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Submit a ProposalHeterocyclic Compounds as Pharmaceutical Ingredients
One Line Description
Unlock the therapeutic potential of N, O, and S-based heterocycles with this comprehensive guide to the synthesis, characterization, and biological interactions of the compounds currently redefining modern drug design.
Audience
Academics, researchers, and industry professionals specializing in material sciences, medical science, pharmacy, environmental, chemical, biochemical, and biomedical engineering, biotechnology, and nanoscience.
Academics, researchers, and industry professionals specializing in material sciences, medical science, pharmacy, environmental, chemical, biochemical, and biomedical engineering, biotechnology, and nanoscience.
Description
Heterocyclic compounds have proven their potential as an active pharmaceutical ingredient due to the presence of N, O, and S in their chemical make-up, making them ideal hydrogen bond acceptors. Recently, a large number of heterocyclic compounds have been documented as drugs after clearing all the phases of preclinical and clinical trials and are commercially available worldwide. This book provides a comprehensive look at the active profile of heterocyclic compounds and their potential applications as antibacterial, antiviral, anti-inflammatory, and anti-cancerous agents, as well as many other applications in the fields of pharmaceutical chemistry, pharmacy, cheminformatics, bioinformatics, and related fields. It covers a wide range of topics, including the synthesis and characterization of heterocyclic compounds, the mechanism of how they interact with biological systems, their proteomics and genotypic activity, and their role as active ingredients against various ailments, including the most fatal diseases like cancer and AIDS. Additionally, the book highlights the challenges and limitations associated with the use of heterocyclic molecules as active pharmaceutical ingredients in terms of their bioavailability and toxicity. This book serves as a valuable resource for researchers, students, and professionals working in the field of drug design using heterocycles.
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Heterocyclic compounds have proven their potential as an active pharmaceutical ingredient due to the presence of N, O, and S in their chemical make-up, making them ideal hydrogen bond acceptors. Recently, a large number of heterocyclic compounds have been documented as drugs after clearing all the phases of preclinical and clinical trials and are commercially available worldwide. This book provides a comprehensive look at the active profile of heterocyclic compounds and their potential applications as antibacterial, antiviral, anti-inflammatory, and anti-cancerous agents, as well as many other applications in the fields of pharmaceutical chemistry, pharmacy, cheminformatics, bioinformatics, and related fields. It covers a wide range of topics, including the synthesis and characterization of heterocyclic compounds, the mechanism of how they interact with biological systems, their proteomics and genotypic activity, and their role as active ingredients against various ailments, including the most fatal diseases like cancer and AIDS. Additionally, the book highlights the challenges and limitations associated with the use of heterocyclic molecules as active pharmaceutical ingredients in terms of their bioavailability and toxicity. This book serves as a valuable resource for researchers, students, and professionals working in the field of drug design using heterocycles.
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Author / Editor Details
Divya Tripathy, PhD is a Professor in the Department of Chemistry in the School of Basic and Applied Sciences at Galgotias University with more than 15 years of experience in teaching, research, and academic leadership. She has published more than 130 peer-reviewed research papers in reputed international journals, authored and edited 11 books, and contributed more than 35 book chapters. Her research focuses on interdisciplinary applications of chemistry in healthcare, environmental remediation, advanced materials, and biomedical technologies.
Divya Tripathy, PhD is a Professor in the Department of Chemistry in the School of Basic and Applied Sciences at Galgotias University with more than 15 years of experience in teaching, research, and academic leadership. She has published more than 130 peer-reviewed research papers in reputed international journals, authored and edited 11 books, and contributed more than 35 book chapters. Her research focuses on interdisciplinary applications of chemistry in healthcare, environmental remediation, advanced materials, and biomedical technologies.
Priyanka Chhabra, PhD is an Assistant Professor in the Amity Institute of Biotechnology at Amity University. Her professional journey reflects a blend of teaching, research, and industry exposure with a strong background in biotechnology and allied fields.
Anjali Gupta, PhD is a Professor in the Department of Chemistry at Galgotias University. She has authored several influential research and review articles and served as a principal investigator for several projects. Her research focuses on biomaterials, MOF-based materials, anti-corrosive coatings, water remediation, and bio-active compounds.
