Medicinal Chemistry

Principles and Practice

By: Frank D King (Editor)

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Paperback | 30 September 2002 | Edition Number 2

At a Glance

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472 Pages

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New edition

Dimensions(cm)
15.9 x 23.4 x 3.0

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This book covers the key topics for drug discovery from the perspective of the practising industrial scientist and manager. Presenting all aspects of the subject from initial lead through to final development, this new edition builds on the highly successful foundations laid by the first edition by introducing new topics such as combinatorial chemistry, genomics and chemoinformatics, alongside revised and updated original chapters. Introducing the cross-disciplinary topics needed, Medicinal Chemistry: Principles and Practice 2nd Edition embraces descriptions of targets, biology, metabolism and pharmacokinetics, genetics, patents and development chemistry. New case histories, strategy and tactics for drug discovery are also introduced. With many chapters written by practitioners from within the pharmaceutical industry, it is an invaluable introduction to medicinal chemistry for new graduates and PhDs. It will also serve to update more experienced scientists on the newer technologies in the field.

Industry Reviews

"Overall an excellent book for those making a move into pharmaceutical/medicinal chemistry research and for those who wish to broaden their knowledge of all the disciplines involved in this area".

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Non-Fiction Medicine Nursing & Ancillary Services Pharmacy & Dispensing Science Chemistry Engineering & Technology Industrial Chemistry & Manufacturing Technologies Industrial Chemistry Pharmaceutical Technology Biology, Life Sciences Biochemistry

Industry & Industrial Studies Manufacturing Industries Pharmaceutical Industries Other Branches of Medicine Pharmacology

