Validamycin and Its Derivatives

Validamycin and Its Derivatives: Discovery, Chemical Synthesis and Biological Activity presents, for the first time, a complete review of the underlying chemistry, synthesis, behavior and application of these compounds.

Beginning with an introduction to validamycin, the book then outlines the key elements of its discovery and production, including details of its structures, isolation, analysis, and issues relating to its large scale production.

Biological activities are then explored in more detail, followed by details of biosynthesis. Further to this, the chemical synthesis of validamycin and its intermediates, including valienamine, validamine, valiolamine, and validoxylamines is reviewed, before preparation of these derivatives and their biological activities are explored.

Finally, the book concludes with a discussion of the economic aspects of working with validamycin and its potential in future applications and trends. With its detailed chemical coverage from a team of expert authors, this detailed guide can be applied to the large-scale industrial production of antibiotics and the adaptation of bioactive agents, from agricultural, to novel pharmaceutical applications.

• Offers complete coverage of validamycin chemistry from a highly experienced team of authors
• Encourages the discovery of further novel drugs based on validamycin derivatives
• Presents an interesting model for establishing new pharmaceutical leads from agricultural sources
• Includes coverage of the total chemical synthesis of validamycin and its intermediates, including valienamine, validamine, valiolamine and validoxylamines

Medicinal chemists and pharmaceutical scientists, particularly those working on the development of novel antibiotics and antidiabetic drugs; biomedical scientists; agricultural chemists; academic researchers and postgraduates studying medicinal chemistry

Chapter 1. An Introduction to Validamycins and Their Derivatives

• Abstract
• 1.1 Importance of Antibiotics
• 1.2 Agricultural Antibiotics for Plant Pathogens
• 1.3 Validamycins: Magic Agricultural Antibiotics
• 1.4 Aims of the Work
• References

Chapter 2. Production of Validamycins

• Abstract
• 2.1 Discovery of Validamycins
• 2.2 Microbes for Producing Validamycins
• 2.3 Production and Isolation of Validamycins and Related Natural Compounds
• 2.4 Structures, Characterization, and Properties of Validamycins and Related Natural Compounds
• 2.5 Biosynthesis of Validamycins
• 2.6 Detection of Validamycin A
• 2.7 Microbial Degradation of Validamycin A
• 2.8 Cloning, Expression, and Deficiency of Genes in the Validamycin Biosynthesis and Their Applications
• 2.9 Fermentation Process for Production of Validamycins
• References

Chapter 3. Bioactivities of Validamycins and Related Natural Compounds

• Abstract
• 3.1 Antifungal Activities
• 3.2 Enzyme Inhibitory Activities
• 3.3 Insecticidal Activity of Validoxylamine A and Related Compounds
• References

Chapter 4. Chemical Synthesis of Validamycin and Related Natural Compounds

• Abstract
• 4.1 Synthesis of Valienamine
• 4.2 Synthesis of epi-Valienamine
• 4.3 Synthesis of Valiolamine
• 4.4 Synthesis of Validamine
• 4.5 Synthesis of Hydroxyvalidamine
• 4.6 Synthesis of Validoxylamines
• 4.7 Synthesis of Validamycins
• References

Chapter 5. Voglibose: An Important Drug for Type 2 Diabetes

• Abstract
• 5.1 Chemical Structures of Various Pseudoaminosugar Glucosidase Inhibitors
• 5.2 α-D-Glucosidase Inhibitory Activity N-Substituted Valiolamine Derivatives and Related Compounds
• 5.3 Physicochemical Properties of Voglibose and Drug Summary
• 5.4 Preparation of Voglibose
• 5.5 Pharmacology, Pharmacokinetics, and Pharmacodynamics
• 5.6 Clinical Efficacy
• 5.7 Safety and Tolerability
• 5.8 Comparison With Other Drugs of Acarbose and Miglitol
• 5.9 Market and Development
• References

Chapter 6. N-Octyl-β-Valienamine and N-Octyl-4-epi-β-Valienamine: Two Highly Potent Drug Candidates for Chemical Chaperone Therapy

• Abstract
• 6.1 Chaperone Therapy
• 6.2 N-Octyl-β-valienamine for Chaperone Therapy of Gaucher Disease
• 6.3 N-Octyl-4-epi-β-valienamine for Chaperone Therapy of GM1-Gangliosidosis
• 6.4 Future Perspectives and Conclusion
• References

Chapter 7. Prospects and Concluding Remarks

• Abstract