Fundamentals Of Medicinal Chemistry And Drug Metabolism

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Fundamentals of Medicinal Chemistry and Drug Metabolism

M. O. Faruk Khan,Ashok Philip
Fundamentals of Medicinal Chemistry and Drug Metabolism Book PDF

Author : M. O. Faruk Khan,Ashok Philip
Publisher : Bentham Science Publishers
Page : 349 pages
File Size : 45,9 Mb
Release : 2018-06-01
Category : Medical
ISBN : 9781681086873

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Fundamentals of Medicinal Chemistry and Drug Metabolism by M. O. Faruk Khan,Ashok Philip Pdf

The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of chemical basis of drug action. This first volume of the series is comprised of 8 chapters focusing on basic background information about medicinal chemistry. It takes a succinct and conceptual approach to introducing important fundamental concepts required for a clear understanding of various facets of pharmacotherapeutic agents, drug metabolism and important biosynthetic pathways that are relevant to drug action. Notable topics covered in this first volume include the scope and importance of medicinal chemistry in pharmacy education, a comprehensive discussion of the organic functional groups present in drugs, and information about four major types of biomolecules (proteins, carbohydrates, lipids, nucleic acids) and key heterocyclic ring systems. The concepts of acid-base chemistry and salt formation, and their applications to the drug action and design follow thereafter. These include concepts of solubility and lipid-water partition coefficient (LWPC), isosterism, stereochemical properties, mechanisms of drug action, drug receptor interactions critical for pharmacological responses of drugs, and much more. Students and teachers will be able to integrate the knowledge presented in the book and apply medicinal chemistry concepts to understand the pharmacodynamics and pharmacokinetics of therapeutic agents in the body.

Fundamentals of Medicinal Chemistry

Gareth Thomas
Fundamentals of Medicinal Chemistry Book PDF

Author : Gareth Thomas
Publisher : John Wiley & Sons
Page : 302 pages
File Size : 43,9 Mb
Release : 2004-04-20
Category : Science
ISBN : 9780470871690

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Fundamentals of Medicinal Chemistry by Gareth Thomas Pdf

Provides a concise introduction to the chemistry of therapeutically active compounds, written in a readable and accessible style. The title begins by reviewing the structures and nomenclature of the more common classes of naturally occurring compounds found in biological organisms. An overview of medicinal chemistry is followed by chapters covering the discovery and design of drugs, pharmacokinetics and drug metabolism, The book concludes with a chapter on organic synthesis, followed by a brief look at drug development from the research stage through to marketing the final product. The text assumes little in the way of prior biological knowledge. relevant biology is included through biological topics, examples and the Appendices. Incorporates summary sections, examples, applications and problems Each chapter contains an additional summary section and solutions to the questions are provided at the end of the text Invaluable for undergraduates studying within the chemical, pharmaceutical and life sciences.

Pharmacokinetics and Metabolism in Drug Design

Dennis A. Smith,Charlotte Allerton,Amit S. Kalgutkar,Han van de Waterbeemd,Don K. Walker
Pharmacokinetics and Metabolism in Drug Design Book PDF

Author : Dennis A. Smith,Charlotte Allerton,Amit S. Kalgutkar,Han van de Waterbeemd,Don K. Walker
Publisher : John Wiley & Sons
Page : 269 pages
File Size : 49,5 Mb
Release : 2012-05-14
Category : Medical
ISBN : 9783527329540

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Pharmacokinetics and Metabolism in Drug Design by Dennis A. Smith,Charlotte Allerton,Amit S. Kalgutkar,Han van de Waterbeemd,Don K. Walker Pdf

In this new edition of a bestseller, all the contents have been brought upto-date by addressing current standards and best practices in the assessment and prediction of ADMET properties. Although the previous chapter layout has been retained, substantial revisions have been made, with new topics such as pro-drugs, active metabolites and transporters covered in detail in a manner useful to the Drug Discovery scientist. The authors discuss the parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects. Uniquely comprehensive, the book relates physicochemistry and chemical structure to pharmacokinetic properties and ultimately drug efficacy and safety.

