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An introduction to medicinal chemistry / Graham L. Patrick

Main Author Patrick, Graham L. Country Reino Unido. Edition 3rd ed Publication Oxford : Oxford University Press, 2005 Description XXVI, 741 p. : il. ; 25 cm ISBN 0-19-927500-9
978-0-19-927500-7
CDU 577.1
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Holdings
Item type Current location Call number Status Date due Barcode Item holds Course reserves
Monografia Biblioteca Geral da Universidade do Minho
BGUM 577.1 - P Available 372458

Mestrado em Química Medicinal Química Medicinal I 1º semestre

Mestrado em Química Medicinal Química Medicinal II 2º semestre

Monografia Biblioteca de Química
BQ 577.1 - P Indisponível | Not available 372459
Total holds: 0

Enhanced descriptions from Syndetics:

Many of us think nothing of taking a painkiller to ease a headache, or to relieve the symptoms of 'flu. But how do drugs have their effect in the human body? How are new drugs discovered and designed to be as effective as possible? An Introduction to Medicinal Chemistry offers an engaginginsight into the one field of chemistry that arguably has the greatest impact on our quality of life than any other.Newly structured into four parts, the book opens in Part A with an introduction to pharmacodynamics and pharmacokinetics. Pharmacodynamics considers the types of molecular targets used by drugs, the interactions which are involved when a drug meets that target, and the consequences of thoseinteractions. Pharmacokinetics considers the issues involved in a drug reaching its target in the first place. Part B goes on to examine the general principles and strategies involved in discovering and designing new drugs and developing them for the marketplace, while Part C looks at particular'tools of the trade' which are invaluable in those processes. Finally, Part D covers a selection of specific topics within medicinal chemistry. Reflecting a change in emphasis in medicinal chemistry research, this Part takes us from the largely trial-and-error approach to drug design to the rationalapproach, and explores the most recent advances in molecular biology and genetics which have revolutionised drug design.With a striking new two-colour text design, and greatly enriched learning features, the third edition conveys the fascination of working in a field which overlaps the disciplines of chemistry, biochemistry, physiology, microbiology, cell biology, and pharmacology. A must-have textbook for anystudent of medicinal chemistry.Online Resource Centre- Figures available to download, to facilitate lecture preparation- 3D molecular structures, to enable students to visualise key structures in an interactive way- Multiple choice questions with answers, to support and encourage independent learning

