Stefan Bräse - Böcker

Most current state-of-the-art overview of this important class of compounds, encompassing many new and emerging applicationsThe number of articles on organic azides continues to increase tremendously; on average, there are more than 1000 new publications a yearCovers basic chemistry as well as state-of-the-art applications in life science and materials scienceWorld-ranked authors describe their own research in the wider context of azide chemistryIncludes a chapter on safe synthesis and handling (azides can decompose explosively)

One strategy to expedite the discovery of new drugs, a process that is somewhat slow and serendipitous, is the identification and use of privileged scaffolds. This book covers the history of the discovery and use of privileged scaffolds and addresses the various classes of these important molecular fragments. The first of the benzodiazepines, a class of drugs that is powerful for treating anxiety, may not have been discovered had it not been for a chance experiment on the contents of a discarded flask found during a lab clean-up. Some years later, scientists discovered that benzodiazepine derivatives were also effective in treating other diseases. This class of molecules was the first to be described as privileged in the sense that it is especially effective at altering the course of disease. Other privileged molecular structures have since been discovered, and since these compounds are so effective at interacting with numerous classes of proteins, they may be an effective starting point to look for new drugs against the supposedly “undruggable” proteins. Following introductory chapters presenting an overview, a historical perspective and the theoretical background and findings, main chapters describe the structure of privileged structures in turn and discuss major drug classes associated with them and their syntheses. This book provides comprehensive coverage of the subject through chapters contributed by expert authors from both academia and industry and will be an excellent reference source for medicinal chemists of a range of disciplines and experiences.

Themodernbillion-dollardrug-discoveryprocessstronglyreliesonbothhi- throughput synthesis and screening methods. Whereas the latter is based on molecular biological methods, the ef?cient and reliable generation of c- pound collections often makes use of combinatorial chemistry. Discovered in the 1980s, this methodology was explored extensively in the 1990s by groups in academia and in industry. Without any doubt, combinatorial chemistry changed the whole drug-discovery process and found many applications in cropscience and the material sciences. However, since its implementation, solution- and solid-phase techniques have been competing with each other, and although many companies started theircombinatorialchemistryprogramwithsolid-phasetechniques,soluti- phase combinatorial methods have taken over and now account for appro- mately 25% of all combinatorial efforts. The syntheses of complex, non-polymeric structures, discovered in the 1960s by the late Bruce Merri?eld, was largely ignored in the context of solid supports, mainly due to the fact that appropriate synthesis techniques were not available.Since solid-phase chemical methodology strongly differs from traditional solution-phase chemistry, two chapters deal with this topic. The Brase group (Jung, Wiehn, Brase) gives an overview of multifunctional linkers, which can beusedforthegenerationofdiversity-orientedcollections,simplybycleavage fromresins. Still in its infancy, solid-phase reactions employ "simple" amide chemistry in most cases due to their high-yielding, reliable protocols. Ljungdahl, Br- ?eld, and Kann address solid-phase organometallic chemistry, which is now one ofthe great challenges in reliable solid-phase organicsynthesis.

Themodernbillion-dollardrug-discoveryprocessstronglyreliesonbothhi- throughput synthesis and screening methods. Whereas the latter is based on molecular biological methods, the ef?cient and reliable generation of c- pound collections often makes use of combinatorial chemistry. Discovered in the 1980s, this methodology was explored extensively in the 1990s by groups in academia and in industry. Without any doubt, combinatorial chemistry changed the whole drug-discovery process and found many applications in cropscience and the material sciences. However, since its implementation, solution- and solid-phase techniques have been competing with each other, and although many companies started theircombinatorialchemistryprogramwithsolid-phasetechniques,soluti- phase combinatorial methods have taken over and now account for appro- mately 25% of all combinatorial efforts. The syntheses of complex, non-polymeric structures, discovered in the 1960s by the late Bruce Merri?eld, was largely ignored in the context of solid supports, mainly due to the fact that appropriate synthesis techniques were not available.Since solid-phase chemical methodology strongly differs from traditional solution-phase chemistry, two chapters deal with this topic. The Brase group (Jung, Wiehn, Brase) gives an overview of multifunctional linkers, which can beusedforthegenerationofdiversity-orientedcollections,simplybycleavage fromresins. Still in its infancy, solid-phase reactions employ "simple" amide chemistry in most cases due to their high-yielding, reliable protocols. Ljungdahl, Br- ?eld, and Kann address solid-phase organometallic chemistry, which is now one ofthe great challenges in reliable solid-phase organicsynthesis.

The biological activity of mycotoxins ranges from weak and/or sometimes positive effects, such as antibacterial activity (see penicillin derivatives derived from Penicillium strains) to strong mutagenic (e. g. aflatoxins, patulin), carcinogenic (e. g. aflatoxins), teratogenic, neurotoxic (e. g. ochratoxins), nephrotoxic (e. g. fumonisins, citrinin), hepatotoxic, and immunotoxic (e. g. ochratoxins, diketopiperazines) activity. Nowadays, many laboratories around the world are specialized in the detection of mycotoxins in food products and contaminated material found in housing. In this volume, a focus on the most important classes of mycotoxins is provided and their chemistry of the last ten years is discussed. In each Section, the individual biological impact is outlined. Sections are arranged according to mycotoxin classes (e. g. aflatoxins) and/or structural classes (e. g. resorcinyl lactones, diketopiperazines). The biology of mycotoxins is also described.