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Table of Contents
Preface
1. Heterocyclic Molecules as an Active Pharmaceutical Ingredient: An Introduction
Anushka Sharma, Awaneet Kaur, Pranav Gupta, Debashis Paramanick and Abdulsalam Alhalmi
1.1 Introduction
1.2 Synthetic Approach for Heterocyclic Compound
1.2.1 Microwave-Assisted Synthesis
1.2.1.1 Pyrazole Derivatives
1.2.1.2 Benzo[b]furans Synthesis
1.2.1.3 Tetrazole Derivatives
1.2.1.4 Benzimidazole Derivatives
1.2.2 Solvent-Free Synthesis
1.2.3 Synthesis of Heterocyclic Compounds Using Nanocatalysts
1.2.3.1 Indole Synthesis
1.2.3.2 Imidazole Synthesis
1.2.4 Ultrasound-Mediated Synthesis
1.3 Medicinal Impact of Heterocyclic Moieties
1.4 Pharmaceutical Applications of Heterocyclic Compounds
1.4.1 Heterocycles as Drugs
1.4.2 Heterocycles as Polymers
1.4.3 Heterocycles as Dyes
1.5 Advantages of Using Heterocycles in Drug Design
1.5.1 Versatility and Reactivity
1.5.2 Enhanced Selectivity and Potency
1.6 Challenges in Developing Heterocyclic Active Pharmaceutical Ingredients
1.7 Recent Advances in Heterocyclic Chemistry
1.8 Conclusion
References
2. Biologically Active Nitrogen Heterocyclic Compounds
Diwakar Chauhan, Monika Chauhan, Priya Tyagi and Amrita Kaushik
2.1 Introduction
2.2 History of Nitrogen-Containing Heterocycles
2.3 Classification of Nitrogen Heterocycles
2.3.1 Nitrogen Heterocycles with Four Members
2.3.2 Nitrogen Heterocycles with Five Members
2.3.3 Nitrogen Heterocycles with Six Members
2.3.4 Fused or Condensed Nitrogen Heterocycles
2.4 N-Heterocycles Containing Medicinally Important Drugs
2.5 Biological Activity
2.5.1 Anti-Alzheimer’s Disease Activity
2.5.2 Anticancer Activity
2.5.3 Antibacterial Activity
2.5.4 Anti-Parkinson’s Activity
2.5.5 Anti-Inflammatory Activity
2.5.6 Antidiabetic Agent
2.5.7 Antiviral Activity
2.5.8 Antioxidant Activity
2.6 Conclusion
Abbreviations
References
3. Heterocyclic Compounds as Antimicrobial (Antibacterial, Antifungal, Antiviral, and Anthelmintics) Agent
Gaurank Pal, Devaang Mathur, Lakshit Srivastav, Vishal Mehare, Ajay Gupta, Shruti Khanna Ahuja and Puja Prasad
3.1 Introduction
3.2 Heterocyclic Compounds as Antimicrobial Agent
3.2.1 Application of Heterocyclic Compounds as Antibacterial Agent
3.2.1.1 Pyrrole
3.2.1.2 Furan
3.2.1.3 Thiophene
3.2.1.4 Indole
3.2.1.5 Quinoline
3.2.1.6 Imidazole
3.2.1.7 Pyrazole
3.2.1.8 Oxazole
3.2.1.9 Thiazole
3.2.1.10 Pyrimidine
3.2.1.11 Pyridine
3.2.2 Antifungal Activity and Structure–Activity Relationship of Heterocyclic Compounds
3.2.2.1 Triazole
3.2.2.2 Imidazoles
3.2.2.3 Oxazoles
3.2.2.4 Thiazoles
3.2.2.5 Pyrimidines
3.2.2.6 Benzimidazoles
3.2.2.7 Benzothiazoles
