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Full Description
Agricultural fungicides and pharmaceutical antifungals unified in one reference
Industry consolidation through mergers and corporate divestitures has complicated the information flow between agrochemical fungicide and pharmaceutical antifungal research, limiting cross-disciplinary innovation. Fungicides and Antifungals: Antimycotics in Agriculture and Medicine reconnects these two domains by presenting the most important antimycotic compound classes from both crop protection and medicine in a single, structured volume designed to accelerate the discovery of novel agents.
Each chapter follows a consistent format covering all important products and their discovery, mode of action, spectrum of activity, resistance issues, synthesis, structure-activity relationships, and analogs. The book treats four principal antifungal classes — azoles, echinocandins, polyenes, and allylamines — alongside three major fungicidal classes: DMIs, strobilurins, and SDHIs.
Readers will also find:
An introductory chapter comparing key characteristics that distinguish antifungal drug development from agrochemical fungicide research
Historical context tracing the parallel evolution of agricultural fungicides and pharmaceutical antifungals from early discoveries to current commercial products
Comparative analysis of discovery strategies used across agrochemical and pharmaceutical research to identify effective antimycotic compounds
Presentation of the four most important oomycetes-selective fungicide classes
A dedicated chapter on very recent fungicides and antifungals with a novel mode of action
Organic chemists, agricultural scientists, biochemists, and life scientists working in academia or at agrochemical and pharmaceutical companies will find this volume directly applicable to their antimycotic research. It is also a targeted resource for university institute libraries and governmental authorities involved in crop protection or public health.
Contents
About the Author xiii
Preface xv
1 Significance of Fungicides and Antifungals for Agriculture and Medicine 1
1.1 Terminology 1
1.2 History 2
1.3 Demand 4
1.4 Cross-Industry 7
1.5 Innovation 10
2 Allylamine Antifungals: History, Activity, Synthesis, Resistance, MoA, and SAR 25
2.1 Products 25
2.2 History 26
2.3 Mode of Action 26
2.4 Biological Activity and Spectrum 28
2.5 Resistance 31
2.6 Synthesis 31
2.7 Structure-Activity Relationships and Analogs 34
3 Polyene Antifungals: History, Activity, Synthesis, Resistance, MoA, and SAR 43
3.1 Products 43
3.2 History 44
3.3 Mode of Action 45
3.4 Biological Activity and Spectrum 48
3.5 Resistance 51
3.6 Synthesis 52
3.7 Structure-Activity Relationships and Analogs 55
4 Echinocandin Antifungals: History, Activity, Synthesis, Resistance, MoA, and SAR 69
4.1 Products 69
4.2 History 71
4.3 Mode of Action 71
4.4 Biological Activity and Spectrum 74
4.5 Resistance 77
4.6 Synthesis 78
4.7 Structure-Activity Relationships and Analogs 82
5 Azole Antifungals and DMI Fungicides: History, Activity, Synthesis, Resistance, MoA, and SAR 95
5.1 Products 95
5.2 History 99
5.3 Mode of Action 102
5.4 Biological Activity and Spectrum 104
5.5 Resistance 109
5.6 Synthesis 111
5.7 Structure-Activity Relationships and Analogs 114
6 Strobilurin Fungicides: History, Activity, Synthesis, Resistance, MoA, and SAR 135
6.1 Products 135
6.2 History 136
6.3 Mode of Action 140
6.4 Biological Activity and Spectrum 142
6.5 Resistance 144
6.6 Synthesis 146
6.7 Structure-Activity Relationships and Analogs 150
7 Succinate Dehydrogenase Inhibiting (SDHI) Fungicides: History, Activity, Synthesis, Resistance, MoA, and SAR 165
7.1 Products 165
7.2 History 168
7.3 Mode of Action 170
7.4 Biological Activity and Spectrum 172
7.5 Resistance 174
7.6 Synthesis 175
7.7 Structure-Activity Relationships and Analogs 181
8 Oomycetes-selective Fungicides: History, Activity, Synthesis, Resistance, MoA, and SAR 193
8.1 Introduction 193
8.2 Phenylamides 194
8.3 Oomycetes-selective Complex III Inhibitors 198
8.4 Carboxylic Acid Amide Fungicides 203
8.5 Oxysterol-binding Protein Inhibitors 209
9 Fungicides and Antifungals with a Novel Mode of Action: Inhibitors of Dihydroorotate Dehydrogenase, Glycosylphosphatidylinositol-anchored Proteins, Aminoacyl-tRNA Synthetases, and Histone Deacetylase 225
9.1 Introduction 225
9.2 Inhibitors of Dihydroorotate Dehydrogenase 226
9.3 Inhibitors of Glycosylphosphatidylinositol-anchored Proteins 230
9.4 Inhibitors of Aminoacyl-tRNA Synthetases 234
9.5 Inhibitors of Histone Deacetylase 237
Index 249
