N-Heterocycles: Synthesis and Biological Evaluation

Description

This book presents an overview of recent advancements for the synthesis of smalland medium-sized nitrogen-containing heterocycles, including pyrroles, indoles, pyrimidines, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with pharmaceutical uses. The book also discusses various properties and performance attributes of azaheterocycles including their bioactivity and synthetic strategies. The book can be a valuable reference for beginners, researchers, and professionals interested in organic synthesis and medicinal chemistry Cover Half Title N-Heterocycles: Synthesis and Biological Evaluation Copyright Preface Contents Editors and Contributors 1. Pyridines, Dihydropyridines and Piperidines: An Outline on Synthesis and Biological Activities 1.1 Pyridine 1.1.1 Introduction 1.1.2 Historical Background of Pyridine 1.1.3 General Approaches to Pyridine Rings 1.1.4 Biological Activity 1.1.5 Conclusion 1.2 Dihydropyridines 1.2.1 Introduction 1.2.2 Historical Background of Dihydropyridine 1.2.3 General Approaches to Achieve DHP Rings 1.2.4 Biological Activity 1.2.5 Conclusion 1.3 Piperidines 1.3.1 Introduction 1.3.2 Historical Background of Piperidine 1.3.3 General Approaches to Piperidine Rings 1.3.4 Biological Activity 1.3.5 Conclusion References 2. Imidazole, Hydantoins, Thiazole, and Oxazole: A Journey on Synthetic and Biological Relevance 2.1 Imidazole or 1,3-Diazole 2.1.1 Introduction 2.1.2 Synthesis of Imidazole 2.1.3 Synthesis of Novel Imidazole Derivatives of 4-Aminoquinoline Using Van Leusen Multicomponent Synthetic Protocol 2.1.4 Pharmacological Activities 2.2 Hydantoins or Imidazolidine-2,4-Diones 2.2.1 Introduction 2.2.2 Hydantoins Syntheses 2.2.3 Natural Products Containing a Hydantoin Moiety 2.2.4 Pharmacological Drugs Containing a Hydantoin Moiety 2.3 Thiazole or 1,3-Thiazole 2.3.1 Introduction 2.3.2 Thiazole Synthesis 2.3.3 Functionalizing Positions 2.3.4 Pharmacological Drugs Containing Thiazole Moiety 2.3.5 Natural Compound Containing Thiazole Core 2.4 Oxazole or 1,3-Oxazole 2.4.1 Introduction 2.4.2 Oxazole Synthesis 2.5 Synthetic and Natural Oxazoles 2.5.1 Oxazoles Synthetics and Your Pharmacological Activities 2.5.2 Natural Oxazoles References 3. Lactams, Azetidines, Penicillins, and Cephalosporins: An Overview on the Synthesis and Their Antibacterial Activity 3.1 Lactams 3.1.1 Introduction 3.1.2 Synthesis of 2-Azetidinones (β-Lactams) 3.2 Azetidines 3.2.1 Introduction 3.2.2 Azetidine Synthesis 3.2.3 Azetidines Reactions 3.2.4 Azetidines Therapeutics Use 3.2.5 Natural Azetidines 3.3 Penicillins 3.4 Cephalosporins References 4. Synthesis and Biological Importance of Pyrazole, Pyrazoline, and Indazole as Antibacterial, Antifungal, Antitubercular, Anticancer, and Anti-inflammatory Agents 4.1 Introduction 4.2 Pyrazole 4.2.1 General Preparations of Pyrazole 4.2.2 Synthesis and Antimicrobial Activity of Some Pyrazole Derivatives 4.2.3 Preparation and Antitubercular Activity of Some Pyrazole Hybrids 4.2.4 A Facile Synthesis of Some Novel Pyrazole Derivatives and Their Anticancer Activity 4.2.5 Synthetic Route for the Preparation of Heterocyclic Motifs Appended as Anti-Inflammatory Pyrazole Analogs 4.2.6 Miscellaneous 4.3 Pyrazoline 4.3.1 Multicomponent Reaction and Antimicrobial Activity of Some Pyrazoline Hybrids 4.3.2 Synthesis and Antitubercular Activity of Some Novel Pyrazoline Derivatives 4.3.3 Conventional Synthetic Route and Anticancer Activity of Some Pyrazoline Hybrids 4.3.4 Facile Synthesis and Anti-inflammatory Activity of Some Novel Pyrazolines 4.3.5 Miscellaneous 4.4 Indazole 4.4.1 Indazole Synthesis by Fischer 4.4.2 Indazole Hybrids: Synthesis and Antimicrobial Activity 4.4.3 Antitubercular Activity and Facile Synthesis of Some Novel Indazoles 4.4.4 Preparation and Anticancer Activity of Some Novel Indazoles 4.4.5 A Facile Synthesis and Anti-inflammatory Activity of Some Indazoles 4.4.6 Miscellaneous 4.5 Conclusion References 5. An Overview on the Synthesis and Biological Studies of Some Seven Membered Heterocyclic Systems 5.1 Introduction 5.2 Azepines and Diazepines 5.2.1 Synthesis of Isolated Azepines 5.2.2 Synthesis of Benzo-Fused Azepines and Diazepines 5.3 Oxazepines and Benzoxazepines 5.4 Isolated and Benso-Fused Thiazepines, Dithiazepines 