3.2.3 The Antiviral Activity and SAR of N-Heterocyclic Compounds
3.2.3.1 Triazoles
3.2.3.2 Thiadiazoles
3.2.3.3 Pyrazoles
3.2.3.4 Pyrimidine
3.2.3.5 Imidazole
3.2.3.6 Indole
3.2.3.7 Thiazoles
3.2.4 Application of Heterocyclic Compound as Anthelmintics Agent
3.2.4.1 Pyrrolidine
3.2.4.2 Imidazole
3.2.4.3 Triazole
3.2.4.4 Thiazole
3.3 Conclusion
References
4. Heterocyclic Compounds as Anticancer Agents
Aadya Singh, Priyanshi Kamboj, Pragya Swami, Puja Prasad and Shruti Khanna Ahuja
4.1 Introduction
4.2 Classification of Heterocyclic Compounds
4.2.1 Monocyclic versus Polycyclic Compounds
4.2.2 Different Types of Heterocyclic Compounds Based on Ring Size
4.2.2.1 Five-Membered Heterocycles
4.2.2.2 Six-Membered Heterocycles
4.2.2.3 Polycyclic Heterocycles
4.2.3 Heterocyclic Compounds Based on the Heteroatom
4.2.3.1 Nitrogen-Based Heterocycles
4.2.3.2 Oxygen-Based Heterocycles
4.2.3.3 Sulfur-Based Heterocycles
4.3 Mechanism of Action of Heterocyclic Compounds
4.3.1 Interaction with Nucleic Acids: Intercalation and Alkylation of DNA
4.3.2 Inhibition of Key Enzymes and Enzymatic Pathways (Targeting Specific Cancer Pathways)
4.3.3 Modulation of Cell Signaling Pathways and Cell Cycle
4.3.4 Interaction with Immune System
4.3.5 Inhibition of Tumor Growth and Metastasis
4.3.6 Role of Heterocycles in Modulating the Tumor Microenvironment
4.4 Key Heterocyclic Anticancer Agents
4.4.1 Alkaloids: Vincristine and Vinblastine, CPT Derivatives
4.4.2 Camptothecin Derivatives
4.4.3 Flavonoids
4.4.4 Flavonols
4.4.5 Nitrogen-Containing Heterocycles: Purines and Pyrimidines, Imidazoles, and Benzimidazoles
4.4.6 Taxanes
4.4.7 Anthracycline
4.5 Challenges in Heterocyclic Anticancer Drug Development
References
5. Heterocyclic Compounds as Anti-Inflammatory Agents
Hemlata Nimesh, Sagar Kumar and Nidhi Shrivastava
5.1 Introduction
5.2 Classification
5.3 Various Heterocyclic Derivatives as Anti-Inflammatory Drugs
5.3.1 Pyrazole and Pyrazolines Derivatives as Anti-Inflammatory Drugs
5.3.2 Pyrimidine Derivatives as Anti-Inflammatory Drugs
5.3.3 Indole Derivatives as Anti-Inflammatory Drugs
5.3.4 Imidazole and Benzimidazole Derivatives as Anti-Inflammatory Drugs
5.3.5 Pyrrole as Anti-Inflammatory Drugs
5.3.6 Furanone as Anti-Inflammatory Drugs
5.3.7 Oxazole and Isoxazole as Anti-Inflammatory Drugs
5.3.8 Thiazole as Anti-Inflammatory Drugs
5.3.9 Pyridine as Anti-Inflammatory Drugs
5.4 Conclusion and Future Prospects
References
6. Heterocyclic Compounds as Antioxidant Agents
Niranjan Kaushik, Shristi Singh, Ajita Paliwal and Sachin Chaudhary
6.1 Introduction: Antioxidants and Oxidative Stress
6.2 Mechanism of Antioxidant Agent
