kawapu007

[ 本帖最后由 kawapu007 于 2008-1-22 14:40 编辑 ]

kawapu007

《 创新药物化学》

最新最权威的药物研发参考书
望大家喜欢
【作　者】: [法]Camille. G. Wermuth主编 迟玉明主译
【丛书名】:
【页　数】: 1024
【尺　寸】:
【读秀号】: 000005703095
【出版社】： 世界图书出版公司
【主题词】： 药物化学
【ISBN号】: 7-5062-6405-6
【出版日期】： 2005
【原书定价】： 150.00
【中图法分类号】： R914
文件名称: chem.pdf
文件大小: 59.81MB
文件类型: Adobe Acrobat 7.0 Document
提取文件：[hidr]
http://disk.kkio.com/pick.aspx?code=我爱卡卡,下载后12小时内我一定删除.000[/hide]

[ 本帖最后由 kawapu007 于 2008-1-23 12:47 编辑 ]

kawapu007

《创新药物化学》一书是留学及曾经留学于海外的五十余位青年学者共同翻译的，而且许多人现在仍工作或学习在海外，他们掌握和了解国外新药研究与开发的先进技术和经验，渴望为祖国的医药事业发展作出自己应用的贡献。
    本书共分为八部分43章，包括了从新药发现到新药上市的所有内容，不仅系统阐述了药物化学的传统内容，也详细介绍了新药研究与开发的最新技术和方法，以及各位作者在应用这些方法和技术时的切身体会和独到见解。
    本书的内容翻译准确、通俗易懂，对药物研究工作者和俗从事药物研究的化学工作者以及高等医药院校的广大师生是一本不可多得的参考书，对企业和研究机构领导的决策也具有重要的参考价值。
    作者简介：
    Gamille-Georges Wermuth，博士，教授，Prestwick Chemical公司的创办者。1969年-2002年为法国Louis Pasteur大学药学院有机化学和药物化学教授。早年在法国土伦的法国海军“Centre d'Etudes Phys-iobiologiques Appliquees a la Marine”服役的两年间，就对药物化学产生了浓厚兴趣。当时，他是在Henri Laborit博士的指导下工作，而Henri Laborit博士本人是人工冬眠的发明者，并发现了氯丙嗪（也称做冬眠灵）。

kawapu007

第一部分 药物化学概要
第1章 药物发展简史——从植物提取物到基因技术的变迁
第2章 药物化学的定义和目的，药物作用的3个阶段以及药物和疾病的分类
第3章 药物效果的测定与表示
第4章 药物靶——药物作用的分子机制
第二部分 先导化合物的发现方法
第5章 新先导化合物的探索方法及独自的研究方法
第6章 药物和先导化合物的来源——天然物
第7章 组合化学基础
第8章 分子生物学在新药开发中的应用
第9章 计算机辅助筛选——通过检索数据库发现先导化合物
第10章 高速化学库——类药性的评价
第11章 网络快递——互联网与药物化学
第三部分 构-效关系的基础研究
第12章 同系物的分子多样性——聚乙烯物和联苯物
第13章 等排性置换为基础的分子变换
第14章 环结构的变换
第15章 药物化学中的构象限制和/或空间阻碍
第16章 同分子孪生药物和异分子孪生药物
第17章 药物中的光学异构
第18章 初步构-效关系的研究方法
第四部分 取代基础和官能团（构-效关系的定性和定量方面）
第19章 取代基的效果
第20章 官能团在药物-受体相互作用中的作用
第21章 化合物性质和药物质量
第22章 定量构-效关系
第五部分 立体构型、受体图像和分子模型
第23章 药物作用机制的立体化学因素I（构象限制、立体障碍和疏水性堆积）
第24章 药效团确定和受体图像
第25章 三维定量构-效关系
第26章 蛋白质晶体学与药物开发
第27章 蛋白质相似模型的建立与新药的发现
第28章 从激动剂转变为拮抗剂（对称性和其他相关问题）
第29章 拟肽的设计
第六部分 影响药动学性质的化学修饰
第30章 体内药物的动态
第31章 生物转化反应
第32章 药物设计的基础知识——药物毒性的化学机制
第33章 前体药物和生物前体的设计
第34章 靶向药物的大分子载体
第七部分 药物和制剂上的化学问题
……
第八部分 新药开发的法律和经济问题
索引

kawapu007

[ 本帖最后由 kawapu007 于 2008-1-22 15:55 编辑 ]

