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Imidazole-Based Drug Discovery covers all categories of imidazole and its derivatives, synthesis, pharmacological applications and drug-based studies. Imidazole scaffolds act as a channel between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. This book provides detailed coverage of several greener synthetic protocols and pharmacological applications of imidazole derivatives that are useful to researchers working on designing more promising clinical lead compounds with this scaffold. It also includes information on past decades of research on the synthesis and biological applications of imidazole derivatives. This is an ideal resource for researchers in organic chemistry both in academic and industrial settings, as well as postgraduates in chemistry and medicinal chemistry. Reviews the most current developments and future perspectives of imidazole on different disease therapies to achieve the ultimate goal of disease eradication Discusses the role of imidazole in contemporary science, technological innovation, drug development, critical challenges and future research directions Covers emerging trends on different eco-benign pathways to synthesize imidazole derivatives for the development of simpler synthetic protocols
Nature has inspired man in all aspects of life, chemistry included. The first antibiotic ever discovered came from nature, and since then, chemists have been probing nature for insights to guide drug discovery and development. Alkaloids are a class of naturally occurring molecules which contain nitrogen atoms and can be found in all forms of life. Imidazole is common structural unit found in many natural molecules, from the simple amino acid histamine to more complex structures like the marine sponge derived alkaloid palau'amine. Many imidazole-containing natural products are biologically active, such as inhibiting the growth of tumors, possessing antibacterial properties, and influencing signaling pathways of cells like an inflammatory response. Access to large quantities of these molecules would aid medical science in drug discovery and design, potentially impacting the overall quality of life for all. It is therefore essential for the chemical community to pursue the synthesis of natural products not only to gain more knowledge in the overall science, allowing for better isolation,characterization, and synthesis of molecules, but also to better the quality of life and health as a whole.Chapter 1 of this dissertation describes the isolation and characterization of spiroleucettadine and terrazoanthines A-C. It further describes, in detail, the unsuccessful attempts to synthesis spiroleucettadine, which prompted its structural revision, and the only reported synthesis of the revised structure.Chapter 2 focuses on our approach to the total synthesis of spiroleucettadine. Initially our strategy centered on employing a novel reaction discovered in our lab to help facilitate the construction of the spirocyclic center. However, we later found this route to not be viable,leading to a significant revision in our strategy.In chapter 3 describe our approach to total synthesis of terrazoanthines A-C. Besides its purification and structural assignment,there are no reports pertaining to this molecule in the literature. Of the 3 molecules, only one of them possesses multiple stereochemical centers. However, upon further examination of the core structure we proposed a concise synthetic route leading to not only all 3 molecule, all possible stereoisomers through the construction of a key symmetric intermediate.In chapter 4 we discuss the oxidative chemistry of tetrahydrobenzimidazole. The two oxidants used were dimethyldioxarine and oxaziridine. The results show the choice of oxidant, N-protecting group,and the functionalization at the C2-position can greatly affect the outcome of the reactions, leading to additions, cyclizations, and ring openings.
Reporting the rapidly growing field of rational drug design, this work is composed from a selected, topical range of chapters written by specialists in each field.
Macromolecular (specifically peptide-based) drugs could potentially be highly effective medicines. However they have a relatively short duration of action and variable therapeutic index. An example of such a peptide is Glucagon-like Peptide I which could potentially be used as a revolutionary drug for diabetes. This is because it stimulates insulin only when the blood glucose level is high thereby reducing the risk of hypoglycemia (a significant disadvantage of using insulin is that an insulin overdose is the single most potent cause of life-threatening hypoglycemia). However it’s short duration of action (half-life of 2 minutes in plasma) precludes its therapeutic use. In this volume, the use of novel therapeutics like GLP1 as an alternative to tradition insulin-based drugs in diabetes is described. Application of Peptide-Based Prodrug Chemistry in Drug Development elucidates the traditional concept of prodrugs as “specialized non-toxic protective groups used in a transient manner to alter or to eliminate certain limiting properties in the parent small molecule” (IUPAC definition). It goes on to provide insight into how prodrugs of peptides (with GLP1 as an example) could be appropriately used to extend the biological half life, broaden the therapeutic index of macromolecules and improve the pharmacodynamics of such drugs. Author explains the logic behind designing peptide prodrugs, synthetic procedures and bioassays to examine the conversion of the prodrug to the drug under therapeutic conditions. The prodrugs described slowly convert to the parent drug at physiological conditions of 37C and pH 7.2 driven by their inherent chemical instability without the need of any enzymatic cleavage. The diketopiperazine and diketomorpholine (DKP and DMP) strategies for prodrug conversion are demonstrated in detail with special emphasis on the chemical flexibility that it offers to develop prodrugs with variable time actions. This book will be of useful to chemists, biochemists, medicinal chemists, biologists and people in the medical profession (doctors). It may be used in undergraduate classes but will certainly help post-graduate students and advanced professionals. The author is grateful to Prof. Richard DiMarchi (Standiford H. Cox Professor of Chemistry and the Linda & Jack Gill Chair in Biomolecular Sciences at Indiana University) for valuable suggestions. The foreword for the book has been written by Prof. Jean Martinez, (Legion d'Honneur awarded by the French Republic; Professor of Chemistry and Medicinal Chemistry of the University of Montpellier, France; and Chairman of European Peptide Society, 2002-2010).
Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.
Privileged Scaffolds in Drug Discovery is the most complete and up-to-date work in the area. Covering a wide range of privileged structures, it is a perfect reference for scientists involved in targeted drug development. The editors recruited epserts from several prestigious Chinese institutions to cover the areas of antiviral drugs, chalcone, pyrimidine, (benz)imidazoles, natural product-derived privileged scaffolds, N-Sulfonyl carboxamides, kinase inhibitors, antitumor molecules, antineurodegenerative drugs, triazoles, oxazolidinone, indole and indoline scaffolds, tigliane diterpenoids, peptide and peptide-based drugs, quassinoids, and others including pseudonatural products, macrocycles, stable peptides and peptidomimetics. The book also explores scaffolds in drug molecules approved in recent years. Privileged Scaffolds in Drug Discovery is a complete reference for researchers in drug discovery and organic synthesis, in academic and corporate settings, who are investigating privileged structures upon which to base new drugs. Researchers in medicinal chemistry and chemical biology will also find the contents of this book valuable. - Provides wide coverage of privileged scaffolds in new drug discovery - Includes complex and diverse natural product scaffolds - Covers applications to peptides and peptide-based drugs
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Imidazole and Benzimidazole Synthesis is a comprehensive survey of the known methods of syntheses and ring modification. It brings together the multitude of synthesis of the imidazole ring in a systemic way interms of specific bond formation, and recommends the most attractive synthetic approaches. It also collects non-ring-synthetic approaches to classes of compounds such as nitro-, halogeno-, and amino-imidazoles, and covers the synthesis of N-substituted compounds and preparations of specific isomers. The only book in print dealing specifically with this topic Comprehensive survey of the known methods of synthesis and ring modification Recommends the most attractive synthetic approaches
This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.