Reversible Covalent Chemistry in Drug Delivery
Authors: Kevin R. West and Sijbren OttoThe targeting of drugs specifically to their sites of action is an important strategy for increasing drug efficacy. Chemists have come up with many elegant schemes that aim to convert drugs into magic bullets. This review focuses on the chemistry that underlies these schemes, with particular emphasis on two types of cleavable covalent bonds that are frequently used to link drugs to their various carriers: disulfide bonds and h Read More
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Reverse Pharmacognosy: Application of Selnergy, a New Tool for Lead Discovery. The Example of ε-Viniferin
The aim of reverse pharmacognosy is to find new biological targets for natural compounds by virtual or real screening and identify natural resources that contain the active molecules. To demonstrate the applicability of this concept, we report here a study on εviniferin, an active ingredient for cosmetic development. Nevertheless, this natural substance is weakly defined in terms of biological properties. SELNERGY Read More
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Macromolecular and Nanotechnological Modification of Camptothecin and its Analogs to Improve the Efficacy
Authors: Hiraku Onishi and Yoshiharu MachidaCamptothecin (CPT) and its analogs are some of the most potent antitumor agents known. However, their poor water-solubility and high toxicity require changes of their physicochemical and biological characteristics. Active lactone forms have provoked interest in the utility of CPT and its analogs again. Macromolecular chemical modifications and nanotechnological formulations have been used to obtain improved systems Read More
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Application of the In Combo Screening Approach For the Discovery of Non-Alkaloid Acetylcholinesterase Inhibitors from Cichorium intybus
Authors: J. M. Rollinger, P. Mock, C. Zidorn, E. P. Ellmerer, T. Langer and H. StuppnerBecause of the direct correlation of cholinergic deficit and the severity of dementia, Alzheimer's disease is preferentially treated with acetylcholinesterase (AChE) inhibitors to supplement the acetylcholine level. In this study we focused on non-alkaloid AChE inhibitors from natural sources in order to discover new lead structures. In the course of in vitro extract screening of Tyrolean plants using an enzyme assay wit Read More
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Artificial Neural Networks to Optimize Formulation Components of a Fixed- Dose Combination of Rifampicin, Isoniazid and Pyrazinamide in a Microemulsion
Authors: B. D. Glass, S. Agatonovic-Kustrin and M. H. WischThe aim of this study to design a stable microemulsion formulation to deliver a combination of rifampicin, isoniazid and pyrazinamide in quantities suitable for administration to a paediatric population. The chemical stability of rifampicin, isoniazid and pyrazinamide alone and in various combinations was investigated in different solvents, solubilizing agents and surfactants. An artificial neural network was used to model d Read More
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Volumes & issues
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Volume 22 (2025)
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Volume 21 (2024)
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Volume 20 (2023)
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Volume 19 (2022)
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Volume 18 (2021)
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Volume 17 (2020)
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Volume 16 (2019)
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Volume 15 (2018)
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Volume 14 (2017)
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Volume 13 (2016)
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Volume 12 (2015)
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Volume 11 (2014)
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Volume 10 (2013)
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Volume 9 (2012)
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Volume 8 (2011)
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Volume 7 (2010)
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Volume 6 (2009)
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Volume 5 (2008)
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Volume 4 (2007)
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Volume 3 (2006)
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Volume 2 (2005)
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Volume 1 (2004)
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