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Prodrug Design

Prodrug Design Book
Author : Vivekkumar K Redasani,Sanjay B. Bari
Publisher : Academic Press
Release : 2015-07-07
ISBN : 0128035579
Language : En, Es, Fr & De

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Book Description :

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

Prodrugs Design

Prodrugs Design Book
Author : Rafik Karaman
Publisher : Nova Science Pub Incorporated
Release : 2014-07-01
ISBN : 9781631177019
Language : En, Es, Fr & De

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Book Description :

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 optimized 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 utilized 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 utilized 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 synthesized. Examples of such prodrugs are presented in the different chapters of the book.

Prodrugs and Targeted Delivery

Prodrugs and Targeted Delivery Book
Author : Jarkko Rautio
Publisher : John Wiley & Sons
Release : 2011-01-11
ISBN : 3527633189
Language : En, Es, Fr & De

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Book Description :

This topical reference and handbook addresses the chemistry, pharmacology, toxicology and the patentability of prodrugs, perfectly mirroring the integrated approach prevalent in today's drug design. It summarizes current experiences and strategies for the rational design of prodrugs, beginning at the early stages of the development process, as well as discussing organ- and site-selective prodrugs. Every company employing medicinal chemists will be interested in this practice-oriented overview of a key strategy in modern drug discovery and development.

Design of Prodrugs

Design of Prodrugs Book
Author : Hans Bundgaard
Publisher : Elsevier Publishing Company
Release : 1985
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Download Design of Prodrugs book written by Hans Bundgaard, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Prodrug Designing of Nsaids

Prodrug Designing of Nsaids Book
Author : Smita Patil,Pramod Shirote,Rajendra Doijad
Publisher : LAP Lambert Academic Publishing
Release : 2012
ISBN : 9783843370578
Language : En, Es, Fr & De

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Book Description :

Separation of therapeutic effects from toxicity is a valuable goal in the drug development process. Prodrug design is a part of the general drug discovery process, in which a unique combination of therapeutically active substances is observed to have desirable pharmacological effects. In human therapy prodrug designing has given successful results in overcoming undesirable properties like absorption, nonspecificity, and poor bioavailability and GIT toxicity. Prodrug design is opening new doors in the challenging field of drug discovery, revolutionizing the art of Drug development.In this dissertation work, Synthesis of amide prodrugs of Niflumic acid and Ketoprofen with Glucosamine was achieved in good yields by a simple technique.Here prodrug approach has been successfully applied in attaining the goal of minimized gastrointestinal toxicity without loss of desired anti-inflammatory activities of the drug.

Development of Macromolecular Prodrug Conjugates for the Diagnosis and Treatment of Musculoskeletal Diseases

Development of Macromolecular Prodrug Conjugates for the Diagnosis and Treatment of Musculoskeletal Diseases Book
Author : Xin Wei
Publisher : Unknown
Release : 2018
ISBN : 0987650XXX
Language : En, Es, Fr & De

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Book Description :

Macromolecular prodrug conjugate is a promising strategy for better diagnosis and treatment of musculoskeletal diseases. Our lab has pioneered this effort and has successfully developed multiple prodrug formulations. The general approach we have taken is to incorporate active ingredient (AI, including imaging probe or therapeutic agents) containing monomers into water-soluble and biocompatible polymers, such as N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymers. Structural parameters of these polymeric prodrugs, such as molecular weight (MW), drug loading, prodrug activation mechanism and the selection of drug payload may greatly affect therapeutic efficacy and the safety of the macromolecular prodrugs. To investigate the impact of these structural parameters in my research, (1) We have synthesized a series of the HPMA copolymer-based dexamethasone prodrugs with different molecular weight and drug loading. After labeling with 125I or fluorescent dye, these prodrugs were administered to a murine implant loosening model. The in vivo/ex vivo pharmacokinetics and biodistribution of these polymers and in vitro and in vivo cellular internalization were analyzed and compared. (2) We designed and synthesized dexamethasone-containing monomers with different releasing chemistry and copolymerized with HPMA. The different in vitro releasing rates of these prodrugs were confirmed. When evaluated in an adjuvant induced arthritis rat model, these prodrugs demonstrated significantly different therapeutic efficacy and duration. (3) To understand if the design principle we learned from the dexamethasone prodrug can be extrapolated to other class of drugs, we replaced dexamethasone with Tofacitinib (Tofa, a disease-modifying antirheumatic drug or DMARD) in the prodrug design. The resulting prodrug (P-Tofa) was found to effectively ameliorate joint inflammation of the adjuvant-induced arthritis rat model. Collectively, the results from these systematic investigations provide us with more insight into the polymeric prodrug design principle and are instructive for the future development and clinical translation of the macromolecular prodrugs for musculoskeletal and other relevant diseases.