6.3 Structures and Classifications of Heterocyclic Compound
6.3.1 Role of Heterocyclic Structure Enhancing Antioxidant Activity
6.3.2 Existing Heterocyclic Antioxidant Compounds
6.4 Types of Heterocyclic Compounds with Antioxidant Properties
6.4.1 Nitrogen-Containing Heterocyclic
6.4.1.1 Pyridine
6.4.1.2 Pyrimidine
6.4.2 Oxygen-Containing Heterocycles
6.4.2.1 Furan
6.4.2.2 Benzofuran
6.4.2.3 Coumarin
6.4.3 Sulfur-Containing Heterocycles
6.4.3.1 Thiophene
6.5 Antioxidant Effect and Mechanism of Action of Polyphenolic Compound
6.5.1 Flavonoids
6.5.1.1 Catechins
6.5.1.2 Flavonols
6.5.2 Phenolic Acids
6.5.3 Stilbenes
6.6 Factors Influencing the Antioxidant Capacity of Polyphenols
6.6.1 Structure
6.6.2 Stability
6.6.3 Bioavailability
6.6.4 Environmental Factor
6.7 Conclusion
References
7. Heterocyclic Compounds as Anticonvulsants, Antipyretics, Antiallergic Agents, and Antileprosy Agents
Anushka Sharma, Awaneet Kaur, Pranav Gupta, Debashis Paramanick and Abdulsalam Alhalmi
7.1 Introduction
7.2 Heterocyclic Compounds as Anticonvulsant Agents
7.3 Heterocyclic Compounds as Antipyretic Agents
7.4 Heterocyclic Compounds as Antiallergic Agents
7.5 Heterocyclic Compounds as Antileprosy Agents
7.6 Recent Advances and Future Prospects
7.6.1 Novel Synthetic Approaches
7.6.2 Drug Design and Molecular Modeling
7.7 Conclusion
References
8. Heterocyclic Compounds as Antihistamine Agents
Avinash Jha, Saurabh Sharma, Deepika Paliwal, Aman Thakur and Saurabh Srivasatva
8.1 Introduction
8.1.1 Overview of Histamine
8.1.2 Histamine Role in Disease
8.1.3 Antihistamine Agents
8.1.3.1 H1 Antihistamine
8.1.4 Role of Heterocyclic Compound in Drug Development
8.2 Histamine Receptor
8.2.1 H1 Receptor
8.2.2 H2 Receptor
8.2.3 H3 Receptor
8.2.4 H4 Receptor
8.3 Imidazole as Antihistamine Agents
8.4 Piperazine as Antihistamine Agents
8.5 Quinazoline as Antihistamine Agents
8.6 Piperadine as Antihistamine Agents
8.7 Ethanolamines as Antihistamine Agents
8.8 Conclusion
References
9. Heterocyclic Compound Having Herbicides Activity
Niranjan Kaushik, Mridul Singh Sengar, Deepika Paliwal and Nadeem Ahmad Siddique
9.1 Introduction
9.1.1 Historical Background
9.1.2 Herbicides
9.2 Mechanisms of Herbicide Action and Their Role in Plant Growth Inhibition
9.2.1 Inhibitors for Lipid Synthesis
9.2.2 Inhibitors of Amino Acid Synthesis
9.2.3 Photosynthesis Inhibitors
9.2.4 Growth Regulators
9.2.5 Nitrogen Metabolism Inhibitors
9.2.6 Pigment Inhibitors
9.2.7 Cell Membrane Disrupter
9.2.8 Seedling Shoot Growth Inhibitors
9.2.9 Seedling Root Growth Inhibitors
9.2.10 Several Innovative Ways That Herbicides Work
9.3 Heterocyclic Having Herbicides Activity
9.3.1 Triazines
9.3.2 Triazinone
