Download or read book Heteroaromatic Lipoxin A4 Analogues written by Colm Duffy and published by Springer Science & Business Media. This book was released on 2012-01-10 with total page 143 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this thesis Colm Duffy reviews the chemistry and biology of stable lipoxin analogues. Colm has prepared for the first time ever a pyridine-containing LXA4 analogue in enantiomerically pure form. Biological evaluation determined that both epimers at the benzylic position suppress key cytokines known to be involved in inflammatory disease, with the (R)-epimer proving most efficacious. Moreover the author developed an excellent route to a related thiophene-containing analogue that also showed interesting biological activity. Both routes have inspired further work in the synthesis of further heteroaromatic analogues for biological evaluation.
Download or read book Synthesis of Heteroaromatic Lipoxin A4 Analogues for Biological Evaluation written by Eibhlín Butler and published by . This book was released on 2013 with total page 196 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis and Biological Evaluation of Stable Heteroaromatic Lipoxin A4 Analogues written by Catherine Tighe and published by . This book was released on 2016 with total page 304 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis and Biological Evaluation of Heteroaromatic Lipoxin A4 Analogues written by Colm Duffy and published by . This book was released on 2010 with total page 170 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis and Biological Evaluation of Heteroaromatic Lipoxin A4 Analogues written by Claire Margaret Wilson and published by . This book was released on 2014 with total page 151 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Lipoxin A4 Analogues written by Andrea Zanetti and published by . This book was released on 2018 with total page 210 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Synthesis of Stable Lipoxin A4 Analogues for Biological Evaluation written by Denise Moran and published by . This book was released on 2017 with total page 178 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book The logic of chemical synthesis written by E.J. Corey and published by Рипол Классик. This book was released on 1991 with total page 447 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Bioisosteres in Medicinal Chemistry written by Nathan Brown and published by John Wiley & Sons. This book was released on 2012-06-18 with total page 249 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.
Download or read book Resolution Pharmacology Innovative Therapeutic Approaches Based on the Biology of Resolution to Control Chronic Diseases of Western Societies written by Mauro Perretti and published by Frontiers Media SA. This book was released on 2019-11-04 with total page 205 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this eBook, we have grouped together 16 original contributions which have addressed the translational potential for therapeutics developed on the conceptual framework of the resolution of inflammation. The take home message of our effort, and the efforts of our colleagues who wrote these pieces, is that completely different drugs can be designed and modelled on the mediators and targets of resolution. By implementing this 180° shift in the way we plan the drug development programme (that is by focusing on agonists and/or promoting the actions of pro-resolution agonists) we can offer a fresh approach to the clinical management of chronic diseases that affect the modern society. With this series of articles we foresee the birth of Resolution Pharmacology. The 16 contributions presented herein confirm the broad relevance of pro-resolving physio-pharmacology with the description of pro-resolving mechanisms in distinct diseases, from atherosclerosis and heart infarct, to cystic fibrosis and diabetes. This testifies on one hand the fundamental role that inflammatory mechanisms play in virtually all pathological settings and, on the other hand, the great potential that a novel approach to anti-inflammatory therapy by exploiting resolution mediators and targets may have. Thus, while there is broad recognition that evidence-based interventions have transformed cardiovascular, inflammation and endocrine care, new therapies are still needed for growing numbers of patients with unmet needs. As an example, an estimated 17 million people world-wide die annually of cardiovascular diseases, particularly heart attacks and strokes. Cardiovascular diseases occur almost equally in men and women and are the leading cause of death and morbidity worldwide. It is estimated that only 1/1,000 compounds entering preclinical testing are then trialled in man and the actual cost of developing a new therapeutic into clinical practice has grown exponentially over the past two decades (estimated $1.2B). Over the last 20 years or more, scientists have appreciated the biology of the resolution of inflammation, which provides a new paradigm in our understanding of the inflammatory process with the appreciation of genetic, molecular and cellular mechanisms that are engaged to actively resolve inflammation. The ‘resolution of acute inflammation’ is enabled by counter-regulatory checkpoints to terminate the host reaction while at the same time promoting healing and repair. The potential of lipid mediators to