Domino Reactions In Drug Discovery

Domino Reactions in Drug Discovery presents a concise selection of domino reactions employed in routes for the synthesis of pharmaceuticals, agrochemicals and the design of new drug candidates. These versatile reactions play an important and integral part in both the aesthetic appeal and functional aspects of strategic drug discovery, lending enhanced efficiency and synthetic versatility to pharmaceutical drug design. Due to their atom economy, these reactions are increasingly popular in the development of complex scaffolds and multifunctional derivatives aimed at the synthesis of new chemical entities and approved APIs across diverse therapeutic classes, including antidiabetics [DPP4 inhibitors], anticancer therapies and HIV integrase inhibitors. Features illustrated schemes with mechanisms, procedures and results Includes a compendium of Domino Name Reactions for drugs Provides a concise, comprehensive coverage of domino reactions in drug discovery, with a focus on sustainable practices

The follow-up to the successful "Domino Reaction in Organic Synthesis", this ready reference brings up to date on the original concept. The chapters have been arranged according to the name of well-known transformations of the first step and in combination with the formed products. Each chapter is written by an internationally renowned expert, and the book is edited by L. F. Tietze, who established the concept of domino reactions. The one-stop source for all synthetic chemists to improve the synthetic efficiency and allow an ecologically and economically beneficial preparation of every chemical compound.

Domino reactions enable you to build complex structures in one-pot reactions without the need to isolate intermediates- a dream comes true. In this book, the well-respected expert, Professor Lutz Tietze, summarizes the possibilities of this reaction type - an approach for an efficiant, economically benificial and ecological benign synthesis. A definite must for every organic chemist.

In the very first book on this hot topic, the expert editors andauthors present a comprehensive overview of these elegantreactions. From the contents: Organoboron compounds Free-radical mediated multicomponent coupling reactions Applications in drug discovery Metal catalyzed reactions Total synthesis of natural products Asymmetric isocyanide-based reactions The Biginelli reaction Asymmetric isocyanide-based reactions The Domino-Knoevenagel-Hetero-Diels-Alder Reaction and relatedtransformations Catalytic asymmetric reactions Algorithm based methods for discovering novel reactions Post-condensation modifications of the Passerini and Ugireactions An essential reference for organic and catalytic chemists, andthose working in organometallics both in academia and industry.

Chromene is a naturally abundant heterocyclic compound found in alkaloids, tocopherols, terpenes and other compounds. Its derivatives can be used as a scaffold that exhibits pharmacological activity in the human body. Chromene drugs and related bioactive molecules are the prime focus of this reference. It presents 13 thoroughly researched chapters that comprehensively cover all aspects about the molecule. Starting with a detailed introduction to its role and importance in drug discovery, the book goes into the details of chromene structure, synthesis and pharmacology. Readers can gain knowledge of different commercial medicines based on chromene and its pharmacological activity against different diseases. The elaborate topics in the book will help researchers working on chromene based drugs. Key highlights of the book include: - Complete coverage of chromene’s role in nature and drug development with references to historical background and current developments - References to commercial and preclinical drugs and patents of interest - Explanation of chromene bioacivity in different diseases (antioxidant, antidiabetic, antinflammatory, antibacterial and antifungal activities, antitumour, immunomodulatory activity) - Explanation of chromene activity against SARS-Cov2

This book covers the latest developments in asymmetric domino reactions, focussing on those published in the last 6 years. These fascinating reactions have rapidly become one of the most current fields in organic chemistry, since they allow reaching easily high molecular complexity in an economically favourable way with advantages of savings in solvent, time, energy, and costs. Unsurprisingly, the high levels of efficiency and enantioselectivity generally reached in these reactions have been exploited for the production of a wide number of complex chiral molecules with dense stereochemistry and functionality, which are motifs present in biologically active compounds and natural products. The book is divided into three principal sections, dealing successively with asymmetric domino reactions based on the use of chiral auxiliaries, asymmetric domino reactions based on the use of chiral metal catalysts, and asymmetric domino reactions based on the use of chiral organocatalysts, covering the literature since the beginning of 2006.

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

Discover an enhanced synthetic approach to developing andscreening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developinglarge collections of structurally diverse small molecules as probesto investigate biological pathways. This book presents the mosteffective methods in diversity-oriented synthesis for creatingsmall molecule collections. It offers tested and proven strategiesfor developing diversity-oriented synthetic libraries and screeningmethods for identifying ligands. Lastly, it explores some promisingnew applications based on diversity-oriented synthesis that havethe potential to dramatically advance studies in drug discovery andchemical biology. Diversity-Oriented Synthesis begins with an introductorychapter that explores the basics, including a discussion of therelationship between diversity-oriented synthesis and classiccombinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of smallmolecules using diversity-oriented principles, includingpeptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis bydescribing chemical libraries Provides modern approaches to screening diversity-orientedsynthetic libraries, including high-throughput and high-contentscreening, small molecule microarrays, and smart screeningassays Presents the applications of diversity-oriented syntheticlibraries and small molecules in drug discovery and chemicalbiology, reporting the results of key studies and forecasting therole of diversity-oriented synthesis in future biomedicalresearch This book has been written and edited by leading internationalexperts in organic synthesis and its applications. Theircontributions are based on a thorough review of the currentliterature as well as their own firsthand experience developingsynthetic methods and applications. Clearly written and extensively referenced,Diversity-Oriented Synthesis introduces novices to thishighly promising field of research and serves as a springboard forexperts to advance their own research studies and develop newapplications.