9.3.3 Pyridine
9.3.4 Pyrazole Benzophenone Derivatives
9.3.5 Imidazolines
9.4 Environmental Impact and Resistance Management
9.4.1 Environmental Considerations
9.4.2 Fundamentals of How Weeds React to a Climate with Higher CO2 and Temperature
9.4.3 Resistance Develop in Transgenic Plants
9.5 Field Applications
9.6 Future Prospects of Heterocyclic Herbicides
9.7 Conclusion
References
10. Heterocyclic Compounds as Antihypertensive Agents
Manjot Singh, Deepika Paliwal, Aman Thakur, Manvi Karayat and Saurabh Srivasatva
10.1 Introduction
10.1.1 Marketed Drugs for Hypertension
10.1.2 Significance of Heterocyclic Compounds
10.1.3 Structural Versatility of Heterocyclic Compounds
10.1.4 Pharmacophoric Potential of Heterocyclic Rings
10.1.5 Enhancement of Bioavailability and Stability
10.1.6 Specific Mechanistic Action
10.2 Heterocyclic Moieties against Hypertension
10.2.1 Indole and Indazole Moiety
10.2.2 Imidazole
10.2.3 Furan
10.2.4 Tetrazole
10.2.5 Thiadiazole
10.2.6 Quinazoline
10.2.7 Thiazolidine
10.2.8 Triazole
10.2.9 Pyridine
10.3 Future Prospective
10.4 Conclusion
References
11. In Silico Studies on Heterocyclics as an Active Pharmaceutical Agent
Anurag Paul, Debanjali Adhikary, Abdul Kareem Parchur, Gayatri Sharma and Apoorva Mishra
11.1 Introduction
11.2 In Silico Approaches for Heterocyclic Drug Discovery
11.2.1 Molecular Docking
11.2.2 Molecular Dynamic Simulations
11.2.3 Quantitative Structure–Activity Relationship
11.2.4 Pharmacophore Modeling
11.2.5 ADMET and Toxicity Prediction
11.3 Heterocyclic Compounds as Active Pharmaceutical Agents
11.3.1 Antifungal Activity
11.3.2 Antibacterial Activity
11.3.3 Anticancer Activity
11.3.4 Herbicidal Activity
11.3.5 Anticonvulsant
11.4 Challenges and Future Trends
11.5 Conclusion
References
12. Piperazine Derivatives: Potential Antimicrobial Agents
R. Prathap, Rashmi Dubey, Anjali Gupta and Divya Bajpai Tripathy
12.1 Introduction
12.2 Synthetic Strategies for Piperazine Derivatives
12.2.1 Synthesis of 1-Benzyl-4-Phenylpiperazine
12.2.2 Synthesis of 1-Phenylpiperazine
12.2.3 Synthesis of 1-[(4-Chlorophenyl)sulfonyl]piperazine
12.2.4 Synthesis of Piperazine-Phthalimide Derivatives
12.2.5 Synthesis of Sulfonyl Piperazine
12.2.6 Synthesis of 1-(2,5-Dimethoxyphenyl)piperazine
12.3 Structural Relationship of Piperazine Derivatives
12.4 Antimicrobial Activities of Piperazine Derivatives
12.4.1 Antibacterial Activity
12.4.2 Antifungal Activity
12.4.3 Antiparasitic Activity
12.4.4 Anticancerous Activities of Piperazine Derivatives
12.5 Synergistic Activity of Piperazine Derivatives with Other Antimicrobial Agents, Enhancing Their Effectiveness against Certain Pathogens
