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.

This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

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.

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

Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain applications. Chapters cover such topics as therapeutic use of benzimidazole in conditions like diabetes, viruses, and parasitic diseases; X-ray crystal structure of selected benzimidazole derivatives; benzimidazole compounds for cancer therapy; and others.

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint