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 vitro

D3 Testing drugs in vivo

Section E-Drug discovery

E1 The lead compound

E2 Natural sources of lead compounds

E3 Synthetic sources of lead compounds

F1 Synthetic considerations

Section F-Synthesis

F2 Stereochemistry

F3 Combinatorial synthesis

Section G-Structure-activity relationships

G1 Definition of structure-activity relationships

G2 Binding interactions

G3 Functional groups as binding groups

G4 The pharmacophore

G5 Quantitative structure-activity relationships

H1 Aims of drug design

Section H-Target orientated 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

J1 Patenting and chemical development

Section J-Patenting and manufacture

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 pharmaceutical chemistry

K3 Drug metabolism studies

K4 Clinial 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(1900-1930)

M4 The dawn of the antibacterial age(1930-1945)

M5 The antibiotic age(1945-1970s)

M6 The age of reason(1970s to present)

Further reading

Index