12.6 Mechanism of Action
12.6.1 Inhibition of Cell Wall Synthesis
12.6.2 Inhibition of Protein Synthesis
12.6.3 Disruption of Membrane Integrity
12.6.4 Inhibition of Nucleic Acid Synthesis
12.7 Applications of Piperazine Derivatives as Microbial Agents
12.7.1 In human medicine
12.7.2 Treatment of Bacterial Infections
12.7.3 Treatment of Fungal Infections
12.7.4 Treatment of Parasitic Infections
12.7.5 Disinfection and Sanitation
12.7.6 As Anticancerous Agents
12.8 In Veterinary Medicine
12.8.1 Treatment of Bacterial Infections in Livestock
12.8.2 Treatment of Parasitic Infections in Pets
12.8.3 Use as a Disinfectant
12.9 In Agriculture
12.9.1 Control of Plant Pathogens
12.9.2 Preservation of Crops
12.9.3 Control of Nematodes
12.10 Challenges and Future Prospects
12.11 Conclusion
References
13. Synthetic Drug Discovery Strategy of Benzimidazole Derivatives and Their Applications
Prasad Vijay Korake, Diwakar Chauhan and Subhalaxmi Pradhan
Abbreviations
13.1 Introduction
13.2 Benzimidazole as an Antifungal Agent
13.3 Benzimidazole as an Antimicrobial Agent
13.4 Benzimidazole as an Anticancer Agent
13.5 Conclusion
References
14. Synthesis and Biological Evaluation of Thiophene-and Piperazine-Based Active Compounds
Ayyagari Subramanya Sharma, Subhalaxmi Pradhan and Prashant Kumar
14.1 Introduction
14.2 Chemistry of Thiophene and Synthesis of Its Derivative
14.2.1 Metal-Catalyzed Synthetic Approaches
14.2.2 Metal-Free Synthetic Approaches
14.2.3 Multicomponent Synthetic Approaches
14.3 Biological Application of Thiophene and Its Derivatives
14.3.1 Mono-Substituted Thiophene Derivatives as Anticancer Agents
14.3.2 Di-Substituted Thiophene Derivatives as Anticancer Agents
14.3.3 Tri-Substituted Thiophene Derivatives as Anticancer Agents
14.3.4 Biological Application of Thiophene Derivatives as Antimalarial Agent
14.3.5 Biological Application of Thiophene-Based Compounds as Anti-nflammatory Agent
14.3.6 Biological Applications Thiophene-Based Compounds as Antidepressant
14.3.7 Biological Applications of Thiophene Analogs as Anti-Inflammatory and Analgesic
14.3.8 Biological Applications of Thiophene Analogs as Anticonvulsant
14.3.9 Biological Applications of Thiophene-Based Compound as Antidiabetic Agent
14.4 Biological Application of Piperazine-Based Compounds
14.4.1 Piperazine as an Antimicrobial Agent
14.4.2 Anticancer Activity of Piperazine
14.4.3 Antioxidant Activity of Piperazine
14.4.4 Antitumor Activity of Piperazine
14.4.5 Piperazine: Insecticidal Activity
14.4.6 Piperazine: Antidiabetic Activity
14.4.7 Piperazine Derivatives as Anti-Inflammatory and Analgesic Agents
14.5 Conclusion
References
15. Heterocyclic Compounds as Antileprotic Agents
Sanjita Das, Anjali Singh, Shalini Gautam and Gyas Khan
15.1 Introduction
15.2 Historical Perspectives
15.3 Pathophysiology
15.4 Classification of Heterocyclic Antileprotic Drugs
15.4.1 Characteristics of Structure
15.4.2 Heterocyclic Ring’s Role in Mechanism of Action
15.5 Important Heterocyclic Antileprotic Drugs
15.5.1 Clofazimine
15.5.2 Rifampin
15.5.3 Ethionamide
15.5.4 Dapsone or Di-Amino-Diphenyl-Sulfone
15.5.5 Fluoroquinolones
15.5.6 Minocycline
15.5.7 Clarithromycin
15.6 Advances in Antileprotic Agents
15.7 Obstacles and Prospects for the Development of Heterocyclic Antileprotic Drugs
References
16. Bromodomains: Biomedical Applications of Active Ingredients