Hydrolysis in Drug and Prodrug Metabolism

Hydrolysis in Drug and Prodrug Metabolism Book
Author : Bernard Testa,Joachim M. Mayer,Joachim Mayer
Publisher : John Wiley & Sons
Release : 2003-08
ISBN : 9783906390253
Language : En, Es, Fr & De

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Book Description :

Many drugs and other xenobiotics (e.g., preservatives, insecticides, and plastifiers) contain hydrolyzable moieties such as ester or amide groups. In biological media, such foreign compounds are, therefore, important substrates for hydrolytic reactions catalyzed by hydrolases or proceeding non-enzymatically. Despite their significance, until now, no book has been dedicated to hydrolysis and hydrolases in the metabolism of drugs and other xenobiotics. This work fills a gap in the literature and reviews metabolic reactions of hydrolysis and hydarion from the point of views of enzymes, substrates, and reactions.

Recent Advancement in Prodrugs

Recent Advancement in Prodrugs Book
Author : Kamal Shah,Durgesh Nandini Chauhan,Nagendra Singh Chauhan,Pradeep Mishra
Publisher : CRC Press
Release : 2020-05-13
ISBN : 1000057992
Language : En, Es, Fr & De

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Book Description :

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.

Use of the Combination of Prodrug Design and Salt Optimization

Use of the Combination of Prodrug Design and Salt Optimization Book
Author : Anders Bach Nielsen
Publisher : Unknown
Release : 2004
ISBN : 9788778346339
Language : En, Es, Fr & De

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Book Description :

Download Use of the Combination of Prodrug Design and Salt Optimization book written by Anders Bach Nielsen, available in PDF, EPUB, and Kindle, or read full book online anywhere and anytime. Compatible with any devices.

Textbook of Drug Design and Discovery Third Edition

Textbook of Drug Design and Discovery  Third Edition Book
Author : Tommy Liljefors,Povl Krogsgaard-Larsen,Ulf Madsen
Publisher : CRC Press
Release : 2002-07-25
ISBN : 9780415282888
Language : En, Es, Fr & De

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Book Description :

Building on the success of the previous editions, Textbook of Drug Design and Discovery has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The book follows drug design from the initial lead identification through optimization and structure-activity relationship with reference to the final processes of clinical evaluation and registration. Chapters investigate the design of enzyme inhibitors and drugs for particular cellular targets such as ion channels and receptors, and also explore specific classes of drug such as peptidomimetics, antivirals and anticancer agents. The use of gene technology in pharmaceutical research, computer modeling techniques, and combinatorial approaches are also included.

Drug Discovery Handbook

Drug Discovery Handbook Book
Author : Shayne Cox Gad
Publisher : John Wiley & Sons
Release : 2005-07-08
ISBN : 0471728772
Language : En, Es, Fr & De

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Book Description :

The Drug Discovery Handbook gives professionals a tool tofacilitate drug discovery by bringing together, for the first timein one resource, a compendium of methods and techniques that needto be considered when developing new drugs. This comprehensive, practical guide presents an explanation of thelatest techniques and methods in drug discovery, including: Genomics, proteomics, high-throughput screening, and systemsbiology Summaries of how these techniques and methods are used todiscover new central nervous system agents, antiviral agents,respiratory drugs, oncology drugs, and more Specific approaches to drug discovery, including problems thatare encountered, solutions to these problems, and limitations ofvarious methods and techniques The thorough coverage and practical, scientifically validproblem-solving approach of Drug Discovery Handbook will serve asan invaluable aid in the complex task of developing new drugs.