Pharmacokinetics and Metabolism in Drug Design

Dennis A. Smith,Han van de Waterbeemd,Don K. Walker
Pharmacokinetics and Metabolism in Drug Design Book PDF

Author : Dennis A. Smith,Han van de Waterbeemd,Don K. Walker
Publisher : John Wiley & Sons
Page : 207 pages
File Size : 44,8 Mb
Release : 2006-08-21
Category : Medical
ISBN : 9783527608287

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Pharmacokinetics and Metabolism in Drug Design by Dennis A. Smith,Han van de Waterbeemd,Don K. Walker Pdf

In this new edition of a bestseller, all the contents have been updated and new material has been added, especially in the areas of toxicity testing and high throughput analysis. The authors, all of them employed at Pfizer in the discovery and development of new active substances, discuss the significant parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. They cover everything from the fundamental principles right up to the impact of pharmacokinetic parameters on the discovery of new drugs. While aimed at all those dealing professionally with the development and application of pharmaceutical substances, the readily comprehensible style makes this book equally suitable for students of pharmacy and related subjects.

Metabolism, Pharmacokinetics, and Toxicity of Functional Groups

Dennis A. Smith
Metabolism Pharmacokinetics and Toxicity of Functional Groups Book PDF

Author : Dennis A. Smith
Publisher : Royal Society of Chemistry
Page : 545 pages
File Size : 47,9 Mb
Release : 2010
Category : Medical
ISBN : 9781849730167

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Metabolism, Pharmacokinetics, and Toxicity of Functional Groups by Dennis A. Smith Pdf

Written by medicinal chemists and ADMET scientists with a combined experience of over 300 years this aid to discovering drugs provides detailed coverage on absorption, distribution, metabolism, excretion and toxicology issues associated with new drugs.

Drug Metabolism Prediction

Johannes Kirchmair
Drug Metabolism Prediction Book PDF

Author : Johannes Kirchmair
Publisher : John Wiley & Sons
Page : 538 pages
File Size : 45,7 Mb
Release : 2014-08-25
Category : Medical
ISBN : 9783527335664

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Drug Metabolism Prediction by Johannes Kirchmair Pdf

The first professional reference on this highly relevant topic, for drug developers, pharmacologists and toxicologists. The authors provide more than a systematic overview of computational tools and knowledge bases for drug metabolism research and their underlying principles. They aim to convey their expert knowledge distilled from many years of experience in the field. In addition to the fundamentals, computational approaches and their applications, this volume provides expert accounts of the latest experimental methods for investigating drug metabolism in four dedicated chapters. The authors discuss the most important caveats and common errors to consider when working with experimental data. Collating the knowledge gained over the past decade, this practice-oriented guide presents methods not only used in drug development, but also in the development and toxicological assessment of cosmetics, functional foods, agrochemicals, and additives for consumer goods, making it an invaluable reference in a variety of disciplines.

Pharmacokinetics and Metabolism in Drug Design, Volume 13

Dennis A. Smith,Han van de Waterbeemd,Don K. Walker
Pharmacokinetics and Metabolism in Drug Design Volume 13 Book PDF

Author : Dennis A. Smith,Han van de Waterbeemd,Don K. Walker
Publisher : Wiley-VCH
Page : 172 pages
File Size : 49,6 Mb
Release : 2001
Category : Medical
ISBN : UOM:39015056694030

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Pharmacokinetics and Metabolism in Drug Design, Volume 13 by Dennis A. Smith,Han van de Waterbeemd,Don K. Walker Pdf

The medical benefits of a drug are not only dependent on its biological effect, but also on its "life cycle" within the organism - from its absorption into the blood, distribution to tissue until its eventual breakdown or excretion by the liver and kidneys. This book explains in readily comprehensible terms the problems that may arise, and how these may be taken into account at an early stage in drug development.

Drug-like Properties: Concepts, Structure Design and Methods

Li Di,Edward H Kerns
Drug like Properties Concepts Structure Design and Methods Book PDF

Author : Li Di,Edward H Kerns
Publisher : Elsevier
Page : 549 pages
File Size : 41,7 Mb
Release : 2010-07-26
Category : Science
ISBN : 9780080557618

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Drug-like Properties: Concepts, Structure Design and Methods by Li Di,Edward H Kerns Pdf

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint

The Art of Drug Synthesis

Douglas S. Johnson,Jie Jack Li
The Art of Drug Synthesis Book PDF

Author : Douglas S. Johnson,Jie Jack Li
Publisher : John Wiley & Sons
Page : 295 pages
File Size : 50,7 Mb
Release : 2013-02-26
Category : Science
ISBN : 9781118678466

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The Art of Drug Synthesis by Douglas S. Johnson,Jie Jack Li Pdf