kawapu007

Table of Contents

A Brief History Of Drugs; From Plant Extracts To DNA Technology.
Medicinal Chemistry: Definition And Objectives, The Three Main Phases Of Drug Activity, Drug And Diseases Classifications.
Measurement And Expression Of Drug Effects.
Drug Targets: Molecular Mechanisms Of Drug Action.
Strategies In The Search For New Lead Compounds Or Original Working Hypotheses.
Natural Products As Pharmaceuticals And Sources For Lead Structures.
Basics Of Combinatorial Chemistry.
The Contribution Of Molecular Biology To Drug Discovery.
Electronic Screening: Lead Finding From Database Mining.
High-Speed Chemistry Libraries: Assessment Of Drug-Likeness.
Web Alert — Using The Internet For Medicinal Chemistry.
Molecular Variations In Homologous Series: Vinylogues And Benzologues.
Molecular Variations Based On Isosteric Replacements.
Ring Transformations.
Introduction Of Conformational Restriction And/Or Steric Hindrance.
Identical And Non Identical Twin Drugs.
Optical Isomerism In Drugs.
Application Strategies For The Primary Structure-Activity Relationship Exploration.
Specific Substituent Groups.
The Role Of Functional Groups In Drug–Receptor Interactions.
Compound Properties And Drug Quality.
Quantitative Approaches To Structure-Activity Relationships.
Structural Aspects Of Drug Action I.
Pharmacophore Identification And Receptor Mapping.
Three-Dimentional Quantitative Structure-Property Relationships.
Protein Crystallography And Drug Discovery.
Protein Comparative Modelling And Drug Discovery.
The Transition From Agonist To Antagonist Activity:
Symmetry And Other Considerations.
Design Of Peptidomimetics.
The Fate Of Xenobiotics In Living Organisms.
Biotransformation Reactions.
Chemical Mechanisms Of Toxicity.
Basic Knowledge For Designing Safer Drugs.
Designing Prodrugs And Bioprecursors.
Macromolecular Carriers For Drug Targeting.
Preparation Of Water Soluble Compounds Through Salt Formation.
Preparation Of Water-Soluble Compounds By Covalent Attachment Of Solubilizing Moieties.
Drug Solubilization With Organic Solvents, Surfactants And Lipids.
Improvement Of Drug Properties By Cyclodextrins.
Chemical And Physicochemical Solutions To Formulation Problems.
Discover A Drug Substance, Formulate And Develop It To A Product.
Drug Nomenclature.
Legal Aspects Of Product Protection.
The Consumption And Production Of Pharmaceuticals.

wild_boy

真是一本好书。楼主辛苦啦。

y8d4p

好东西啊，看看就流口水！哎！

kawapu007

wild_boy

帮顶一下。

liuyihua

帮顶一下。

yundewuyu

不知道怎么样，下来看看先！

鹤影2004

提取码变了?还是删除了?已经无法提取了!

kawapu007

有机会再上传，网盘的内容给pc删了

wild_boy

007,第三版找到啦！！

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[ 本帖最后由 wild_boy 于 2008-12-3 13:31 编辑 ]

wild_boy

The Practice of Medicinal Chemistry, Third Edition
By Camille Georges Wermuth



Publisher:   Academic Press
Number Of Pages:   982
Publication Date:   2008-07-23
ISBN-10 / ASIN:   0123741947
ISBN-13 / EAN:   9780123741943
Binding:   Hardcover



Now in its third edition, this classic reference is the one-stop-shop for information on the foundations of medicinal chemistry for pharmaceutical researchers who are involved in drug development & discovery but who do not have a background in medicinal chemistry. Wermuth aids pharmaceutical researchers and chemists in making faster, more accurate identifications of the active substances that could potentially treat the disorder they are researching. New chapters on Drug Absorption & Transport give pharmaceutical scientists information on how potential drugs can move through the drug discovery/development phases more quickly. This third edition still stands as the only source for practical aspects of medicinal chemistry by focusing on the daily problems met by the medicinal chemist in drug discovery.

