Contents

1.1 Medicinal Chemistry—An Interdisciplinary Science 1

1.2 Drug Discovery—A Historical Perspective 2

1.3 Therapeutic Targets—Identification and Validation 4

1.4 The Drug Development Process—An Outline 5

1.5 Discovery of Drug Candidates 6

1.5.1 Natural Products—Role in Target Identification 6

1.5.2 Natural Products as Lead Structures 7

1.5.3 Basic Principles in Lead Development and Optimization 9

1.5.3.1 Bioisosterism 10

1.5.3.2 Stereochemistry 10

1.5.3.3 Membrane Penetration—Including Lipinski Rule of Five 12

1.5.3.4 Structure-Based Drug Design 12

1.6 Individualized Medicine and Concluding Remarks 13

Further Readings 13

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