The Art of Drug Synthesis illustrates how chemistry, biology, pharmacokinetics, and a host of other disciplines come together to produce successful medicines. The authors have compiled a collection of 21 representative categories of drugs, from which they have selected as examples many of the best-selling drugs on the market today. An introduction to each drug is provided, as well as background to the biology, pharmacology, pharmacokinetics, and drug metabolism, followed by a detailed account of the drug synthesis. Edited by prominent scientists working in drug discovery for Pfizer Meets the needs of a growing community of researchers in pharmaceutical R&D Provides a useful guide for practicing pharmaceutical scientists as well as a text for medicinal chemistry students An excellent follow-up to the very successful first book by these editors, Contemporary Drug Synthesis, but with all new therapeutic categories and drugs discussed.

Drug Metabolism

Corina Ionescu,Mino R. Caira
Drug Metabolism Book PDF

Author : Corina Ionescu,Mino R. Caira
Publisher : Springer Science & Business Media
Page : 444 pages
File Size : 55,6 Mb
Release : 2006-02-28
Category : Medical
ISBN : 1402041411

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Drug Metabolism by Corina Ionescu,Mino R. Caira Pdf

Drug Metabolism: Current Concepts provides a comprehensive understanding of the processes that take place following ingestion of a medicinal agent or xenobiotic, with an emphasis on the crucial role of metabolism (biotransformation). How a sound knowledge of these phenomena is incorporated into the design of effective new drug candidates is also explained. The user-friendly text focuses on concepts rather than extraneous details and is supported by many illustrated examples of biotransformations as well as frequent references to current critical reviews and articles highlighting the nature of research objectives in this vibrant area of medicinal development. The final topic on strategies for drug design relies on the background provided by the rest of the book. This book is ideally suited as an advanced text for courses in drug metabolism for students of medicine, pharmacy, pharmacology, biochemistry; and for courses in drug design and drug delivery for students of medicinal chemistry. It is also appropriate for professional seminars or courses that relate to the fate of a drug in the body, drug interactions, adverse reactions and drug design.

Reactive Drug Metabolites

Amit S. Kalgutkar,Deepak Dalvie,R. Scott Obach,Dennis A. Smith
Reactive Drug Metabolites Book PDF

Author : Amit S. Kalgutkar,Deepak Dalvie,R. Scott Obach,Dennis A. Smith
Publisher : John Wiley & Sons
Page : 445 pages
File Size : 48,8 Mb
Release : 2012-09-06
Category : Medical
ISBN : 9783527655762

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Reactive Drug Metabolites by Amit S. Kalgutkar,Deepak Dalvie,R. Scott Obach,Dennis A. Smith Pdf

Closing a gap in the scientifi c literature, this first comprehensive introduction to the topic is based on current best practice in one of the largest pharmaceutical companies worldwide. The first chapters trace the development of our understanding of drug metabolite toxicity, covering basic concepts and techniques in the process, while the second part details chemical toxicophores that are prone to reactive metabolite formation. This section also reviews the various drug-metabolizing enzymes that can participate in catalyzing reactive metabolite formation, including a discussion of the structure-toxicity relationships for drugs. Two chapters are dedicated to the currently hot topics of herbal constituents and IADRs. The next part covers current strategies and approaches to evaluate the reactive metabolite potential of new drug candidates, both by predictive and by bioanalytical methods. There then follows an in-depth analysis of the toxicological potential of the top 200 prescription drugs, illustrating the power and the limits of the toxicophore concept, backed by numerous case studies. Finally, a risk-benefi t approach to managing the toxicity risk of reactive metabolite-prone drugs is presented. Since the authors carefully develop the knowledge needed, from fundamental considerations to current industry standards, no degree in pharmacology is required to read this book, making it perfect for medicinal chemists without in-depth pharmacology training.

Drug Metabolism in Drug Design and Development

Donglu Zhang,Mingshe Zhu,William G. Humphreys
Drug Metabolism in Drug Design and Development Book PDF

Author : Donglu Zhang,Mingshe Zhu,William G. Humphreys
Publisher : John Wiley & Sons
Page : 448 pages
File Size : 55,6 Mb
Release : 2007-11-16
Category : Science
ISBN : 0470191686

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Drug Metabolism in Drug Design and Development by Donglu Zhang,Mingshe Zhu,William G. Humphreys Pdf

The essentials of drug metabolism vital to developing new therapeutic entities Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers: * Basic concepts of drug metabolism * The role of drug metabolism in the pharmaceutical industry * Analytical techniques in drug metabolism * Common experimental approaches and protocols Drug Metabolism in Drug Design and Development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques. This is a comprehensive, hands-on reference for drug metabolism researchers as well as other professionals involved in pre-clinical drug discovery and development.

