November 23, 2020

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Prodrug Design

Prodrug Design
Author : Vivekkumar K Redasani,Sanjay B. Bari
Publisher : Academic Press
Release Date : 2015-07-07
Category : Science
Total pages :84
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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
Author : Rafik Karaman
Publisher : Nova Science Pub Incorporated
Release Date : 2014-07-01
Category : Medical
Total pages :277
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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.

Design of Prodrugs

Design of Prodrugs
Author : Hans Bundgaard
Publisher : Elsevier Publishing Company
Release Date : 1985
Category : Biopharmaceutics
Total pages :360
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Hydrolysis in Drug and Prodrug Metabolism

Hydrolysis in Drug and Prodrug Metabolism
Author : Bernard Testa,Joachim M. Mayer,Joachim Mayer
Publisher : John Wiley & Sons
Release Date : 2003-08
Category : Science
Total pages :780
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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.

Prodrugs

Prodrugs
Author : Valentino Stella,Ronald Borchardt,Michael Hageman,Reza Oliyai,Hans Maag,Jefferson Tilley
Publisher : Springer Science & Business Media
Release Date : 2007-03-12
Category : Medical
Total pages :1464
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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.

Prodrugs and Targeted Delivery

Prodrugs and Targeted Delivery
Author : Jarkko Rautio
Publisher : John Wiley & Sons
Release Date : 2011-01-11
Category : Medical
Total pages :520
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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.

Textbook of Drug Design and Discovery, Third Edition

Textbook of Drug Design and Discovery, Third Edition
Author : Tommy Liljefors,Povl Krogsgaard-Larsen,Ulf Madsen
Publisher : CRC Press
Release Date : 2002-07-25
Category : Medical
Total pages :592
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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.

Advances in Prodrug Design for Parkinson's Disease

Advances in Prodrug Design for Parkinson's Disease
Author : Anonim
Publisher : Unknown
Release Date : 2018
Category :
Total pages :129
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ABSTRACT: Introduction : Parkinson's Disease (PD) is a neurodegenerative disorder of the central nervous system (CNS) characterized by motor dysfunctions, such as bradykinesia, rigidity, neuropsychiatric symptoms, and others. The pharmacological treatment of the disease is only symptomatic since, to date, there is no treatment to stop or slow PD. Currently, L-Dopa (LD) remains the gold standard therapy even though it undergoes peripheral metabolism causing several side effects, such as nausea, vomiting and orthostatic hypotension. Areas covered : This review is focused on recent developments in strategies involving prodrugs to enhance DA and/or LD absorption, their chemical and enzymatic stabilities, and selective targeting to the central nervous system. Expert opinion : The prodrug strategy remains one of the most promising approaches to improve pharmaceutical, pharmacokinetic, and pharmacodynamic properties of hydrophilic compounds, such as anti-Parkinson drugs (DA and LD). Prodrugs developed in recent years have demonstrated good pharmacokinetic profiles, affording a sustained release of LD and reducing its plasma level fluctuations. The development of new prodrugs that may reach the BBB unaltered and with a good ADME (Absorption, Distribution, Metabolism, Elimination) profile and pharmacological efficacy represents an exciting challenge for medicinal chemists.

Gibaldi's Drug Delivery Systems in Pharmaceutical Care

Gibaldi's Drug Delivery Systems in Pharmaceutical Care
Author : Mary Lee,Archana Desai
Publisher : ASHP
Release Date : 2007
Category : Medical
Total pages :525
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It is important to make therapeutics a critical component of teaching about dosage forms and to make dosage forms and drug delivery systems an integral part of therapeutics. This book will be the first to focus on the therapeutic impact of drug dosage forms.Tying together concepts of traditional pharmaceutics with therapeutics, Drug Delivery Systemsin Pharmaceutical Care demonstrates how the modern clinical pharmacist can integrate knowledge in pharmaceutical sciences and therapeutics with appreciation of patient needs and nuances to advise on preferable and optimal product choices.Each chapter represents a collaboration of a clinical pharmacist practitioner and a pharmaceutical scientist. This unique perspective takes the science of dosage form design and helps translate the theory into the pragmatic.Special Features: Case studies and problems to help students get a better understanding of concepts Well-organized chapters with outlines and objectives Summary tables and helpful figures, along with reasonable compilations of original references Final sections with 'Learning Points' that reinforce essential material. Foreword by William J. Jusko, PhD, Professor and Chair, University of Buffalo, Department of Pharmaceutical Sciences

Drug Absorption Evaluation, Prodrug Design and Intestinal Transporter Expression by Genechip Analysis

Drug Absorption Evaluation, Prodrug Design and Intestinal Transporter Expression by Genechip Analysis
Author : Duxin Sun
Publisher : Unknown
Release Date : 2002
Category :
Total pages :129
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Enzyme-Prodrug Strategies for Cancer Therapy

Enzyme-Prodrug Strategies for Cancer Therapy
Author : Roger G. Melton,Richard J. Knox
Publisher : Springer Science & Business Media
Release Date : 2012-12-06
Category : Medical
Total pages :257
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Antibody-directed enzyme prodrug therapy (ADEPT) directly addresses the major problem in cancer chemotherapy-its lack of selectivity. Antibody delivery combined with the amplification provided by the enzymatic activation of prodrugs enables selection to be made between tumour and normal tissue. ADEPT offers a novel field of opportunities in the therapy of systemic cancer and may be a major advance for the treatment of solid tumours. This book is the first to describe ADEPT in detail. Each chapter reviews an aspect of the immunology, enzymology, biochemistry, chemistry, and cancer chemotherapy which have been integrated into the ADEPT concept. An additional chapter describes the related approach of gene-directed enzyme prodrug therapy (GDEPT). This latter approach is still in its infancy but ADEPT has entered the clinic. The initial clinical studies with ADEPT are included and discussed in detail.

Application of Peptide-Based Prodrug Chemistry in Drug Development

Application of Peptide-Based Prodrug Chemistry in Drug Development
Author : Arnab De
Publisher : Springer Science & Business Media
Release Date : 2012-08-18
Category : Medical
Total pages :89
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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).

Peptide Transport and Delivery Into the Central Nervous System

Peptide Transport and Delivery Into the Central Nervous System
Author : Laszlo Prokai,Katalin Prokai-Tatrai
Publisher : Springer Science & Business Media
Release Date : 2003
Category : Medical
Total pages :245
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Various peptides native to the brain and the spinal cord, as well as various synthetic peptides, peptide analogues and peptidomimetics could be useful in the treatment of diseases of the central nervous system. This book provides an overview of the role and neuropharmaceutical potential of these peptides, and discusses the state of the art and future trends in the use of peptide pharmacotherapy involving the brain.

Design of Biopharmaceutical Properties Through Prodrugs and Analogs

Design of Biopharmaceutical Properties Through Prodrugs and Analogs
Author : Edward B. Roche
Publisher : Amer Pharmacutical Assn
Release Date : 1977
Category : Medical
Total pages :455
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Chirality in Drug Design and Development

Chirality in Drug Design and Development
Author : Indra K. Reddy,Reza Mehvar
Publisher : CRC Press
Release Date : 2004-03-15
Category : Science
Total pages :1200
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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 characteristics of specific enantiomers and chiral drug compounds and addresses in one convenient reference all the major challenges pertaining to drug chirality that have been neglected in the literature. Chirality in Drug Design and Development collects the latest studies from an interdisciplinary team of experts on chiral drug design.