Contributors	p. xxi
Abbreviations	p. xxiii
General References	p. xxvii
Drug-Receptor Interactions	p. 1
Introduction	p. 1
Receptor Proteins	p. 2
Mechanism of Drug Action: Agonism and Antagonism	p. 5
Receptor Subtypes	p. 6
Drug Selectivity	p. 9
Quantification of Drug-Receptor Interactions	p. 10
From Antagonists to Inverse Agonists	p. 21
Final Considerations	p. 23
Selected Reading	p. 23
An Introduction to Ion Channels	p. 25
Introduction	p. 25
Structure, Function and Classification	p. 26
Representative Examples	p. 29
Conclusion	p. 40
References	p. 40
Intracellular Targets	p. 42
Introduction	p. 42
Antibacterial Inhibitors of Protein Synthesis	p. 42
Bacterial Topoisomerase Inhibitors: Fluoroquinolones	p. 47
Nuclear Receptors	p. 52
Protein Kinases	p. 57
References	p. 62
Enzyme Inhibitors	p. 64
Introduction	p. 64
Enzyme Inhibitor Categories	p. 67
Opportunities in Drug Design	p. 79
Classes of Enzymes and Examples of Enzyme Inhibitors	p. 82
Concluding Remarks	p. 89
References	p. 90
Biological Evaluation of Novel Compounds	p. 91
Introduction	p. 91
Primary Screens	p. 93
Secondary Assays	p. 101
Drug Metabolism and Pharmacokinetics (DMPK)	p. 111
Pharmacodynamic Assays	p. 111
Animal Models--Pre-clinical Proof of Concept	p. 113
Acknowledgements	p. 116
References	p. 116
Pharmacokinetics	p. 118
Introduction	p. 118
The Process and Terminology of Drug Delivery	p. 119
The Blood (or Plasma) Concentration-Time Curve	p. 120
Bioavailability	p. 124
Clearance	p. 125
Volume of Distribution	p. 129
Half-life	p. 133
'Advanced'. Pharmacokientics	p. 136
Conclusions	p. 137
References	p. 137
Bibliography	p. 137
Drug Metabolism	p. 138
Introduction	p. 138
Distribution of Drug Metabolism Enzymes	p. 138
The Drug Metabolising Enzymes	p. 139
Conclusions	p. 153
References and Bibliography	p. 153
Toxicology in the Drug Discovery Process	p. 155
Introduction	p. 155
Overview of Toxicity Assessment in Drug Discovery	p. 157
In Silico Systems for Assessing Toxicity	p. 159
Introduction to In Vitro Systems	p. 161
In Vivo Toxicology in Candidate Selection	p. 173
The Use of New Technologies in Safety Assessment	p. 176
Summary	p. 179
References	p. 179
Chemical Development	p. 182
Introduction	p. 182
Illustrative Examples	p. 190
Future Trends	p. 192
Acknowledgement	p. 193
References	p. 193
Physicochemical Properties	p. 195
Introduction	p. 195
Solubility	p. 196
Lipophilicity	p. 200
Hydrogen Bonding	p. 203
Molecular Size	p. 204
Ionisation Constants	p. 205
Electronic Properties	p. 207
Estimation of Other Molecular Properties	p. 208
Relationships to Drug Disposition	p. 210
References	p. 213
Quantitative Structure-Activity Relationships	p. 215
Introduction	p. 215
Background to QSAR	p. 217
Compound Selection	p. 220
Describing Chemical Structure	p. 223
Building QSAR Models	p. 225
Artificial Intelligence	p. 238
Summary	p. 240
References	p. 241
Computational Chemistry and Target Structure	p. 243
Introduction - The Basic Toolkit	p. 243
Structural Information for Computational Chemistry	p. 246
The Use of Structure in Drug Design	p. 248
Related (Homologous) Structures	p. 250
The Absence of Target Structural Information	p. 253
When the Target Structure Is Almost Irrelevant	p. 254
Conclusion	p. 257
References	p. 257
Patent Medicine	p. 260
Introduction	p. 260
What Are Patents?	p. 262
What Is Patentable?	p. 265
'Patentese'	p. 269
Applying for Patents	p. 271
Prosecution and Litigation	p. 276
Trips and US Practice	p. 278
The Biotech Revolution	p. 280
Advance Module	p. 283
Sites for Sore Eyes	p. 285
Conclusion	p. 286
References and Notes	p. 287
An Introduction to Molecular Biology	p. 291
Introduction	p. 291
Nucleic Acids	p. 291
Proteins	p. 293
The Flow of Genetic Information	p. 294
DNA Replication	p. 294
Transcription	p. 296
RNA Processing	p. 297
Protein Synthesis	p. 297
The Genetic Code	p. 300
Post Translational Modification	p. 302
The Control of Transcription and Translation	p. 302
Genomics	p. 302
Nucleic Acid Analysis and Recombinant DNA Technology	p. 304
Bioinformatics and the Internet	p. 322
Human Genome Mapping Project	p. 324
References	p. 325
Strategy and Tactics in Drug Discovery	p. 327
Introduction	p. 327
Target Identification and Validation	p. 328
Lead Identification	p. 330
Lead Optimisation	p. 332
Development Candidate	p. 334
Back-up/Follow-up	p. 335
Optimising the Chances for Success	p. 335
Decision Making in Medicinal Chemistry	p. 338
Patents	p. 357
Conclusion	p. 358
References	p. 358
Combinatorial Chemistry: Tools for the Medicinal Chemist	p. 359
Introduction	p. 359
Concepts in Combinatorial Chemistry	p. 360
Impact of CC on the Drug Discovery Process	p. 363
Solid-phase Synthesis ed. 'Drug-like' Molecules	p. 364
Solution-phase Library Synthesis	p. 368
Solid Phase Versus Solution Phase	p. 372
Laboratory Automation and Equipment	p. 373
Biological Activity from Compound Libraries	p. 377
Conclusions	p. 379
References	p. 381
The Identification of Selective 5-HT[subscript 2C] Receptor Antagonists: A New Approach to the Treatment of Depression and Anxiety	p. 382
Introduction to Depression	p. 382
Rationale for 5-HT[subscript 2C] Antagonists in Depression	p. 383
Initial Lead: Identification of SB-200646	p. 383
Conformational Restriction: Identification of SB-206553	p. 384
Molecular and Receptor Modelling Studies	p. 385
Bioisosteric Replacement of the N-Methylindole	p. 387
Identification of Biarylcarbamoylindolines	p. 391
Bispyridyl Ethers: Identification of SB-243213	p. 393
Synthesis of SB-243213	p. 394
Summary	p. 395
References	p. 395
The Identification of the HIV Protease Inhibitor Saquinavir	p. 397
Introduction	p. 397
Primary Assay	p. 399
Inhibitor Design	p. 399
Synthesis of Saquinavir	p. 405
Clinical Data	p. 405
Conclusion	p. 406
References	p. 406
Discovery of Vioxx (Rofecoxib)	p. 407
Introduction	p. 407
Lead Molecules	p. 409
Identification of Rofecoxib (MK-966)	p. 410
In Vivo Activity of Rofecoxib	p. 412
Clinical Results	p. 413
Conclusion	p. 414
References	p. 414
NK1 Receptor Antagonists	p. 415
Introduction	p. 415
Medicinal Chemistry Programme	p. 416
Profile of MK-869 Clinical Candidate	p. 423
Clinical Results	p. 424
References	p. 427
Appendices
Ranking of Key Ethical Drug Products in 2000 (US$ Sales Value)	p. 428
Summary of Receptor Properties	p. 430
Plot of Molar Concentration vs. g ml[superscript -1] for Different Molecular Weights	p. 440
Table of Molar Concentration vs. g ml[superscript -1] for Different Molecular Weights	p. 441
Conversion Table for IC[subscript 50] (K[subscript i]) to pIC[subscript 50] (pK[subscript i])	p. 441
Subject Index	p. 442
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Medicinal Chemistry

Principles and Practice

At a Glance

Paperback

Industry Reviews

Shipping

How to return your order

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