Textbook of Drug Design and Discovery

Textbook of Drug Design and Discovery Book
Author : Kristian Stromgaard,Povl Krogsgaard-Larsen,Ulf Madsen
Publisher : CRC Press
Release : 2009-10-07
ISBN : 1439882401
Language : En, Es, Fr & De

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Book Description :

The molecular biological revolution and the mapping of the human genome continue to provide new challenges and opportunities for drug research and design. Future medicinal chemists and drug designers must have a firm background in a number of related scientific disciplines in order to understand the conversion of new insight into lead structures an

Chirality in Drug Design and Development

Chirality in Drug Design and Development Book
Author : Indra K. Reddy,Reza Mehvar
Publisher : CRC Press
Release : 2004-03-15
ISBN : 9780203021811
Language : En, Es, Fr & De

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Book Description :

Covering every essential element in the development of chiral products, this reference provides a solid overview of the formulation, biopharmaceutical characteristics, and regulatory issues impacting the production of these pharmaceuticals. It supports researchers as they evaluate the pharmacodynamic, pharmacokinetic, and toxicological characterist

Application of Peptide Based Prodrug Chemistry in Drug Development

Application of Peptide Based Prodrug Chemistry in Drug Development Book
Author : Arnab De
Publisher : Springer Science & Business Media
Release : 2012-08-18
ISBN : 1461448751
Language : En, Es, Fr & De

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Book Description :

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).

Prodrugs

Prodrugs Book
Author : Valentino Stella,Ronald Borchardt,Michael Hageman,Reza Oliyai,Hans Maag,Jefferson Tilley
Publisher : Springer Science & Business Media
Release : 2007-08-26
ISBN : 0387497854
Language : En, Es, Fr & De

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Book Description :

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.

Computational Drug Design

Computational Drug Design Book
Author : D. C. Young
Publisher : John Wiley & Sons
Release : 2009-01-28
ISBN : 9780470451847
Language : En, Es, Fr & De

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Book Description :

Helps you choose the right computational tools and techniques to meet your drug design goals Computational Drug Design covers all of the major computational drug design techniques in use today, focusing on the process that pharmaceutical chemists employ to design a new drug molecule. The discussions of which computational tools to use and when and how to use them are all based on typical pharmaceutical industry drug design processes. Following an introduction, the book is divided into three parts: Part One, The Drug Design Process, sets forth a variety of design processes suitable for a number of different drug development scenarios and drug targets. The author demonstrates how computational techniques are typically used during the design process, helping readers choose the best computational tools to meet their goals. Part Two, Computational Tools and Techniques, offers a series of chapters, each one dedicated to a single computational technique. Readers discover the strengths and weaknesses of each technique. Moreover, the book tabulates comparative accuracy studies, giving readers an unbiased comparison of all the available techniques. Part Three, Related Topics, addresses new, emerging, and complementary technologies, including bioinformatics, simulations at the cellular and organ level, synthesis route prediction, proteomics, and prodrug approaches. The book's accompanying CD-ROM, a special feature, offers graphics of the molecular structures and dynamic reactions discussed in the book as well as demos from computational drug design software companies. Computational Drug Design is ideal for both students and professionals in drug design, helping them choose and take full advantage of the best computational tools available. Note: CD-ROM/DVD and other supplementary materials are not included as part of eBook file.

Recent Advancement in Prodrugs

Recent Advancement in Prodrugs Book
Author : Kamal Shah,Durgesh Nandini Chauhan,Nagendra Singh Chauhan,Pradeep Mishra
Publisher : CRC Press
Release : 2020-05-13
ISBN : 1000057976
Language : En, Es, Fr & De

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Book Description :

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.