1.

Record Nr.

UNINA9910453434903321

Autore

Kerns Edward Harvel

Titolo

Drug-like properties [[electronic resource] ] : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di

Pubbl/distr/stampa

Amsterdam ; ; Boston, : Academic Press, c2008

ISBN

1-281-76371-3

9786611763718

0-08-095162-7

0-08-055761-9

Descrizione fisica

1 online resource (549 p.)

Altri autori (Persone)

DiLi

Disciplina

615/.19

Soggetti

Pharmaceutical chemistry

Drugs - Structure-activity relationships

Drug development

Drugs - Design

Electronic books.

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

Description based upon print version of record.

Nota di bibliografia

Includes bibliographical references (p. 492) and index.

Nota di contenuto

Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties

2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and



Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane

3.4.2 Passive Diffusion at the Molecular Level3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties

Chapter 4 Rules for Rapid Property Profiling from Structure4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals

7.1.1 Solubility Varies with Structure and Physical Conditions7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract

7.3.2 Species Differences in Gastrointestinal Tract

Sommario/riassunto

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,



2.

Record Nr.

UNINA9910483777703321

Autore

Zhang Qizhi

Titolo

An Introduction to Chinese History and Culture / / by Qizhi Zhang

Pubbl/distr/stampa

Berlin, Heidelberg : , : Springer Berlin Heidelberg : , : Imprint : Springer, , 2015

ISBN

3-662-46482-9

Edizione

[1st ed. 2015.]

Descrizione fisica

1 online resource (472 p.)

Collana

China Academic Library, , 2195-1853

Disciplina

300

306

900

Soggetti

Cultural studies

History

Cultural Studies

History, general

Lingua di pubblicazione

Inglese

Formato

Materiale a stampa

Livello bibliografico

Monografia

Note generali

Description based upon print version of record.

Nota di contenuto

Chapter 1: A Scientific Approach to the Origins of Chinese Civilization -- Chapter 2: Ancient Chinese Society and the Change of Dynasties -- Chapter 3: The Golden Ages of the Han, Tang and Qing Dynasties: a Comparative Analysis -- Chapter 4: Transportation Systems and Cultural Communication in Ancient China -- Chapter 5: Ethnic Relations in Chinese History -- Chapter 6: The Systems of Politics, Law and Selecting Officials in Ancient China -- Chapter 7: Agriculture, Handicraft and Commerce in Ancient China -- Chapter 8: The Military Thought and Military Systems of Ancient China -- Chapter 9: The Rich and Colorful Social Life in Ancient China -- Chapter 10: The Evolution of Ancient Chinese Thought -- Chapter 11: The Treasure House of Ancient Chinese Literature and Art -- Chapter 12: The Emergence and Progress of Ancient Chinese Historiography -- Chapter 13: Reflection on Ancient Chinese Science and Technology -- Chapter 14: New Issues in the Modern History of China -- Chapter 15: A General Progression to the Socialist Modernization of the People's Republic of China.

Sommario/riassunto

This book breaks with convention and provides an overview of Chinese history in the form of special topics. These topics include the major



issues of “A Scientific Approach to the Origins of Chinese Civilization,” “Ancient Chinese Society and the Change of Dynasties,” “The Golden Ages of the Han, Tang and Qing Dynasties: a Comparative Analysis,” “Transportation Systems and Cultural Communication in Ancient China,” “Ethnic Relations in Chinese History,”“The Systems of Politics, Law and Selecting Officials in Ancient China,”“Agriculture, Handicraft and Commerce in Ancient China,” “The Military Thought and Military Systems of Ancient China,” “The Rich and Colorful Social Life in Ancient China,” “The Evolution of Ancient Chinese Thought,” “The Treasure House of Ancient Chinese Literature and Art,” “The Emergence and Progress of Ancient Chinese Historiography,” “Reflection on Ancient Chinese Science and Technology,” “New Issues in the Modern History of China,” and “A General Progression to the Socialist Modernization of the People’s Republic of China.” The book is based on current literature and research by university students. The modern history section is relatively concise, while the topics related to ancient Chinese history are longer, reflecting the country’s rich history and corresponding wealth of materials. There is also an in-depth discussion on the socialist modernization of the People’s Republic of China. The book provides insights into Chinese history, allowing readers “to see the value of civilization through history; to see the preciseness of history through civilization.”  It focuses on the social background, lifestyle and development processes to illustrate ideologies and ideas.