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(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
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