enact pro-resolving effects in the context of cystic fibrosis is presented by Recchiuti et al., while Fredman reasons on the potential for these molecules in atherosclerosis. This resonates well with the contributions from Bäck and colleagues who have focused on pro-resolving receptors to offer vasculo-protection in intimal hyperplasia and more generally in cardiovascular disease. On the same vein is the scholar contribution of Leoni and Soehnlein who focus on heart disease, with Qin et al. presenting the latest findings on the effect of an Annexin A1-derived peptide in myocardial infarction. Hansen et al. and de Gaetano et al. bring in the complexity of diabetes and associated morbidity with a focus on specialised pro-resolving lipid mediators but also introducing the potential of dietary approaches. As the western diet favours disease, an omega-3 rich diet can lead to higher availability of lipid mediators to afford tissue protection if not reverting its pathological status. Docosahexaenoic acid and its bioactive derivatives are endowed with potent anti-nociceptive properties following bone fracture, as shown by Zhang et al. The broad relevance of the pharmacological approach reaches the skin with Resolvin D1 protecting against UV irradiation (Saito et al.). Reduced skin inflammation is also achieved with an Annexin A1 peptide that impacts on the outcome of heterologous transplantation (Lacerda et al.). Indeed, modulating the phenotype of immune cells can provide long lasting beneficial outcomes, as attained with CDK inhibitors (Cartwright et al.) and PI3K inhibitors in experimental gout (Galvao et al.). Such an effect is also achieved with a third group of pro-resolving therapeutics, the melanocortin receptor agonists, with important modulation of macrophage reactivity (Patruno et al.) with Spana et al., providing new pharmacology following selective activation of the MC1 receptor. Finally, Hopkin et al. discuss the potential for targeting immune cell trafficking as a way to control immune mediated diseases, bringing in not only pro-resolving mediator agonists, but also approaches to reduce chemo/cytokine gradients or modulating S1P and 11-beta hydroxysteroid dehydrogenase. Finally, we wish to highlight that this wealth of science has also bought to the forefront specific pro-resolving receptors (including FPR2/ALX, GPR32, ChemR23 and MC1), all G protein coupled receptors that are therefore amenable to pharmacological exploitation for drug discovery programmes. We see that not only agonists to the receptors can be developed, some of them modelled on the natural ligands (e.g. resolvins, lipoxins, Annexin A1-derived peptides or melanocortin peptides), but also that the creativity of this pharmacology can be attained through biased ligands and positive allosteric modulators. Deep knowledge of pro-resolving receptor biology and their cell-specific signalling can accelerate the generation of novel anti-inflammatory depicted on the resolution of inflammation. In conclusion, with this eBook, we propose time is ready to exploit the concepts of resolution and use its targets and mediators for the identification of better drugs to establish ‘Resolution Pharmacology’. We predict Resolution Pharmacology will represent an important innovation in the way common diseases will be treated in the next decades of this millennium.
Download or read book Immunopharmacology and Inflammation written by Carlo Riccardi and published by Springer. This book was released on 2018-06-09 with total page 330 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive overview of the current research on inflammation and immunopharmacology, with particular attention to the use of anti-inflammatory drugs, this book discusses future trends in this area of pharmacological research. It addresses an audience with basic knowledge in the inflammatory process, immune system and pharmacology. The book meets the needs of graduate students, junior and senior researchers and is useful as a source of the most current information for those already working in these fields.
Download or read book Heterocyclic N Oxides written by Oleg V. Larionov and published by Springer. This book was released on 2017-07-12 with total page 163 pages. Available in PDF, EPUB and Kindle. Book excerpt: The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.
Download or read book Encyclopedia of Signaling Molecules written by Sangdun Choi and published by Springer. This book was released on 2017-12-15 with total page 6330 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of this encyclopedia presents over 400 biologically important signaling molecules and the content is built on the core concepts of their functions along with early findings written by some of the world’s foremost experts. The molecules are described by recognized leaders in each molecule. The interactions of these single molecules in signal transduction networks will also be explored. This encyclopedia marks a new era in overview of current cellular signaling molecules for the specialist and the interested non-specialist alike. Currently, there are more than 30,000 genes in human genome. However, not all the proteins encoded by these genes work equally in order to maintain homeostasis. Understanding the important signaling molecules as completely as possible will significantly improve our research-based teaching and scientific capabilities.