NEW TO THIS EDITION:
* Focus on chemoinformatics and drug discovery
* Enhanced pedagogical features
* New chapters including:
- Drug absorption and transport
- Multi-target drugs
* Updates on hot new areas:
NEW! Drug discovery and the latest techniques
NEW! How potential drugs can move through the drug discovery/ development phases more quickly
NEW! Chemoinformatics

[ 本帖最后由 wild_boy 于 2008-12-3 13:26 编辑 ]

wild_boy

Part I: General Aspects of Medicinal Chemistry
  Chapter 1 - A History of Drug DiscoveryFrom first steps of chemistry to achievements in molecular pharmacology, Pages 1-62, François Chast
  Chapter 2 - Medicinal ChemistryDefinitions and Objectives, Drug Activity Phases, Drug Classification Systems, Pages 63-72, Peter Imming
  Chapter 3 - Measurement and Expression of Drug Effects, Pages 73-84, Jean-Pierre Nowicki, Bernard Scatton
  Chapter 4 - Molecular Drug Targets, Pages 85-105, Jean-Pierre Gies, Yves Landry
  Chapter 5 - Drug Targets, Target identification, Validation and Screening, Pages 106-121, Kenton H. Zavitz, Paul L. Bartel, Adrian N. Hobden

Part II: Lead Compound Discovery Strategies
  Chapter 6 - Strategies in the Search for New Lead Compounds or Original Working Hypotheses, Pages 123-143, Camille G. Wermuth
  Chapter 7 - High-Throughput Screening and Drug Discovery, Pages 144-158, John R. Proudfoot
  Chapter 8 - Natural Products as Pharmaceuticals and Sources for Lead Structures, Pages 159-186, David J. Newman, Gordon M. Cragg, David G. I. Kingston
  Chapter 9 - Biology Oriented Synthesis and Diversity Oriented Synthesis in Compound Collection Development, Pages 187-209, Kamal Kumar, Stefan Wetzel, Herbert Waldmann
  Chapter 10 - In Silico ScreeningHit Finding from Database Mining, Pages 210-227, Thierry Langer, Sharon D. Bryant
  Chapter 11 - Fragment-Based Drug Discovery, Pages 228-243, Bennett T. Farmer, Allen B. Reitz
  Chapter 12 - Lead-Likeness and Drug-Likeness, Pages 244-254, Alex Polinsky
  Chapter 13 - Web AlertUsing the Internet for Medicinal Chemistry, Pages 255-272, David Cavalla

Part III: Primary Exploration of Structure–Activity Relationships
  Chapter 14 - Molecular Variations in Homologous SeriesVinylogues and Benzologues, Pages 273-289, Camille G. Wermuth
  Chapter 15 - Molecular Variations Based on Isosteric Replacements, Pages 290-342, Paola Ciapetti, Bruno Giethlen
  Chapter 16 - Ring Transformations, Pages 343-362, Christophe Morice, Camille G. Wermuth
  Chapter 17 - Conformational Restriction and/or Steric Hindrance in Medicinal Chemistry, Pages 363-379, André Mann
  Chapter 18 - Homo and Heterodimer Ligands: the Twin Drug Approach, Pages 380-414, Jean-Marie Contreras, Wolfgang Sippl
  Chapter 19 - Application Strategies for the Primary Structure–Activity Relationship Exploration, Pages 415-427, Camille G. Wermuth

Part IV: Substituents and Functions: Qualitative and Quantitative Aspects of Structure–Activity Relationships
  Chapter 20 - Substituent Groups, Pages 429-463, Patrick Bazzini, Camille G. Wermuth
  Chapter 21 - The Role of Functional Groups in Drug–Receptor Interactions, Pages 464-480, Laurent Schaeffer
  Chapter 22 - Compound Properties and Drug Quality, Pages 481-490, Christopher A. Lipinski
  Chapter 23 - Quantitative Approaches to Structure–Activity Relationships, Pages 491-513, Han van de Waterbeemd, Sally Rose

Part V: Spatial Organization, Receptor Mapping and Molecular Modeling
  Chapter 24 - OverviewThe Search for Biologically Useful Chemical Space, Pages 515-520, David J. Triggle
  Chapter 25 - Pharmacological Space, Pages 521-532, Andrew L. Hopkins
  Chapter 26 - Optical Isomerism in Drugs, Pages 533-548, Camille G. Wermuth
  Chapter 27 - Multi-target DrugsStrategies and Challenges for Medicinal Chemists, Pages 549-571, Richard Morphy, Zoran Rankovic
  Chapter 28 - Pharmacophore Identification and Pseudo-Receptor Modeling, Pages 572-586, Wolfgang Sippl
  Chapter 29 - 3D Quantitative Structure–Property Relationships, Pages 587-604, Thierry Langer, Sharon D. Bryant
  Chapter 30 - Protein Crystallography and Drug Discovery, Pages 605-634, Jean-Michel Rondeau, Herman Schreuder