5.4.1 Synthesis of Thiazepines 5.4.2 Synthesis of Benzo- and Heterofused Thiazepines 5.4.3 Synthesis of Dithiazepines 5.5 Summary References 6. Various Synthetic Strategies and Therapeutic Potential of Thiadiazole, Oxadiazole, Isoxazole and Isothiazole Derivatives 6.1 Thiadiazole 6.1.1 Introduction 6.1.2 Synthetic Strategies for Thiadiazole 6.1.3 Therapeutic Potential of Thiadiazole Derivatives 6.2 Oxadiazoles 6.2.1 Introduction 6.2.2 Synthetic Strategies for Oxadiazole 6.2.3 Therapeutic Potential of 1,3,4-Oxadiazole Derivatives 6.2.4 Therapeutic Potential of 1,2,4-Oxadiazole Derivatives 6.3 Isoxazole 6.3.1 Introduction 6.3.2 Synthetic Strategies for Isoxazole 6.3.3 Therapeutic Potential of Isoxazoles 6.4 Isothiazole 6.4.1 Introduction 6.4.2 Synthetic Strategies for Isothiazoles 6.4.3 Therapeutic Potential of Isothiazole Derivatives References 7. Sulfur-Containing Pyrazoles, Pyrazolines and Indazoles 7.1 Introduction 7.2 Design, Synthesis, and Biological Activities of Sulfur-Containing Pyrazoles 7.2.1 Synthesis of Sulfanyl Pyrazole Derivatives 7.2.2 Synthesis of Sulfanylpyrazolones 7.2.3 Synthesis of Sulfanyl Pyrazoles Linked to the Sulfur Atom Through Spacers 7.3 Sulfur-Containing Pyrazolines 7.4 Synthesis of Practically Important Sulfanyl Indazoles 7.5 Conclusion References 8. Synthetic Approach of Quinazolines Candidates 8.1 Introduction 8.2 Synthesis Methods 8.3 Classical Methods 8.4 Modern Methods 8.4.1 Metal Catalyst-Based Reaction 8.4.2 Synthesis by Using Reagent or Base 8.4.3 Microwave-Based Reaction 8.5 Conclusion References 9. An Overview of Cinnolines, Quinazolines and Quinoxalines: Synthesis and Pharmacological Significance 9.1 Introduction 9.1.1 N-Heterocyclic Compounds 9.2 Cinnoline 9.2.1 Introduction 9.2.2 Various Approaches for the Preparation of Cinnolines 9.3 Quinazoline 9.3.1 Introduction 9.3.2 Various Approaches for the Preparation of quinazolines 9.4 Quinoxaline 9.4.1 Introduction 9.4.2 Various Approaches for the Preparation of Quinoxalines 9.5 Conclusion References 10. Pharmacological Significance of Triazoles and Tetrazoles in Neurodegenerative Disease: An Overview 10.1 Introduction 10.2 Synthesis of Triazole and Tetrazole Derivatives 10.2.1 Synthesis of 1-Substituted 1H Tetrazole 10.2.2 Synthesis of 5-Substituted 1H Tetrazole 10.2.3 Synthesis of 1, 5-Disubstituted Tetrazoles 10.2.4 Synthesis of 2-Substituted 2H Tetrazoles 10.2.5 Synthesis of 2, 5-Disubstituted Tetrazoles 10.2.6 Synthesis of 1, 2, 4-Triazoles 10.3 Drugs Containing Triazole and Tetrazole Moiety 10.4 Drugs in Clinical Trials 10.5 Alzheimer’s Disease (AD) 10.5.1 Cholinesterase Inhibitors 10.5.2 Tau Inhibitors 10.5.3 GSK-3β Inhibitors 10.5.4 MA/MAO Inhibitors 10.5.5 BACE-1 Inhibitors 10.5.6 NMDA Receptor Antagonists 10.5.7 Anti-inflammatory Agents 10.5.8 Anti-oxidants 10.6 Parkinson’s Disease 10.7 Amyotrophic Lateral Sclerosis 10.8 Conclusion and Future Directions References 11. An Insight into the Synthesis and Pharmacological Activities of Indoles, Isoindoles and Carbazoles 11.1 Introduction 11.1.1 N-Heterocyclic Compounds 11.2 Indole 11.2.1 Introduction 11.2.2 Biological Activity 11.2.3 Various Methods for the Synthesis of Indole 11.3 Isoindole 11.3.1 Introduction 11.3.2 Biological Activity 11.3.3 Various Methods for the Synthesis of Isoindole 11.4 Carbazole 11.4.1 Introduction 11.4.2 Biological Activity 11.4.3 Various Methods for the Synthesis of Carbazole 11.5 Conclusion References 12. Pyrazoles, Indazoles and Pyrazolines: Recent Developments and Their Properties 12.1 Introduction 12.1.1 Pyrazole 12.1.2 Indazole 12.1.3 Pyrazoline 12.2 Synthetic Protocol of Pyrazoles 12.3 Synthetic Protocol of Indazoles 12.4 Synthetic Protocol of Pyrazolines 12.5 Conclusion References 13. Synthesis of Bioactive Thioxoimidazolidinones, Oxazolidinones, Thioxothiazolidinones, Thiazolidinediones 13.1 Thiazolidine 13.1.1 Introduction 13.1.2 Nanocatalytic Processes to Synthesis of 1,3-Thiazolidine-4-Ones 13.2 Thiazolidine-2,4-dione 13.2.1 Introduction 13.2.2 Nanocatalytic Approaches to Gain Thiazolidinediones 13.3 Oxazolidinones 13.3.1 Introduction 13.3.2 Nanocatalytic Synthesis of Oxazolidinones 13.4 Rhodanine and Thiohydantoin 13.4.1 Introduction 13.4.2 Nanocatalytic Transformation for the Synthesis of Rhodanine and Thiohydantoin 13.5 Conclusion References