Download or read book Indoles written by Richard J. Sundberg and published by Elsevier. This book was released on 1996-05-28 with total page 193 pages. Available in PDF, EPUB and Kindle. Book excerpt: Indoles continue to be of great interest to the pharmaceutical industry and at the current time several thousand specific new derivatives are reported annually. Research has been driven by the wide range of indole derivatives which occur in nature and through the biological activity of many indole derivatives, of both natural and synthetic origin.This book provides a systematic guide to the most useful and important reactions in the field for both synthesis and synthetic modification of the indole ring. While including the most recently developed and promising methods, it also updates informationavailable on classical methods to give the reader an up-to-date and comprehensive view of the subject. The methods are illustrated by procedures drawn from the literature and by tables including examples chosen to indicate both the scope of applicabilityand variations in methodology. The organization of the book is based on the retrosynthetic concept of identifying the bond(s) formed in the reaction, which in turn identifies potential starting materials. Includes systematic summaries of the most important methods for the construction of indoles from aromatic precursors Discusses methods for preparing indoles by annelation of pyrroles Covers methods for adding or modifying substituent groups, including methods for introducing the tryptamine and tryptophan side-chainsExamines reduction/oxidation reactions that are specific for indoles Considers use of cycloaddition reactions for synthetic elaboration of indoles
Download or read book Boronic Acids written by Dennis G. Hall and published by John Wiley & Sons. This book was released on 2006-05-12 with total page 571 pages. Available in PDF, EPUB and Kindle. Book excerpt: For the first time, the whole field of organoboronic acids is presented in one comprehensive handbook. Professor Dennis Hall, a rising star within the community, covers all aspects of this important substance class, including applications in chemistry, biology and medicine. Starting with an introduction to the structure, properties, and preparation of boronic acid derivatives, together with an overview of their reactions and applications, the book goes on to look at metal-catalyzed borylation of alkanes and arenas, coupling reactions and rhodium-catalyzed additions of boronic acids to alkenes and carbonyl compounds. There follows chapters on copper-promoted C-O and C-N cross-coupling of boronic acids, recent applications in organic synthesis, as well as alpha-haloalkylboronic esters in asymmetric synthesis. Later sections deal with cycloadditions, organoboronic acids, oxazaborolidines as asymmetric inducers, and boronic acid based receptors and sensors. The whole is rounded off with experimental procedures, making this invaluable reading for organic, catalytic and medicinal chemists, as well as those working in organometallics.
Download or read book Oral Wound Healing written by Hannu Larjava and published by John Wiley & Sons. This book was released on 2012-05-15 with total page 433 pages. Available in PDF, EPUB and Kindle. Book excerpt: Oral Wound Healing: Cell Biology and Clinical Management brings experts from around the world together to provide an authoritative reference on the processes, principles and clinical management of wound healing in the oral mucosa. Promoting a thorough understanding of current research on the topic, this new resource draws together thinking on the basic biological processes of wound healing in the oral environment, as well as providing more detailed information and discussion on processes such as inflammation, reepithelialization and angiogenesis. Beyond this, the book goes on to examine topics pertinent to the effective clinical management of oral wound healing, bringing together chapters on large dento-facial defects, dental implants, periodontal regeneration, and pulp healing.An essential synthesis of current research and clinical applications, Oral Wound Healing will be an indispensable resource for dental specialists, oral and maxillofacial surgeons as well as researchers in oral medicine and biology.
Download or read book Visible Light Photocatalysis in Organic Chemistry written by Corey R.J. Stephenson and published by John Wiley & Sons. This book was released on 2018-05-29 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: Filling the need for a ready reference that reflects the vast developments in this field, this book presents everything from fundamentals, applications, various reaction types, and technical applications. Edited by rising stars in the scientific community, the text focuses solely on visible light photocatalysis in the context of organic chemistry. This primarily entails photoinduced electron transfer and energy transfer chemistry sensitized by polypyridyl complexes, yet also includes the use of organic dyes and heterogeneous catalysts. A valuable resource to the synthetic organic community, polymer and medicinal chemists, as well as industry professionals.