Part VI: Chemical Modifications Infl uencing the Pharmacokinetic Properties
  Chapter 31 - Physiological Aspects Determining the Pharmacokinetic Properties of Drugs, Pages 635-654, Koen Boussery, Frans M. Belpaire, Johan Van de Voorde
  Chapter 32 - Biotransformation Reactions and Their Enzymes, Pages 655-673, Bernard Testa
  Chapter 33 - Biotransformations Leading to Toxic MetabolitesChemical Aspect, Pages 674-696, Anne-Christine Macherey, Patrick M. Dansette
  Chapter 34 - Drug Transport Mechanisms and their Impact on the Disposition and Effects of Drugs, Pages 697-710, Jean-Michel Scherrmann
  Chapter 35 - Strategies for Enhancing Oral Bioavailability and Brain Penetration, Pages 711-720, Brian C. Shook, Paul F. Jackson
  Chapter 36 - Designing Prodrugs and Bioprecursors, Pages 721-746, Camille G. Wermuth

Part VII: Pharmaceutical and Chemical Means to Solubility and Formulation Problems
  Chapter 37 - Preparation of Water-Soluble Compounds Through Salt Formation, Pages 747-766, Michael J. Bowker, P. Heinrich Stahl
  Chapter 38 - Preparation of Water-Soluble Compounds by Covalent Attachment of Solubilizing Moieties, Pages 767-785, Camille G. Wermuth
  Chapter 39 - Drug Solubilization with Organic Solvents, or Using Micellar Solutions or Other Colloidal Dispersed Systems, Pages 786-812, Michael J. Bowker, P. Heinrich Stahl
  Chapter 40 - Improvement of Drug Properties by Cyclodextrins, Pages 813-840, Kaneto Uekama, Fumitoshi Hirayama
  Chapter 41 - Chemical and Physicochemical Approaches to Solve Formulation Problems, Pages 841-853, Camille G. Wermuth

Part VIII: Development of New Drugs: Legal and Economic Aspects
  Chapter 42 - Discover a Drug Substance, Formulate and Develop It to a Product, Pages 855-866, Bruno Galli, Bernard Faller
  Chapter 43 - Drug Nomenclature, Pages 867-877, R.G. Balocco Mattavelli, J.C. Dong, S. Lasseur, S. Kopp
  Chapter 44 - Legal Aspects of Product ProtectionWhat a Medicinal Chemist Should Know About Patent Protection, Pages 878-893, Maria Souleau
  Chapter 45 - The Consumption and Production of Pharmaceuticals, Pages 894-921, Bryan G. Reuben

wild_boy

再给加上一本好书
Handbook of Assay Development in Drug Discovery

Handbook of Assay Development in Drug Discovery
By Lisa K. Minor



Publisher:   CRC
Number Of Pages:   488
Publication Date:   2006-01-20
ISBN-10 / ASIN:   1574444719
ISBN-13 / EAN:   9781574444711
Binding:   Hardcover


The need to screen targets faster and more efficiently, coupled with advances in parallel and multiplex chemical synthesis, has contributed to the increasing use of multiwell assays for drug discovery. The Handbook of Assay Development in Drug Discovery is a reference that describes the complete armament of tools currently available for performing various assay techniques.

Featuring contributions from assay developers in the pharmaceutical and vendor communities, the book presents descriptions of methods, laboratory guidelines and protocols used to perform such methods, specific examples of each assay system, and troubleshooting tools. The handbook describes biochemical assay classes as well as non-class specific assay development for cell-based assays. It covers a wide range of target classesâ ”including kinases, proteases, nuclear receptors, and GPCRsâ ”and describes currently employed methods and assay types, such as radioligand binding assays, image analysis assays, enzyme fragment complementation, and bioluminescent and fluorescent-based assays.

Designed as a guide to running an assay from start to finish, the Handbook of Assay Development in Drug Discovery is an ideal bench top companion for discovery researchers, laboratory managers, academics, and other scientists involved in drug discovery screening, lead profiling, therapeutic target evaluation, and assay development and implementation in the pharmaceutical and biotechnology industries.



Summary: The Up to Date State of the Art
Rating: 5

This authors of this book represent a who's who of the industry. To be as advanced as possible, Dr. Minor has had individual chapters written by experts from equipment vendors (GE, PerkinElmer); pharmaceutical companies (J&J, Merck, Lilly), government (NIH) and more. These individual chapters describe in practical terms what these organizations have developed.

The book is meant as a general guidebook that one will take to the workbench. It includes descriptions of methods, exact protocols used to perform such methods, and troubleshooting tools. These techniques have been led by the need to screen targets more rapidly and with more efficiency than in previous years and by advances in chemistry allowing parallel or multiplex chemical synthesis to provide more compounds for screening.

The book should be of interest to those in discovery research as well as those in the academic world who wish to know what has become available in recent years.

Links

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