Heterocyclic Chemistry in Drug Discovery


Book Description

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.




Piperidine-Based Drug Discovery


Book Description

Piperidine-Based Drug Discovery outlines the complexities of Piperidine scaffold use in drug discovery, including derivative chemistry, structural properties, methods of synthesis and practical implementations. Piperidine scaffolds are the cornerstones of over 70 commercialized drugs (including multiple blockbusters). Designed as a guide for both experts and students working in this and related areas, it is hoped that this volume will encourage and inspire the continued design and development of novel pharmaceuticals based on Piperidine and its derivatives. Heterocyclic compounds are of central importance to medicinal chemistry, as demonstrated by the high percentage of marketable drugs that feature heterocyclic fragments in their structures. As starting points for drug discovery they offer a broad range of attractive properties, and a detailed understanding of the particular characteristics of each is of great benefit to researchers. The most commonly used heterocycle among US FDA approved pharmaceuticals, Piperidine is an extremely important building block in the synthesis of medicinal agents. This heterocycle and its derivatives exhibit a number of important functionalities and have been employed variously as CNS modulators, antiaggregants, anticoagulants, antihistamines, anti-cancer drugs and analgesics. - Explores this extremely important heterocycle to a high level of detail - Describes synthesis methods for 70 current drugs based on Piperidine scaffolds - Gives drug designers all the key knowledge required to develop new drugs utilizing Piperidine - Provides pharmacologists a solid overview of the chemical background of existing Piperidine-based drugs




Key Heterocycle Cores for Designing Multitargeting Molecules


Book Description

Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. - Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules - Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents - Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases




Handbook of Heterocyclic Chemistry


Book Description

Provides a one-volume overall picture of the largest of the classical divisions of organic chemistry, suitable for the graduate or advanced undergraduate student, as well as for research workers, both specialists in the field and those engaged in another discipline and requiring knowledge of heterocyclic chemistry. It represents Volume 9 of Comprehensive Heterocyclic Chemistry and utilizes the general chapters which appear in the 8-volume work. The highly systematic coverage given to the subject makes this the most authoritative one-volume account of modern heterocyclic chemistry available.




Advances in Heterocyclic Chemistry


Book Description

Established in 1960, Advances in Heterocyclic Chemistry is the definitive serial in the area-one of great importance to organic chemists, polymer chemists, and many biological scientists. Written by established authorities in the field, the comprehensive reviews combine descriptive chemistry and mechanistic insight and yield an understanding of how the chemistry drives the properties. - Up-to-date results in the subject which continues to gain importance and expand - Makes available to graduate students and research workers in academic and industrial laboratories the latest reviews on wide variety of heterocyclic topics - The series forms a very substantial database covering wide areas of heterocyclic chemistry




Fluorine in Heterocyclic Chemistry Volume 2


Book Description

This two-volume work combines comprehensive information on the chemistry of the fluorinated heterocycles. The material has been divided such that the first volume is dedicated to 5-membered fluorinated heterocycles and macrocycles, while the second volume combines data connected with the chemistry of fluorine containing 6-membered heterocycles. Both volumes will be of interest to synthetic organic chemists in general, and particularly for those colleagues working in the fields of heterocyclic-compound chemistry, materials chemistry, medicinal chemistry, and fluorine chemistry. All information is presented and classified clearly to be effective source for broad auditory of chemists. It will be interesting for scientists working in the field of inorganic and coordination chemistry. Fluorinated heterocycles are becoming increasingly important in many areas including the pharmaceutical industry, materials science and agriculture. The presence of fluorine can result in substantial functional changes in the biological as well as physicochemical properties of organic compounds. Incorporation of fluorine into drug molecules can greatly affect their physicochemical properties, such as bond strength, lipophilicity, bioavailability, conformation, electrostatic potential, dipole moment, pKa etc. as well as pharmacokinetic properties, such as tissue distribution, rate of metabolism and pharmacological properties, such as pharmacodynamics and toxicology.




