Chapter 1:Introduction
What are drugs and why do we need new ones?
Drug discovery and design, a historical outline
Methods and routes of administration, the pharmaceutical phase
Introduction to drug action
Classification of drugs
Drug Stability
Sources of Drugs
Drug development and production
Summary
Chapter 2: Drug Discovery By Design
Introduction
Stereochemistry and drug design
Structure-activity relationships (SAR)
Quantitative structure-activity relationships (QSAR)
Computer-aided drug design
Combinatorial chemistry
Summary
Chapter 3: Drug solubility
Introduction
The structure of bulk liquids
Solutions
Solubility
Solubility and the structure of the solute
Salt formation
The incorporation of water-solubilising groups in a structure
Formulation methods of improving water solubility
The effect of the pH on the solubility of acidic and basic drugs
Partition
Surfactants, structure and action
Summary
Chapter 4: Biological membranes
Introduction
The plasma membrane
The transfer of species through cell membranes
Drug action that affects the structure of cell membranes and walls
Summary
Chapter 5: Pharmacokinetics
Introduction
Drugs
Pharmacokinetic models
Intravascular administration
Extravascular administration
The use of pharmacokinetics in drug design
Extraploation of animal experiments to humans
Summary
Chapter 6 - Enzymes
Introduction
Classification and nomenclature
Active sites and catalytic action
Regulation of enzyme activity
The specific nature of enzyme action
The mechanisms of enzyme action
The generalphysical factors affecting enzyme action
Enzyme kinetics
Enzyme inhibitors
Transition state inhibitors
Enzymes and drug design: some general considerations
Examples of drugs used as enzyme inhibitors
Ribozymes
Summary
Chapter 7: Complexes and chelating agents
Introduction
The shapes and structures of complexes
Stability
The general roles of metal complexes in biological processes
Therapeutic uses
Drug action and metal chelation
Summary
Chapter 8: Receptors and messengers
Introduction
The bonding of ligands to receptors
Structure and classification of receptors
General mode of operation
Ligand-response relationships
Drug action and design
Summary
Chapter 9: Drug Metabolism
Introduction
Secondary pharmacological implications of metabolism
Sites of action
Phase I metabolic reactions
Phase II metabolic routes
Pharmacokinetics of metabolites
Drug metabolism and drug design
Prodrugs
Summary
Chapter 10: Nucleic acids
Introduction
Deoxyribonucleic acids (DNA)
The general functions of DNA
Genes
Replication
Ribonucleic acids (RNA)
Messenger RNA (mRNA)
Transfer RNA (tRNA)
Ribosomal RNA (rRNA)
Protein synthesis
Protein synthesis in prokaryotic and eukaryotic cells
Bacterial protein synthesis inhibitors (antimicrobials)
Drugs that target nucleic acids
Viruses
Recombinant DNA (genetic engineering)
Summary
Chaper 11: Nitric oxide
Introduction
The structure of nitric oxide
The chemical properties of nitric oxide
The cellular production and role of nitric oxide
The role of nitric oxide in physiological and pathophysiological states
Therapeutic possibilities
Summary
Chapter 12: An introduction to organic drug and analogue synthesis
Some general considerations
Asymmetry in syntheses
Designing organic sysntheses
Partial organic synthesisn of xenobiotics
Summary