Sweta Raj, Anjan Kumar Nayak, Harsh Vardhan and Divya Bajpai Tripathy
16.1 Introduction
16.1.1 Significance in Medical Researches
16.2 History and Discovery of BRDs
16.2.1 Evolution of BRD Research
16.2.2 Structure of BRDs
16 2.3 Interaction with Acetylated Lysines
16.3 BRDs as Drug Targets
16.3.1 Drug Design Strategies Targeting BRDs
16.4 BRD Inhibitors
16.5 Next-Generation BRDs Inhibitors
16.5.1 Two Classes of BET Inhibitors
16.6 BET Inhibitors in Clinical Trials
16.6.1 Key Insights on Selectivity between BRD4 (BRD1) and BRD3 (BRD2)
16.6.2 BD2 Selectivity (Why Target Selective Compounds?)
16.7 Resistance toward BET Inhibitors
16.8 Toxicity of BET Inhibitors Used Clinically
16.9 BRD Inhibition and Human Diseases
16.9.1 Cancer
16.9.2 Cardiovascular Disease
16.10 Conclusion and Future Perspectives
References
Index
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Preface
1. Heterocyclic Molecules as an Active Pharmaceutical Ingredient: An Introduction
Anushka Sharma, Awaneet Kaur, Pranav Gupta, Debashis Paramanick and Abdulsalam Alhalmi
1.1 Introduction
1.2 Synthetic Approach for Heterocyclic Compound
1.2.1 Microwave-Assisted Synthesis
1.2.1.1 Pyrazole Derivatives
1.2.1.2 Benzo[b]furans Synthesis
1.2.1.3 Tetrazole Derivatives
1.2.1.4 Benzimidazole Derivatives
1.2.2 Solvent-Free Synthesis
1.2.3 Synthesis of Heterocyclic Compounds Using Nanocatalysts
1.2.3.1 Indole Synthesis
1.2.3.2 Imidazole Synthesis
1.2.4 Ultrasound-Mediated Synthesis
1.3 Medicinal Impact of Heterocyclic Moieties
1.4 Pharmaceutical Applications of Heterocyclic Compounds
1.4.1 Heterocycles as Drugs
1.4.2 Heterocycles as Polymers
1.4.3 Heterocycles as Dyes
1.5 Advantages of Using Heterocycles in Drug Design
1.5.1 Versatility and Reactivity
1.5.2 Enhanced Selectivity and Potency
1.6 Challenges in Developing Heterocyclic Active Pharmaceutical Ingredients
1.7 Recent Advances in Heterocyclic Chemistry
1.8 Conclusion
References
2. Biologically Active Nitrogen Heterocyclic Compounds
Diwakar Chauhan, Monika Chauhan, Priya Tyagi and Amrita Kaushik
2.1 Introduction
2.2 History of Nitrogen-Containing Heterocycles
2.3 Classification of Nitrogen Heterocycles
2.3.1 Nitrogen Heterocycles with Four Members
2.3.2 Nitrogen Heterocycles with Five Members
2.3.3 Nitrogen Heterocycles with Six Members
2.3.4 Fused or Condensed Nitrogen Heterocycles
2.4 N-Heterocycles Containing Medicinally Important Drugs
2.5 Biological Activity
2.5.1 Anti-Alzheimer’s Disease Activity
2.5.2 Anticancer Activity
2.5.3 Antibacterial Activity
2.5.4 Anti-Parkinson’s Activity
2.5.5 Anti-Inflammatory Activity
2.5.6 Antidiabetic Agent
2.5.7 Antiviral Activity
2.5.8 Antioxidant Activity
2.6 Conclusion
Abbreviations
References
3. Heterocyclic Compounds as Antimicrobial (Antibacterial, Antifungal, Antiviral, and Anthelmintics) Agent
Gaurank Pal, Devaang Mathur, Lakshit Srivastav, Vishal Mehare, Ajay Gupta, Shruti Khanna Ahuja and Puja Prasad
3.1 Introduction
3.2 Heterocyclic Compounds as Antimicrobial Agent
3.2.1 Application of Heterocyclic Compounds as Antibacterial Agent
3.2.1.1 Pyrrole
3.2.1.2 Furan
3.2.1.3 Thiophene
3.2.1.4 Indole
3.2.1.5 Quinoline
3.2.1.6 Imidazole
3.2.1.7 Pyrazole
3.2.1.8 Oxazole
3.2.1.9 Thiazole
3.2.1.10 Pyrimidine
3.2.1.11 Pyridine
3.2.2 Antifungal Activity and Structure–Activity Relationship of Heterocyclic Compounds
3.2.2.1 Triazole
3.2.2.2 Imidazoles