Table of contents provided by Syndetics

  • List of Boxes (p. xxii)
  • Acronyms and Abbreviations (p. xxiii)
  • Classification of Drugs (p. xxv)
  • 1 By pharmacological effect (p. xxv)
  • 2 By chemical structure (p. xxv)
  • 3 By target system (p. xxv)
  • 4 By site of action (p. xxv)
  • Naming of Drugs (p. xxvii)
  • Part A Pharmacodynamics and pharmacokinetics
  • 1 Drugs and the medicinal chemist (p. 3)
  • 2 The why and the wherefore: drug targets (p. 8)
  • 2.1 Why should drugs work? (p. 8)
  • 2.2 Where do drugs work? (p. 8)
  • 2.3 Intermolecular bonding forces (p. 10)
  • 2.4 Drug targets (p. 17)
  • 3 Proteins as drug targets (p. 24)
  • 3.1 Primary structure of proteins (p. 24)
  • 3.2 Secondary structure of proteins (p. 25)
  • 3.3 Tertiary structure of proteins (p. 25)
  • 3.4 Quaternary structure of proteins (p. 32)
  • 3.5 Post-translational modifications (p. 33)
  • 3.6 Proteomics (p. 34)
  • 3.7 Drug action at proteins (p. 34)
  • 3.8 Peptides or proteins as drugs (p. 36)
  • 3.9 Monoclonal antibodies in medicinal chemistry (p. 37)
  • 4 Proteins as drug targets: enzymes (p. 41)
  • 4.1 Enzymes as catalysts (p. 41)
  • 4.2 How do enzymes lower activation energies? (p. 42)
  • 4.3 The active site of an enzyme (p. 42)
  • 4.4 Substrate binding at an active site (p. 43)
  • 4.5 The catalytic role of enzymes (p. 44)
  • 4.6 Regulation of enzymes (p. 48)
  • 4.7 Isozymes (p. 50)
  • 4.8 Enzyme inhibitors (p. 52)
  • 4.9 Enzyme kinetics (p. 61)
  • 5 Proteins as drug targets: receptors (p. 66)
  • 5.1 The receptor role (p. 66)
  • 5.2 Neurotransmitters and hormones (p. 66)
  • 5.3 Receptors (p. 69)
  • 5.4 How is the message received? (p. 69)
  • 5.5 How does a receptor change shape? (p. 72)
  • 5.6 The design of agonists (p. 73)
  • 5.7 Design of antagonists (p. 78)
  • 5.8 Partial agonists (p. 80)
  • 5.9 Inverse agonists (p. 81)
  • 5.10 Desensitization and sensitization (p. 83)
  • 5.11 Tolerance and dependence (p. 83)
  • 5.12 Cytoplasmic receptors (p. 84)
  • 5.13 Receptor types and subtypes (p. 84)
  • 5.14 Affinity, efficacy, and potency (p. 86)
  • 6 Proteins as drug targets: receptor structure and signal transduction (p. 90)
  • 6.1 Receptor families (p. 90)
  • 6.2 Receptors that control ion channels (ligand-gated ion channel receptors) (p. 90)
  • 6.3 Structure of G-protein-coupled receptors (p. 93)
  • 6.4 Signal transduction pathways for G-protein-coupled receptors (p. 97)
  • 6.5 Signal transduction involving G-protein-coupled receptors and cyclic AMP (p. 99)
  • 6.6 Signal transduction involving G-protein-coupled receptors and phospholipase C (p. 104)
  • 6.7 Kinase-linked (1-TM) receptors (p. 108)
  • 6.8 Intracellular receptors (p. 112)
  • 7 Nucleic acids as drug targets (p. 117)
  • 7.1 Structure of DNA (p. 117)
  • 7.2 Ribonucleic acid and protein synthesis (p. 122)
  • 7.3 Drugs and nucleic acids (p. 126)
  • 7.4 Antisense therapy (p. 128)
  • 7.5 Genetic illnesses (p. 128)
  • 7.6 Molecular biology and genetic engineering (p. 129)
  • 8 Pharmacokinetics and related topics (p. 134)
  • 8.1 Pharmacodynamics and pharmacokinetics (p. 134)
  • 8.2 Drug absorption (p. 134)
  • 8.3 Drug distribution (p. 136)
  • 8.4 Drug metabolism (p. 138)
  • 8.5 Drug excretion (p. 149)
  • 8.6 Drug administration (p. 150)
  • 8.7 Drug dosing (p. 153)
  • 8.8 Formulation (p. 156)
  • 8.9 Drug delivery (p. 156)
  • Part B Drug discovery, design, and development
  • 9 Drug discovery: finding a lead (p. 163)
  • 9.1 Choosing a disease (p. 163)
  • 9.2 Choosing a drug target (p. 163)
  • 9.3 Identifying a bioassay (p. 166)
  • 9.4 Finding a lead compound (p. 171)
  • 9.5 Isolation and purification (p. 181)
  • 9.6 Structure determination (p. 182)
  • 9.7 Herbal medicine (p. 183)
  • 10 Drug design: optimizing target interactions (p. 185)
  • 10.1 Structure-activity relationships (p. 185)
