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Iminosugars form undoubtedly the most attractive of carbohydrate mimics reported so far. In these structures, the substitution of the endocyclic oxygen of sugars by a basic nitrogen atom leads to remarkable biological properties and raises many challenges in organic synthesis. Since the discovery of their biological activity as glycosidase inhibitors in the 1970’s, these polyvalent molecules have progressively made their way from the laboratory to the clinic. The impressive series of discoveries in the field over the past ten years indicates clearly that it is “a boom time” for iminosugar chemistry and biology. The scope of their profile as inhibitors has been extended to a number of enzymes such as phosphorylases, glycosyltransferases or metalloproteinases, and iminosugars now constitute lead compounds for the development of new therapeutic agents for a wide range of diseases including diabetes, viral infections, lysosomal storage disorders and tumor metastasis. Latest developments, from iminosugar synthesis to their use in clinical studies, are presented in this book, which contains contributions from over fifteen of the major chemists, biochemists and drug developers in this rapidly expanding field. An extensive table correlating the structures of more than 600 iminosugars of therapeutic interest with their biological activities is also included in the book and should prove particularly useful to aid with the design and the discovery of novel bioactive substances. Iminosugars: From Synthesis to Therapeutic Application provides a unique resource for academic and industrial researchers working in the field of iminosugars and glycomimetics of biological and/or therapeutic interest: organic chemists, medicinal chemists, carbohydrate chemists and medical scientists.
Iminosugars as Glycosidase Inhibitors Nojirimycin and Beyond Edited by Arnold E. Stutz "Nowadays as a result of these manifold synthetic efforts a large number of inhibitors are available, that can be applied selectively for many different glycosidases. They are important aids to explain the construction and degradation particularly of complex carbohydrate side chains such as those found in glycoproteins and glycolipids. The amount of chemical and biochemical information has meanwhile grown to such an extent that it is almost impossible to keep track of the developments. Therefore it is particularly pleasing that contributions from experts for the individual fields are collected together in one work, thus providing a comprehensive overview. In this way this book gives a representative cross-section of the field. The book will be a generally interesting source of information for chemists and biochemists." (From the foreword by H. Paulsen). A table which lists over 400 glycosidase inhibitors, more than 200 enzymes with 323 citations and over 1500 invaluable sets of data completes the book.
This book contains original papers and reviews on carbohydrate research in medicine, authored by participants of the 29th International Carbohydrate Symposium, where this topic had a special emphasis. The focus on biological events involving carbohydrates and glycoconjugates has delivered reliable approaches for disease treatment and diagnosis. Research on carbohydrate-based compounds for therapeutic applications is illustrated in various contributions, namely those covering the development of novel agents against Alzheimer’s disease, e.g. the neuroprotective C-glucosylated flavones and the isonucleoside-based cholinesterase inhibitors. New imino sugar glucosidase inhibitors are also disclosed, a class of compounds with potential for diabetes, Gaucher disease or cancer treatment. Also the development of a useful synthetic method towards multivalent glycoclusters of biomedical interest is here highlighted. The relevance of glycomimetics in drug discovery and the progress on carbohydrates in early diagnosis and cancer treatment are reviewed. Noteworthy is the chitosan-based delivery system for drug oral administration, a new biomaterial-based approach to improve bioavailability. Another study on the conformation of Streptococcus capsular polysaccharide backbones by molecular modelling provides useful information for bacterial immunotherapeutic approaches. All original contributions and reviews clearly demonstrate the potential of glycosciences for innovation in medicinal (glyco)chemistry and pharmaceutical research.
This volume provides a collection of contemporary perspectives on using activity-based protein profiling (ABPP) for biological discoveries in protein science, microbiology, and immunology. A common theme throughout is the special utility of ABPP to interrogate protein function and small-molecule interactions on a global scale in native biological systems. Each chapter showcases distinct advantages of ABPP applied to diverse protein classes and biological systems. As such, the book offers readers valuable insights into the basic principles of ABPP technology and how to apply this approach to biological questions ranging from the study of post-translational modifications to targeting bacterial effectors in host-pathogen interactions.
This contributed volume contains 25 chapters from leading international scientists working on dengue and Zika viruses, who came together in Praia do Tofo in Mozambique to discuss the latest developments in the fields of epidemiology, pathogenesis, structural virology, immunology, antiviral drug discovery and development, vaccine efficacy, and mosquito control programs. The meeting venue offered an opportunity to discuss current research on these flaviviruses in an idyllic setting, and also to develop first-hand appreciation of the issues in infectious diseases facing developing countries and of the research gaps in Africa. For readers, who should include basic and clinical researchers in the field and public health professionals, the chapters are organized to provide a comprehensive overview of the various topics in current dengue and Zika virus research. A unique feature of the proceedings of this meeting is the inclusion of the discussions that took place following presentations. These have been transcribed and appended to the end of the relevant chapters, and they form the “salt in the soup” of this book.
This third edition is a comprehensive and extended study about the best known approaches for preparing the main types of glycosides, covering the classic and more recent glycosylation reactions used for preparing simple and challenging glycosides currently used as potent antiviral and antineoplastic drugs, or fluorogenic substrates used for enzymatic detection in cell biology. Besides, this new edition provides more examples of the glycosidic methodologies followed for preparing complex glycoconjugates such as glycoproteins and glycosphingolipids and gangliosides used as adjuvants or as synthetic vaccines candidates. Also, additional mechanistic evidence is presented for better understanding of the glycosylation reaction, trying to identify the variables mainly depending on protecting and leaving groups, as well as catalyst and reaction condition which altogether directs the anomeric stereo control. A chapter on the glycoside hydrolysis is included in view of the increasing interest in the use of biomass as a natural and renewable source for obtaining important intermediates or products used in food or valuable materials. The author includes information in the characterization of glycosides section with the aim of giving additional tools for the structural assignment through NMR, X-Ray and mass spectra techniques.
Carbohydrate Chemistry demonstrates the interdisciplinary nature of modern carbohydrate research, and benefits any researcher who wishes to learn about the latest developments in the carbohydrate field.