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- Volume 17, Issue 32, 2011
Current Pharmaceutical Design - Volume 17, Issue 32, 2011
Volume 17, Issue 32, 2011
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Editorial [Hot Topic: Prodrugs: Pharmaceutical Design and Current Perspectives (Executive Guest Editor: Josef Jampilek)]
More LessProdrug approaches become more and more important due to undesirable properties (poor bioavailability) of modern potential drugs. This problem can be solved by optimization of physico-chemical, biopharmaceutical or pharmacokinetic properties of the molecule, i.e. by design of prodrugs. Prodrugs are typically developed to overcome pharmaceutical, pharmacokinetic, and pharmacodynamic barriers. They are designed to Read More
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L-Dopa Prodrugs: An Overview of Trends for Improving Parkinson's Disease Treatment
Authors: Antonio Di Stefano, Piera Sozio, Laura Serafina Cerasa and Antonio IannitelliL-Dopa is the mainstay of Parkinson's disease therapy; this drug is usually administered orally, but it is extensively metabolized in the gastrointestinal tract, so that relatively little arrives in the bloodstream as intact L-Dopa. The peripheral conversion of L-Dopa by amino acid decarboxylase to dopamine is responsible for the typical gastrointestinal and cardiovascular side effects. To minimize the conversion to Read More
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Salicylanilide Ester Prodrugs as Potential Antimicrobial Agents - a Review
Authors: Martin Kratky and Jarmila VinsovaSalicylanilides have been a subject of interest in medicinal chemistry as a group with a wide range of biological activities. The antibacterial (including antimycobacterial) and antifungal activities have come to be viewed as very significant. The synthesis of new prodrugs to counter a number of problematic properties of salicylanilides is a current trend. This article brings together the known basic facts about these pro Read More
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Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives
Authors: Martin Dolezal, Diana Kesetovic and Jan ZitkoDesign, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from Nphenylpyrazine- 2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting >50% inhibition in the prima Read More
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A Prodrug Approach to Improve the Physico-Chemical Properties and Decrease the Genotoxicity of Nitro Compounds
Authors: Man Chin Chung, Priscila Longhin Bosquesi and Jean Leandro dos SantosIn therapeutics research, the nitro compounds are part of an important group of drugs with multiple pharmacological activities. However, in drug design, the inclusion of a nitro group in a molecule changes the physico-chemical and electronic properties and is associated with increased mutagenicity and carcinogenicity. In addition, several studies have related the relationship between the antimicrobial and/or anti-protoz Read More
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Prodrugs for Targeted Tumor Therapies: Recent Developments in ADEPT, GDEPT and PMT
Authors: Lutz F. Tietze and Kianga SchmuckThe treatment of cancer with common anti-proliferative agents generally suffers from an insufficient differentiation between normal and malignant cells which results in extensive side effects. To enhance the efficacy and reduce the normal tissue toxicity of anticancer drugs, numerous selective tumor therapies have emerged including the highly promising approaches ADEPT (Antibody-Directed Enzyme Prodrug Therapy), GDEPT Read More
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Prodrugs in Photodynamic Anticancer Therapy
Authors: Robert Musiol, Maciej Serda and Jaroslaw PolanskiPhotodynamic therapy (PDT), the concept of cancer treatment through the selective uptake of a light-sensitive agent followed by exposure to a specific wavelength, is limited by the transport of a photosensitizer (PS) to the tumor tissue. Porphyrin, an important PS class, can be used in PDT in the form of its prodrug molecule 5-aminolevulinic acid (5-ALA). Unfortunately, its poor pharmacokinetic properties make this compound Read More
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Prodrugs and Endogenous Transporters: Are They Suitable Tools for Drug Targeting into the Central Nervous System?
Authors: Barbara Pavan and Alessandro DalpiazHydrophilic drugs, or neuroactive agents characterized by high molecular weight, do not have the physico-chemical properties required for passive diffusion across the blood brain barrier (BBB). The prodrug approach by lipidization of hydrophilic drugs generally allows to sensibly increase their permeability across BBB, even if this phenomenon is often not associated to an effective entry into the brain of the lipidized drugs. It has Read More
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Recent Advances in the Design and Synthesis of Prednisolone and Methylprednisolone Conjugates
Authors: Eliska Bilkova, Ales Imramovsky and Milos SedlakGlucocorticoid drugs are commonly used in the treatment of many acute and chronic inflammatory diseases. However, application of these steroids is limited because of their physico-chemical properties, such as very low water solubility. Glucocorticoids also exhibit serious adverse side effects. Therefore, new drug delivery systems are being developed, with the aim of improving the physicochemical properties of glucoc Read More
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Chitosan Derivatives with Antimicrobial, Antitumour and Antioxidant Activities - a Review
Authors: Jarmila Vinsova and Eva VavrikovaChitosan is a linear polysaccharide with a good biodegradability, biocompatibility, and no toxicity, which provide it with huge potential for future development. The chitosan molecule appears to be a suitable polymeric complex for many biomedical applications. This review gathers current findings on the antibacterial, antifungal, antitumour and antioxidant activities of chitosan derivatives and concurs with our previous revie Read More
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Volumes & issues
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Volume 31 (2025)
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Volume 30 (2024)
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Volume 29 (2023)
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Volume 28 (2022)
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Volume 27 (2021)
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Volume 26 (2020)
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Volume 25 (2019)
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Volume 24 (2018)
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Volume 23 (2017)
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Volume 22 (2016)
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Volume 21 (2015)
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Volume 20 (2014)
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Volume 19 (2013)
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Volume 18 (2012)
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Volume 17 (2011)
- Issue 38
- Issue 37
- Issue 36
- Issue 35
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- Issue 32
- Issue 31
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- Issue 12
- Issue 11
- Issue 10
- Issue 9
- Issue 8
- Issue 7
- Issue 6
- Issue 5
- Issue 4
- Issue 3
- Issue 2
- Issue 1
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Volume 16 (2010)
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Volume 15 (2009)
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Volume 14 (2008)
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Volume 13 (2007)
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Volume 12 (2006)
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Volume 11 (2005)
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Volume 10 (2004)
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Volume 9 (2003)
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Volume 8 (2002)
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Volume 7 (2001)
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Volume 6 (2000)
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