  • 10.2 Identification of a pharmacophore (p. 198)
  • 10.3 Drug optimization: strategies in drug design (p. 200)
  • 10.4 A case study: oxamniquine (p. 219)
  • 11 Drug design: optimizing access to the target (p. 226)
  • 11.1 Improving absorption (p. 226)
  • 11.2 Making drugs more resistant to chemical and enzymatic degradation (p. 229)
  • 11.3 Making drugs less resistant to drug metabolism (p. 232)
  • 11.4 Targeting drugs (p. 234)
  • 11.5 Reducing toxicity (p. 235)
  • 11.6 Prodrugs (p. 236)
  • 11.7 Drug alliances (p. 242)
  • 11.8 Endogenous compounds as drugs (p. 243)
  • 12 Drug development (p. 250)
  • 12.1 Preclinical and clinical trials (p. 250)
  • 12.2 Patenting and regulatory affairs (p. 257)
  • 12.3 Chemical and process development (p. 260)
  • Part C Tools of the trade
  • 13 Quantitative structure-activity relationships (QSAR) (p. 271)
  • 13.1 Graphs and equations (p. 271)
  • 13.2 Physicochemical properties (p. 272)
  • 13.3 Hansch equation (p. 281)
  • 13.4 Craig plot (p. 282)
  • 13.5 Topliss scheme (p. 283)
  • 13.6 Bioisosteres (p. 286)
  • 13.7 Free-Wilson approach (p. 287)
  • 13.8 Planning a QSAR study (p. 287)
  • 13.9 Case study (p. 287)
  • 13.10 3D QSAR (p. 291)
  • 14 Combinatorial synthesis (p. 299)
  • 14.1 Combinatorial synthesis in medicinal chemistry (p. 299)
  • 14.2 Solid phase techniques (p. 300)
  • 14.3 Methods of parallel synthesis (p. 305)
  • 14.4 Methods in mixed combinatorial synthesis (p. 306)
  • 14.5 Isolating the active component in a mixture: deconvolution (p. 309)
  • 14.6 Structure determination of the active compound(s) (p. 312)
  • 14.7 Limitations of combinatorial synthesis (p. 314)
  • 14.8 Examples of combinatorial syntheses (p. 316)
  • 14.9 Dynamic combinatorial chemistry (p. 318)
  • 14.10 Planning and designing a combinatorial synthesis (p. 321)
  • 14.11 Testing for activity (p. 322)
  • 15 Computers in medicinal chemistry (p. 326)
  • 15.1 Molecular and quantum mechanics (p. 326)
  • 15.2 Drawing chemical structures (p. 327)
  • 15.3 3D structures (p. 327)
  • 15.4 Energy minimization (p. 328)
  • 15.5 Viewing 3D molecules (p. 329)
  • 15.6 Molecular dimensions (p. 329)
  • 15.7 Molecular properties (p. 330)
  • 15.8 Conformational analysis (p. 335)
  • 15.9 Structure comparisons and overlays (p. 338)
  • 15.10 Identifying the active conformation (p. 340)
  • 15.11 3D pharmacophore identification (p. 342)
  • 15.12 Docking procedures (p. 345)
  • 15.13 Automated screening of databases for lead compounds (p. 349)
  • 15.14 Protein mapping (p. 349)
  • 15.15 De novo design (p. 353)
  • 15.16 Planning combinatorial syntheses (p. 361)
  • 15.17 Database handling (p. 362)
  • 15.18 Case study (p. 363)
  • Part D Selected topics in medicinal chemistry
  • 16 Antibacterial agents (p. 379)
  • 16.1 The history of antibacterial agents (p. 379)
  • 16.2 The bacterial cell (p. 381)
  • 16.3 Mechanisms of antibacterial action (p. 382)
  • 16.4 Antibacterial agents which act against cell metabolism (antimetabolites) (p. 382)
  • 16.5 Antibacterial agents which inhibit cell wall synthesis (p. 388)
  • 16.6 Antibacterial agents which act on the plasma membrane structure (p. 420)
  • 16.7 Antibacterial agents which impair protein synthesis-translation (p. 424)
  • 16.8 Agents which act on nucleic acid transcription and replication (p. 428)
  • 16.9 Miscellaneous agents (p. 433)
  • 16.10 Drug resistance (p. 433)
  • 17 Antiviral agents (p. 440)
  • 17.1 Viruses and viral diseases (p. 440)
  • 17.2 Structure of viruses (p. 441)
  • 17.3 Life cycle of viruses (p. 441)
  • 17.4 Vaccination (p. 442)
  • 17.5 Antiviral drugs: general principles (p. 443)
  • 17.6 Antiviral drugs used against DNA viruses (p. 444)
  • 17.7 Antiviral drugs acting against RNA viruses: HIV (p. 450)
