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Recent Advancement in Prodrugs Drugs used as medicines have many limitations like low chemical stability, aqueous solubility, or oral absorption/bioavailability, rapid presystemic metabolism, toxicity, inadequate site specificity, or poor patient acceptance/compliance (unwanted adverse effects, unacceptable taste or odor, irritation or pain). Prodrugs design is an approach to overcome these limitations. Key features Covers recent advancements in development of prodrugs Presents balanced synthesis and applications of prodrug chemistry Discusses broad spectrum of prodrug categories and outlines industrial applications Reviews prodrugs in cancer nanomedicine, its therapy and treatment Elucidates mathematical models to study the kinetics of prodrugs This book covers recent advances in the design of prodrugs. It contains all the significant recent examples of prodrug chemistry developments and will aid academics and researchers seeking to generate new projects in the field.
Recent Advancement in Prodrugs Drugs used as medicines have many limitations like low chemical stability, aqueous solubility, or oral absorption/bioavailability, rapid presystemic metabolism, toxicity, inadequate site specificity, or poor patient acceptance/compliance (unwanted adverse effects, unacceptable taste or odor, irritation or pain). Prodrugs design is an approach to overcome these limitations. Key features Covers recent advancements in development of prodrugs Presents balanced synthesis and applications of prodrug chemistry Discusses broad spectrum of prodrug categories and outlines industrial applications Reviews prodrugs in cancer nanomedicine, its therapy and treatment Elucidates mathematical models to study the kinetics of prodrugs This book covers recent advances in the design of prodrugs. It contains all the significant recent examples of prodrug chemistry developments and will aid academics and researchers seeking to generate new projects in the field.
These volumes represent a comprehensive guide to prodrugs. They guide the reader through the current status of the prodrug concept and its many applications and highlight its many successes in overcoming formulation and delivery of problematic drugs. Replete with examples of approved and marketed prodrugs, these volumes introduce the topic to the novice as well as professional in the design of prodrugs.
The book covers up-to-date information on nucleosides and antiviral chemotherapy contributed by the world experts in the field of nucleoside. This book is the result of a meeting honoring Dr. Jack J. Fox, who was one of the pioneers in nucleoside chemistry and chemotherapy. This book consists of 15 excellent chapters in the area, which include topics from recent synthetic methodologies, nucleoside kinase implicated in chemotherapy and drug design, excellent reviews on antiviral agents, nucleoside metabolism/mode of action in parasites, new compounds under clinical and pre-clinical trials, IMPDH inhibitors to review on nucleoside prodrugs.
The prodrug approach is a promising and well established strategy for the development of new entities that possess superior efficacy, selectivity and reduced toxicity. Hence an optimised therapeutic outcome can be accomplished using this approach. Prodrug design is becoming more elaborate in the development of efficient and selective drug delivery systems. The targeted prodrug approach, in combination with gene delivery and controlled expression of enzymes and carrier proteins, is a promising strategy for precise and efficient drug delivery and enhancement of the therapeutic effect. This book describes in details all prodrug approaches and examples of prodrugs that succeeded to enter the market. There are two major prodrug design approaches that are considered as widely used among all other approaches: the targeted drug design approach by which prodrugs can be designed to target specific enzymes or carriers by considering enzyme-substrate specificity or carrier-substrate specificity in order to overcome various undesirable drug properties. Examples for such approach is the antibody-directed enzyme prodrug therapy (ADEPT), gene-directed enzyme prodrug therapy (GDEPT), virus-directed enzyme prodrug therapy (VDEPT) and GDEPT. In addition, this book describes in details a novel prodrug chemical approach which is based on intramolecular reactions that were utilised to understand how enzymes exert their high catalysis. The information gained from the experimental and theoretical calculations on these enzyme models was used to design efficient chemical moieties to be utilised as prodrug linkers with the potential to release the corresponding parent drugs in a slow or fast release manner. Several prodrugs for commonly used drugs suffer from low bioavailability or/and bitter sensation were designed using quantum mechanics methods (DFT and ab initio) and recently a large number among these prodrugs were synthesised. Examples of such prodrugs are presented in the different chapters of the book.
Learn why some drug discovery and development efforts succeed . . . and others fail Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies. Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining: All phases of drug discovery and development from initial idea to commercialization Some of today's most important and life-saving medications Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies Examples of prodrugs and inhaled drugs Reasons why certain drugs failed to advance to market despite major research investments Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies. Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.
Advances in Prodrugs: Design and Therapeutic Applications provides a versatile tool in prodrug design and development as well as a concrete perspective on clinical and preclinical studies currently available on prodrugs. The first part of this book discusses different chemical classes of prodrugs, with particular emphasis on metabolic pathways and mechanisms involved in the activation of their functional groups. The second part of the book covers therapeutic applications of prodrugs against the most discussed diseases, providing detailed discussion on recent achievements in the field. This book offers researchers involved in drug discovery key criteria for the successful development of prodrug-based therapeutic tools.Prodrugs are inactive drug precursors which undergo different chemical transformation by metabolic processes to provide pharmacologically active compounds. Prodrugs include a broad range of structurally diverse molecules employed for the treatment of several diseases. - Highlights chemistry and pharmacology-related aspects, offering a versatile tool for readers involved in prodrug development and study - Discusses in-depth treatment of several activation mechanisms and applications for disease treatments - Covers a range of topics from basic contents, design, and mechanisms of actions to current applications in drugs
Prodrug Design: Perspectives, Approaches and Applications in Medicinal Chemistry provides a focused overview of this critical area of drug discovery, as that continuous process strives not only to discover new drug compounds but also to modify the existing ones. This valuable primer supports this mission of drug development and its goal of reducing undesired effects and improving therapeutic effectiveness of drug compounds. Providing a unique compilation of data, insightful case studies, and review of existing literature in the area, the book will promote innovation in medicinal and pharmaceutical chemistry research, exploring the limitations of existing drugs and their improvement. Prodrug Design reviews marketed compounds, the safety of promoieties, and a detailed classification of prodrugs organized by therapeutic area for easy reference. - Offers unique, detailed overview of Prodrug research and literature - Provides detailed chemical structures - Includes Prodrug listing by therapeutic area
This authoritative volume explores the fundamental concepts and numerous applications of targeted delivery of drugs to the body. This compilation has been divided into eight sections comprised of the basic principles of drug targeting, disease and organ/organelle-based targeting, passive and active targeting strategies, and various advanced drug delivery tools such as functionalized lipidic, polymeric and inorganic nanocarriers. Together, the twenty-three chapters cover a wide range of topics in the field, including tumor and hepatic targeting, polymer-drug conjugates, nanoemulsion, physical and biophysical characteristics of nanoparticles, and in vivo imaging techniques, among others. The book also examines advanced characterization techniques, regulatory hurdles and toxicity-related issues that are key features for successful commercialization of targeted drug delivery system products. Targeted Drug Delivery is a comprehensive reference guide for drug delivery researchers, both beginners and those already working in the field.
Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design. Section VII looks at Trends and Perspectives in the pharmaceuticals market. - Critical reviews of the previous year's literature in many topics of interest to medicinal chemists - Highlights major developments in medicinal chemistry - Includes a comprehensive set of cumulative indices to easily locate topics in all published volumes