Abbreviations
Preface
About the author
Section A-The science of medicinal chemistry
A1 Introduction
A2 From concept to market
Section B-Drug targets
B1 Enzymes
B2 Receptors
B3 Carrier proteins
B4 Structural proteins
B5 Nucleic acids
B6 Lipids
B7 Carbohydrates
Section C-Pharmacokinetics
C1 Pharmacokinetics
C2 Drug absorption
C3 Drug distribution
C4 Drug metabolism
C5 Drug excretion
C6 Drug administration
C7 Drug dosing
Section D-Biological testing and bioassays
D1 Testing drugs
D2 Testing drugs in uitro
D3 Testing drugs in uiuo
Section E-Drug discovery
E1 The lead compound
E2 Natural sources of lead compounds
E3 Synthetic sources of lead compounds
Section F-Synthesis
F1 Synthetic considerations
F2 Stereochemistry
F3 Combinatorial synthesis
Section G-Structure-activity relationships
G1 Definition of structure-activity relationshiips
G2 Binding interactions
G3 Functional groups as binding groups
G4 The pharmacophore
G5 Quantitative structure-activity relationships
Section H-Target orientated drug design
H1 Aims of drug design
H2 Computer aided drug design
H3 Simplification of complex molecules
H4 Conformational restraint
H5 Extra binding interactions
H6 Enhancing existing binding interactions
Section I-Pharmacokinetic orientated drug design
I1 Drug solubility
I2 Drug stability
Section J-Patenting and manufacture
J1 Patenting and chemical development
J2 Optimization of reactions
J3 Scale-up issues
J4 Process development
J5 Specifications
Section K-Preclinical testing and clinical trials
K1 Toxicology
K2 Pharmacology and pharamceutical chemistry
K3 Drug metabolism studies
K4 Clinical trials
K5 Regulatory affairs
Section L-Case study:inhibitors of EGF-receptor kinase
L1 Epidermal growth factor receptor
L2 Testing procedures
L3 From lead compound to dianilino-phthalimides
L4 Modeling studies
L5 4-(Phenylamino)pyrrolopyrimidines
L6 Pyrazolopyrimidines
Section M-History of medicinal chemistry
M1 The age of herbs,potions and magic
M2 The nineteenth century
M3 A fledgling science(19-193)
M4 The dawn of the antibacterial age(193-1945)
M5 The antibiotic age(1945-197s)
M6 The age of reason (197s to present)
Further reading
Index