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Introduction to Medicinal Chemistry

ISBN-10: 0199275009

ISBN-13: 9780199275007

Edition: 3rd 2005 (Revised)

Authors: Graham L. Patrick

List price: $65.00
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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 engaging insight 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 those interactions. 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 anddesigning 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 rational approach, 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 any student 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
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Book details

List price: $65.00
Edition: 3rd
Copyright year: 2005
Publisher: Oxford University Press, Incorporated
Publication date: 6/23/2005
Binding: Paperback
Pages: 776
Size: 7.50" wide x 9.75" long x 1.75" tall
Weight: 3.256
Language: English

List of Boxes
Acronyms and Abbreviations
Classification of Drugs
By pharmacological effect
By chemical structure
By target system
By site of action
Naming of Drugs
Pharmacodynamics and pharmacokinetics
Drugs and the medicinal chemist
The why and the wherefore: drug targets
Why should drugs work?
Where do drugs work?
Intermolecular bonding forces
Drug targets
Proteins as drug targets
Primary structure of proteins
Secondary structure of proteins
Tertiary structure of proteins
Quaternary structure of proteins
Post-translational modifications
Drug action at proteins
Peptides or proteins as drugs
Monoclonal antibodies in medicinal chemistry
Proteins as drug targets: enzymes
Enzymes as catalysts
How do enzymes lower activation energies?
The active site of an enzyme
Substrate binding at an active site
The catalytic role of enzymes
Regulation of enzymes
Enzyme inhibitors
Enzyme kinetics
Proteins as drug targets: receptors
The receptor role
Neurotransmitters and hormones
How is the message received?
How does a receptor change shape?
The design of agonists
Design of antagonists
Partial agonists
Inverse agonists
Desensitization and sensitization
Tolerance and dependence
Cytoplasmic receptors
Receptor types and subtypes
Affinity, efficacy, and potency
Proteins as drug targets: receptor structure and signal transduction
Receptor families
Receptors that control ion channels (ligand-gated ion channel receptors)
Structure of G-protein-coupled receptors
Signal transduction pathways for G-protein-coupled receptors
Signal transduction involving G-protein-coupled receptors and cyclic AMP
Signal transduction involving G-protein-coupled receptors and phospholipase C
Kinase-linked (1-TM) receptors
Intracellular receptors
Nucleic acids as drug targets
Structure of DNA
Ribonucleic acid and protein synthesis
Drugs and nucleic acids
Antisense therapy
Genetic illnesses
Molecular biology and genetic engineering
Pharmacokinetics and related topics
Pharmacodynamics and pharmacokinetics
Drug absorption
Drug distribution
Drug metabolism
Drug excretion
Drug administration
Drug dosing
Drug delivery
Drug discovery, design, and development
Drug discovery: finding a lead
Choosing a disease
Choosing a drug target
Identifying a bioassay
Finding a lead compound
Isolation and purification
Structure determination
Herbal medicine
Drug design: optimizing target interactions
Structure-activity relationships
Identification of a pharmacophore
Drug optimization: strategies in drug design
A case study: oxamniquine
Drug design: optimizing access to the target
Improving absorption
Making drugs more resistant to chemical and enzymatic degradation
Making drugs less resistant to drug metabolism
Targeting drugs
Reducing toxicity
Drug alliances
Endogenous compounds as drugs
Drug development
Preclinical and clinical trials
Patenting and regulatory affairs
Chemical and process development
Tools of the trade
Quantitative structure-activity relationships (QSAR)
Graphs and equations
Physicochemical properties
Hansch equation
Craig plot
Topliss scheme
Free-Wilson approach
Planning a QSAR study
Case study
Combinatorial synthesis
Combinatorial synthesis in medicinal chemistry
Solid phase techniques
Methods of parallel synthesis
Methods in mixed combinatorial synthesis
Isolating the active component in a mixture: deconvolution
Structure determination of the active compound(s)
Limitations of combinatorial synthesis
Examples of combinatorial syntheses
Dynamic combinatorial chemistry
Planning and designing a combinatorial synthesis
Testing for activity
Computers in medicinal chemistry
Molecular and quantum mechanics
Drawing chemical structures
3D structures
Energy minimization
Viewing 3D molecules
Molecular dimensions
Molecular properties
Conformational analysis
Structure comparisons and overlays
Identifying the active conformation
3D pharmacophore identification
Docking procedures
Automated screening of databases for lead compounds
Protein mapping
De novo design
Planning combinatorial syntheses
Database handling
Case study
Selected topics in medicinal chemistry
Antibacterial agents
The history of antibacterial agents
The bacterial cell
Mechanisms of antibacterial action
Antibacterial agents which act against cell metabolism (antimetabolites)
Antibacterial agents which inhibit cell wall synthesis
Antibacterial agents which act on the plasma membrane structure
Antibacterial agents which impair protein synthesis-translation
Agents which act on nucleic acid transcription and replication
Miscellaneous agents
Drug resistance
Antiviral agents
Viruses and viral diseases
Structure of viruses
Life cycle of viruses
Antiviral drugs: general principles
Antiviral drugs used against DNA viruses
Antiviral drugs acting against RNA viruses: HIV
Antiviral drugs acting against RNA viruses: flu virus
Antiviral drugs acting against RNA viruses: cold virus
Broad-spectrum antiviral agents
Bioterrorism and smallpox
Anticancer agents
Cancer: an introduction
Drugs acting directly on nucleic acids
Drugs acting on enzymes: antimetabolites
Hormone-based therapies
Drugs acting on structural proteins
Inhibitors of signalling pathways
Miscellaneous enzyme inhibitors
Miscellaneous anticancer agents
Antibodies, antibody conjugates, and gene therapy
Photodynamic therapy
Cholinergics, anticholinergics, and anticholinesterases
The peripheral nervous system
Motor nerves of the peripheral nervous system
The neurotransmitters
Actions of the peripheral nervous system
The cholinergic system
Agonists at the cholinergic receptor
Acetylcholine: structure, SAR, and receptor binding
The instability of acetylcholine
Design of acetylcholine analogues
Clinical uses for cholinergic agonists
Antagonists of the muscarinic cholinergic receptor
Antagonists of the nicotinic cholinergic receptor
Other cholinergic antagonists
Structure of the nicotinic receptor
Structure of the muscarinic receptor
Anticholinesterases and acetylcholinesterase
Anticholinesterase drugs
Pralidoxime: an organophosphate antidote
Anticholinesterases as 'smart drugs'
The adrenergic nervous system
The adrenergic system
Adrenergic receptors
Endogenous agonists for the adrenergic receptors
Biosynthesis of catecholamines
Metabolism of catecholamines
Drug targets
The adrenergic binding site
Structure-activity relationships
Adrenergic agonists
Adrenergic receptor antagonists
Other drugs affecting adrenergic transmission
The opium analgesics
History of opium
Morphine analogues
Receptor theory of analgesics
Agonists and antagonists
Endogenous opioid peptides
Receptor mechanisms
The future
Antiulcer agents
Peptic ulcers
H[subscript 2] antagonists
Proton pump inhibitors
H. pylori and the use of antibacterial agents
Traditional and herbal medicines
Essential amino acids
The standard genetic code
Statistical data for QSAR
The action of nerves
Bacterial nomenclature
Some clinically important bacteria
The Gram stain
Definitions of different microorganisms
Drugs and their trade names
General Further Reading