  • 17.8 Antiviral drugs acting against RNA viruses: flu virus (p. 471)
  • 17.9 Antiviral drugs acting against RNA viruses: cold virus (p. 483)
  • 17.10 Broad-spectrum antiviral agents (p. 485)
  • 17.11 Bioterrorism and smallpox (p. 486)
  • 18 Anticancer agents (p. 489)
  • 18.1 Cancer: an introduction (p. 489)
  • 18.2 Drugs acting directly on nucleic acids (p. 500)
  • 18.3 Drugs acting on enzymes: antimetabolites (p. 514)
  • 18.4 Hormone-based therapies (p. 519)
  • 18.5 Drugs acting on structural proteins (p. 523)
  • 18.6 Inhibitors of signalling pathways (p. 528)
  • 18.7 Miscellaneous enzyme inhibitors (p. 540)
  • 18.8 Miscellaneous anticancer agents (p. 544)
  • 18.9 Antibodies, antibody conjugates, and gene therapy (p. 547)
  • 18.10 Photodynamic therapy (p. 553)
  • 19 Cholinergics, anticholinergics, and anticholinesterases (p. 558)
  • 19.1 The peripheral nervous system (p. 558)
  • 19.2 Motor nerves of the peripheral nervous system (p. 559)
  • 19.3 The neurotransmitters (p. 560)
  • 19.4 Actions of the peripheral nervous system (p. 561)
  • 19.5 The cholinergic system (p. 562)
  • 19.6 Agonists at the cholinergic receptor (p. 563)
  • 19.7 Acetylcholine: structure, SAR, and receptor binding (p. 565)
  • 19.8 The instability of acetylcholine (p. 567)
  • 19.9 Design of acetylcholine analogues (p. 568)
  • 19.10 Clinical uses for cholinergic agonists (p. 569)
  • 19.11 Antagonists of the muscarinic cholinergic receptor (p. 570)
  • 19.12 Antagonists of the nicotinic cholinergic receptor (p. 575)
  • 19.13 Other cholinergic antagonists (p. 579)
  • 19.14 Structure of the nicotinic receptor (p. 579)
  • 19.15 Structure of the muscarinic receptor (p. 580)
  • 19.16 Anticholinesterases and acetylcholinesterase (p. 581)
  • 19.17 Anticholinesterase drugs (p. 583)
  • 19.18 Pralidoxime: an organophosphate antidote (p. 588)
  • 19.19 Anticholinesterases as 'smart drugs' (p. 589)
  • 20 The adrenergic nervous system (p. 593)
  • 20.1 The adrenergic system (p. 593)
  • 20.2 Adrenergic receptors (p. 594)
  • 20.3 Endogenous agonists for the adrenergic receptors (p. 595)
  • 20.4 Biosynthesis of catecholamines (p. 595)
  • 20.5 Metabolism of catecholamines (p. 595)
  • 20.6 Neurotransmission (p. 596)
  • 20.7 Drug targets (p. 598)
  • 20.8 The adrenergic binding site (p. 599)
  • 20.9 Structure-activity relationships (p. 599)
  • 20.10 Adrenergic agonists (p. 601)
  • 20.11 Adrenergic receptor antagonists (p. 605)
  • 20.12 Other drugs affecting adrenergic transmission (p. 611)
  • 21 The opium analgesics (p. 616)
  • 21.1 History of opium (p. 616)
  • 21.2 Morphine (p. 618)
  • 21.3 Morphine analogues (p. 622)
  • 21.4 Receptor theory of analgesics (p. 632)
  • 21.5 Agonists and antagonists (p. 634)
  • 21.6 Endogenous opioid peptides (p. 636)
  • 21.7 Receptor mechanisms (p. 637)
  • 21.8 The future (p. 639)
  • 22 Antiulcer agents (p. 642)
  • 22.1 Peptic ulcers (p. 642)
  • 22.2 H[subscript 2] antagonists (p. 644)
  • 22.3 Proton pump inhibitors (p. 664)
  • 22.4 H. pylori and the use of antibacterial agents (p. 671)
  • 22.5 Traditional and herbal medicines (p. 672)
  • Appendix 1 Essential amino acids (p. 675)
  • Appendix 2 The standard genetic code (p. 676)
  • Appendix 3 Statistical data for QSAR (p. 677)
  • Appendix 4 The action of nerves (p. 680)
  • Appendix 5 Microorganisms (p. 685)
  • Bacterial nomenclature (p. 685)
  • Some clinically important bacteria (p. 685)
  • The Gram stain (p. 685)
  • Classifications (p. 685)
  • Definitions of different microorganisms (p. 686)
  • Appendix 6 Drugs and their trade names (p. 687)
  • Glossary (p. 695)
  • General Further Reading (p. 711)
  • Index (p. 713)

Author notes provided by Syndetics

Dr Graham L Patrick, Lecturer in Chemistry, Department of Chemistry, University of Paisley, UK.

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