11. Thiazole: A privileged scaffold in drug discovery
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Sunil Kumar
Abstract
Heterocyclic structures have enormous biomedical applications. The heterocyclic core present in various molecules is directly linked to some bioactivity known as pharmacophore whereas a few structural motifs frequently found in various bioactive molecules are termed ‘privileged structures’. It is the minimum structural subunit, common in drugs or lead compounds, which provide ligand points for more than one type of bioreceptor. A focused compound collection based on ‘privileged scaffolds’ may provide high quality leads for further drug development. Several structural motifs are highlighted as privileged scaffolds in literature. Based on our exhaustive literature survey, a heterocyclic ‘1,3-Thiazole’, moiety was observed in several natural products and drugs confirming thiazole as a Privileged Scaffold in drug discovery. This chapter will provide several synthetic approaches toward the construction of this interesting ring system with diverse substitutions. Detailed structures of various thiazole-containing drugs which are currently on the market or in clinical trials are discussed with a special note on their synthesis and mechanism of biological action.
Abstract
Heterocyclic structures have enormous biomedical applications. The heterocyclic core present in various molecules is directly linked to some bioactivity known as pharmacophore whereas a few structural motifs frequently found in various bioactive molecules are termed ‘privileged structures’. It is the minimum structural subunit, common in drugs or lead compounds, which provide ligand points for more than one type of bioreceptor. A focused compound collection based on ‘privileged scaffolds’ may provide high quality leads for further drug development. Several structural motifs are highlighted as privileged scaffolds in literature. Based on our exhaustive literature survey, a heterocyclic ‘1,3-Thiazole’, moiety was observed in several natural products and drugs confirming thiazole as a Privileged Scaffold in drug discovery. This chapter will provide several synthetic approaches toward the construction of this interesting ring system with diverse substitutions. Detailed structures of various thiazole-containing drugs which are currently on the market or in clinical trials are discussed with a special note on their synthesis and mechanism of biological action.
Chapters in this book
- Frontmatter I
- Preface V
- Table of Contents VII
- List of Contributing Authors XI
- 1. Overview of chemical drug design 1
- 2. Drug designing in novel drug discovery: Trends, scope and relevance 15
- 3. Structure- and ligand-based approaches in drug designing 31
- 4. Drug design applied to natural products against neglected diseases 53
- 5. Natural product hybrid compounds as drug leads 87
- 6. Drug metabolism 107
- 7. Mistletoe lectin: A promising cancer therapeutic 165
- 8. Antipsychotics 183
- 9. Chemometric analysis: A novel tool for herbal drug analysis and designing 199
- 10. Copper and its complexes: A pharmaceutical perspective 215
- 11. Thiazole: A privileged scaffold in drug discovery 243
- Index 283
Chapters in this book
- Frontmatter I
- Preface V
- Table of Contents VII
- List of Contributing Authors XI
- 1. Overview of chemical drug design 1
- 2. Drug designing in novel drug discovery: Trends, scope and relevance 15
- 3. Structure- and ligand-based approaches in drug designing 31
- 4. Drug design applied to natural products against neglected diseases 53
- 5. Natural product hybrid compounds as drug leads 87
- 6. Drug metabolism 107
- 7. Mistletoe lectin: A promising cancer therapeutic 165
- 8. Antipsychotics 183
- 9. Chemometric analysis: A novel tool for herbal drug analysis and designing 199
- 10. Copper and its complexes: A pharmaceutical perspective 215
- 11. Thiazole: A privileged scaffold in drug discovery 243
- Index 283