Basic Concepts in Medicinal Chemistry

Marc Harrold,Robin Zavod
Basic Concepts in Medicinal Chemistry Book PDF

Author : Marc Harrold,Robin Zavod
Publisher : ASHP
Page : 405 pages
File Size : 44,8 Mb
Release : 2013-01-18
Category : Medical
ISBN : 9781585283644

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Basic Concepts in Medicinal Chemistry by Marc Harrold,Robin Zavod Pdf

Medicinal chemistry is a complex topic. Written in an easy to follow and conversational style, Basic Concepts in Medicinal Chemistry focuses on the fundamental concepts that govern the discipline of medicinal chemistry as well as how and why these concepts are essential to therapeutic decisions. The book emphasizes functional group analysis and the basics of drug structure evaluation. In a systematic fashion, learn how to identify and evaluate the functional groups that comprise the structure of a drug molecule and their influences on solubility, absorption, acid/base character, binding interactions, and stereochemical orientation. Relevant Phase I and Phase II metabolic transformations are also discussed for each functional group. Key features include: • Discussions on the roles and characteristics of organic functional groups, including the identification of acidic and basic functional groups. • How to solve problems involving pH, pKa, and ionization; salts and solubility; drug binding interactions; stereochemistry; and drug metabolism. • Numerous examples and expanded discussions for complex concepts. • Therapeutic examples that link the importance of medicinal chemistry to pharmacy and healthcare practice. • An overview of structure activity relationships (SARs) and concepts that govern drug design. • Review questions and practice problems at the end of each chapter that allow readers to test their understanding, with the answers provided in an appendix. Whether you are just starting your education toward a career in a healthcare field or need to brush up on your organic chemistry concepts, this book is here to help you navigate medicinal chemistry. About the Authors Marc W. Harrold, BS, Pharm, PhD, is Professor of Medicinal Chemistry at the Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA. Professor Harrold is the 2011 winner of the Omicron Delta Kappa "Teacher of the Year" award at Duquesne University. He is also the two-time winner of the "TOPS" (Teacher of the Pharmacy School) award at the Mylan School of Pharmacy. Robin M. Zavod, PhD, is Associate Professor for Pharmaceutical Sciences at the Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, where she was awarded the 2012 Outstanding Faculty of the Year award. Professor Zavod also serves on the adjunct faculty for Elmhurst College and the Illinois Institute of Technology. She currently serves as Editor-in-Chief of the journal Currents in Pharmacy Teaching and Learning.

Medicinal Chemistry

Gareth Thomas
Medicinal Chemistry Book PDF

Author : Gareth Thomas
Publisher : John Wiley & Sons
Page : 660 pages
File Size : 47,6 Mb
Release : 2011-09-20
Category : Science
ISBN : 9781119965428

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Medicinal Chemistry by Gareth Thomas Pdf

Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and multidisciplinary area of research. Building on the success of the First Edition, this edition has been completely revised and updated to include the latest developments in the field. Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles, assuming little in the way of prior knowledge. The book focuses on the chemical principles used for drug discovery and design covering physiology and biology where relevant. It opens with a broad overview of the subject with subsequent chapters examining topics in greater depth. From the reviews of the First Edition: "It contains a wealth of information in a compact form" ANGEWANDTE CHEMIE, INTERNATIONAL EDITION "Medicinal Chemistry is certainly a text I would chose to teach from for undergraduates. It fills a unique niche in the market place." PHYSICAL SCIENCES AND EDUCATIONAL REVIEWS

Enzyme Inhibition in Drug Discovery and Development

Chuang Lu,Albert P. Li
Enzyme Inhibition in Drug Discovery and Development Book PDF

Author : Chuang Lu,Albert P. Li
Publisher : John Wiley & Sons
Page : 878 pages
File Size : 49,8 Mb
Release : 2010-01-26
Category : Medical
ISBN : 9780470538944

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Enzyme Inhibition in Drug Discovery and Development by Chuang Lu,Albert P. Li Pdf

The science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions—desirable pharmacological effects—and "bad" inhibitions—drug–drug interactions and toxicity. The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug–drug interactions The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.