Drug-like Properties: Concepts, Structure Design and Methods PDF Download
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Author: Li Di
Publisher: Elsevier
ISBN: 0080557619
Category : Science
Languages : en
Pages : 549
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Book Description
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
Author: Li Di
Publisher: Elsevier
ISBN: 0080557619
Category : Science
Languages : en
Pages : 549
Get Book Here
Book Description
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
Author: Richard B. Silverman
Publisher: Elsevier
ISBN: 0080513379
Category : Science
Languages : en
Pages : 650
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Book Description
Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. - New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations - Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years - Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization
Author: Vladimir Pliska
Publisher: Wiley-VCH
ISBN:
Category : Medical
Languages : en
Pages : 472
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Book Description
In keeping with the outstanding importance of lipophilicity in biosciences, this volume examines all its facets in more than twenty contributions from leading experts. It offers a thorough and highly topical survey of this rapidly developing field of research. Color plates demonstrating structural aspects, a vast number of references, and the straightforward presentation of the material make this volume a invaluable tool for all researchers involved in drug design or in the investigation of drug action.
Author: Jennifer B. Dressman
Publisher: CRC Press
ISBN: 1420077341
Category : Medical
Languages : en
Pages : 432
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Book Description
Oral Drug Absorption, Second Edition thoroughly examines the special equipment and methods used to test whether drugs are released adequately when administered orally. The contributors discuss methods for accurately establishing and validating in vitro/in vivo correlations for both MR and IR formulations, as well as alternative approaches for MR an
Author: E. J. Ariëns
Publisher: Elsevier
ISBN: 1483152693
Category : Medical
Languages : en
Pages : 397
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Book Description
Physico-Chemical Aspects of Drug Action, Volume 7 covers topics on drug kinetics and the overall physicochemical properties of the drug in relation therewith, and the physicochemical aspects of the drug-receptor interaction, putting emphasis on receptor mechanisms and specific properties required for certain types of drugs in this respect. The book starts with some contributions dealing with various general aspects of drug kinetics followed by some contributions dealing with the relationship between certain physicochemical properties of drug molecules and their action. The text describes the pharmacokinetics and dose-concentration relationships; the time course of the biological response to drugs; and the empirical equations for correlating biological efficiency of organic compounds. The text also describes molecular basis for the action of chemotherapeutic drugs; the structure-activity studies on sulphonamides; and the water extrusion hypothesis. The mathematical treatment of two-point attachment between drug and receptor; the molecular properties and biological activity of catecholamines and certain related compounds; and the structure-activity relationships of diarylcarbinolethers are also considered. The book further tackles quantum mechanically-derived electronic distributions in the conformers of 2-pam; and the molecular basis for the action of certain drugs in the central nervous system. Pharmacologists and chemists will find the book invaluable.
Author: P. Heinrich Stahl
Publisher: John Wiley & Sons
ISBN: 9783906390581
Category : Medical
Languages : en
Pages : 392
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Book Description
This comprehensive up-to-date guide and information source is an instructive companion for all scientists involved in research and development of drugs and, in particular, of pharmaceutical dosage forms. The editors have taken care to address every conceivable aspect of the preparation of pharmaceutical salts and present the necessary theoretical foundations as well as a wealth of detailed practical experience in the choice of pharmaceutically active salts. Altogether, the contributions reflect the multidisciplinary nature of the science involved in selection of suitable salt forms for new drug products.
Author: Jens Brange
Publisher: Springer Science & Business Media
ISBN: 3662025264
Category : Medical
Languages : en
Pages : 108
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Book Description
Galenical pharmacy or galenics is the science dealing with the pro duction of drug substances from raw materials, the purity of such substances, their formulation into pharmaceutical preparations with the desired effects and safety in use, and the quality control, stability and storage of the preparations. The field has taken its name from the Greek physician Galen (131-201 A.D.), who had a profound influence on medicine for many centuries because he collected and systematized the medicinal knowledge of his time. The discovery of insulin is attributed to Banting and Best who, in 1921, prepared an extract of the pancreas of the fetal calf and showed that the extract was capable of reducing the blood sugar level of a diabetic dog. This outstanding discovery gave rise to the rapid develop ment of the manufacture of insulin of bovine and porcine origin. By 1925, two Danish manufacturers of insulin preparations were established; both have since been in the forefront ofthe development of insulin preparations, the latest achievement being the marketing of human insulin by Novo in 1982. The development of highly purified human insulin produced semisynthetically from porcine insulin or by DNA recombinant methods are significant contributions to safe and efficient insulin therapy. Insulin is a protein which is destroyed in the gastrointestinal tract.
Author: S. N. Pandeya
Publisher: New Age International
ISBN: 9788122409437
Category : Drugs
Languages : en
Pages : 228
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Book Description
The Book Entitled, An Introduction To Drug Design Aims To Optimize The Discovery Of Drugs At A Low Cost And On Occasions To Change Their Pharmacokinetic And Pharmacodyanamic Properties. The Introductory Chapter Which Forms The Basis Of Drug Discovery Is Followed By The Present-Day Thinking Regarding The Best Approaches To Drug Discovery Are Considered. Similarly, There Have Been Major Advances In The Employment Of Computers In Structure-Activity Analysis, And A Discussion Of The State Of The Art In This Area Is Also Included.The Chapter On Qsar Highlights The Role Of Physico-Chemical Parameters In Predicting The Future Course Of Drug Discovery With Rational Drug Design. The Role Of Enzymes In Drug Action Is Well Established, And A Chapter On Design Of Enzyme Inhibitors Is Well Documented. In Addition, The Increased Understanding Of The Design And Utilisation Of Prodrugs Has Led To A Discussion Of The Relevant Issues In This Text.Thus The Book Will Fill The Need Of A Text For Designing New Drugs And The Principles Of New Drug Discovery.
Author: E. J. Ariens
Publisher:
ISBN:
Category : Drugs
Languages : en
Pages : 0
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Book Description
Author: Matthew E. Cross
Publisher: Cambridge University Press
ISBN: 1107615887
Category : Medical
Languages : en
Pages : 439
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Book Description
A quick reference to basic science for anaesthetists, containing all the key information needed for FRCA exams.