Modern Green Chemistry and Heterocyclic Compounds


Book Description

This book covers the general properties of heterocyclic compounds and methods for their preparation to use in applications of green chemistry. Heterocyclic compounds are an important class of molecules in organic chemistry due to their presence in natural products and their use in pharmaceuticals and new materials. They also play a vital role in the metabolism of living cells. Heterocyclic compounds have a wide range of applications in agrochemicals, pharmaceuticals, veterinary products, etc. This research-oriented volume is ideal for readers who want to fully realize the almost limitless potential of heterocyclic compounds and to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features several case studies and step-by-step descriptions of synthetic methods and practical techniques. It also serves as a guide for chemists, offering them new insights and new paths to explore for effective drug discovery.




Name Reactions in Heterocyclic Chemistry


Book Description

Covers important name reactions relevant to heterocyclic chemistry The field of heterocyclic chemistry has long presented a special challenge for chemists. Because of the enormous amount and variety of information, it is often a difficult topic to cover for undergraduate and graduate chemistry students, even in simplified form. Yet the chemistry of heterocyclic compounds and methods for their synthesis form the bedrock of modern medicinal chemical and pharmaceutical research. Thus there is a great need for high quality, up-to-date, and authoritative books on heterocyclic synthesis helpful to both the professional research chemist as well as the advanced student. Name Reactions in Heterocyclic Chemistry provides a one-stop repository for this important field of organic chemistry. The primary topics include three- and four-membered heterocycles, five-membered heterocycles including indoles, furans, thiophenes, and oxazoles, six-membered heterocycles including quinolines, isoquinolines, and pyrimidines, and other heterocycles. Each name reaction is summarized in seven sections: Description Historical perspective Mechanism Variations and improvements Synthetic utility Experimental References Authored by a team of world-renowned contributors - some of whom have discovered the very reactions they describe - Name Reactions in Heterocyclic Chemistry represents a state-of-the-art resource for students and researchers alike.




Green Synthetic Approaches for Biologically Relevant Heterocycles


Book Description

Green Synthetic Approaches for Biologically Relevant Heterocycles, Second Edition, Volume One: Advanced Synthetic Techniques reviews this significant group of organic compounds within the context of sustainable methods and processes, expanding on the first edition with fully updated coverage and a whole range of new chapters. Volume One explores advanced synthetic techniques, with each chapter presenting in-depth coverage of various green protocols for the synthesis of a wide variety of bioactive heterocycles that are classified on the basis of ring-size and/or the presence of heteroatoms. Techniques covered range from high pressure cycloaddition reactions and microwave irradiation to sustainable one-pot domino reactions. This updated edition is an essential resource on sustainable approaches for academic researchers, R&D professionals, and students working across medicinal, organic, natural product and green chemistry. Provides fully updated coverage of the field of greener heterocycle synthesis Includes new chapters on varied multicomponent reactions, alongside both traditional and novel approaches Presents information in an accessible style with an emphasis on sustainability




Vicinal Diaryl Substituted Heterocycles


Book Description

Vicinal Diaryl-Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic Agents draws together all of the key information about these compounds in one place for the first time. Following an informative overview of the importance of these structures to the discovery of potential therapeutic agents, the text goes on to outline the main compound types, with each chapter focusing on the activities of a different structure. Designed to support researchers by consolidating this important information in a single, practical guide, the authors hope to encourage further advancement and development in the discovery of novel therapeutic agents. As flexible building blocks for the production of novel compounds, vicinal diaryl-substituted heterocycles are a rich source of leads for the development of new drugs. Their adaptability means that they can be used to produce structures with a broad range of attractive characteristics, and a large number of vicinal diaryl-substituted heterocyclic compounds have already been synthesized and investigated by medicinal chemists as promising lead molecules. - Collects together details of the key vicinal diaryl-substituted heterocyclic compounds in one place for the first time - Highlights biological activities and SAR of derivatives - Structured practically for ease of navigation between different derivatives