3.2.2.3 Oxazoles
3.2.2.4 Thiazoles
3.2.2.5 Pyrimidines
3.2.2.6 Benzimidazoles
3.2.2.7 Benzothiazoles
3.2.3 The Antiviral Activity and SAR of N-Heterocyclic Compounds
3.2.3.1 Triazoles
3.2.3.2 Thiadiazoles
3.2.3.3 Pyrazoles
3.2.3.4 Pyrimidine
3.2.3.5 Imidazole
3.2.3.6 Indole
3.2.3.7 Thiazoles
3.2.4 Application of Heterocyclic Compound as Anthelmintics Agent
3.2.4.1 Pyrrolidine
3.2.4.2 Imidazole
3.2.4.3 Triazole
3.2.4.4 Thiazole
3.3 Conclusion
References
4. Heterocyclic Compounds as Anticancer Agents
Aadya Singh, Priyanshi Kamboj, Pragya Swami, Puja Prasad and Shruti Khanna Ahuja
4.1 Introduction
4.2 Classification of Heterocyclic Compounds
4.2.1 Monocyclic versus Polycyclic Compounds
4.2.2 Different Types of Heterocyclic Compounds Based on Ring Size
4.2.2.1 Five-Membered Heterocycles
4.2.2.2 Six-Membered Heterocycles
4.2.2.3 Polycyclic Heterocycles
4.2.3 Heterocyclic Compounds Based on the Heteroatom
4.2.3.1 Nitrogen-Based Heterocycles
4.2.3.2 Oxygen-Based Heterocycles
4.2.3.3 Sulfur-Based Heterocycles
4.3 Mechanism of Action of Heterocyclic Compounds
4.3.1 Interaction with Nucleic Acids: Intercalation and Alkylation of DNA
4.3.2 Inhibition of Key Enzymes and Enzymatic Pathways (Targeting Specific Cancer Pathways)
4.3.3 Modulation of Cell Signaling Pathways and Cell Cycle
4.3.4 Interaction with Immune System
4.3.5 Inhibition of Tumor Growth and Metastasis
4.3.6 Role of Heterocycles in Modulating the Tumor Microenvironment
4.4 Key Heterocyclic Anticancer Agents
4.4.1 Alkaloids: Vincristine and Vinblastine, CPT Derivatives
4.4.2 Camptothecin Derivatives
4.4.3 Flavonoids
4.4.4 Flavonols
4.4.5 Nitrogen-Containing Heterocycles: Purines and Pyrimidines, Imidazoles, and Benzimidazoles
4.4.6 Taxanes
4.4.7 Anthracycline
4.5 Challenges in Heterocyclic Anticancer Drug Development
References
5. Heterocyclic Compounds as Anti-Inflammatory Agents
Hemlata Nimesh, Sagar Kumar and Nidhi Shrivastava
5.1 Introduction
5.2 Classification
5.3 Various Heterocyclic Derivatives as Anti-Inflammatory Drugs
5.3.1 Pyrazole and Pyrazolines Derivatives as Anti-Inflammatory Drugs
5.3.2 Pyrimidine Derivatives as Anti-Inflammatory Drugs
5.3.3 Indole Derivatives as Anti-Inflammatory Drugs
5.3.4 Imidazole and Benzimidazole Derivatives as Anti-Inflammatory Drugs
5.3.5 Pyrrole as Anti-Inflammatory Drugs
5.3.6 Furanone as Anti-Inflammatory Drugs
5.3.7 Oxazole and Isoxazole as Anti-Inflammatory Drugs
5.3.8 Thiazole as Anti-Inflammatory Drugs
5.3.9 Pyridine as Anti-Inflammatory Drugs
5.4 Conclusion and Future Prospects
References
6. Heterocyclic Compounds as Antioxidant Agents
Niranjan Kaushik, Shristi Singh, Ajita Paliwal and Sachin Chaudhary
6.1 Introduction: Antioxidants and Oxidative Stress
6.2 Mechanism of Antioxidant Agent
6.3 Structures and Classifications of Heterocyclic Compound
6.3.1 Role of Heterocyclic Structure Enhancing Antioxidant Activity
6.3.2 Existing Heterocyclic Antioxidant Compounds
6.4 Types of Heterocyclic Compounds with Antioxidant Properties
6.4.1 Nitrogen-Containing Heterocyclic
6.4.1.1 Pyridine
6.4.1.2 Pyrimidine
6.4.2 Oxygen-Containing Heterocycles
6.4.2.1 Furan
6.4.2.2 Benzofuran
6.4.2.3 Coumarin
6.4.3 Sulfur-Containing Heterocycles
6.4.3.1 Thiophene
6.5 Antioxidant Effect and Mechanism of Action of Polyphenolic Compound
6.5.1 Flavonoids
6.5.1.1 Catechins
6.5.1.2 Flavonols
6.5.2 Phenolic Acids
6.5.3 Stilbenes
6.6 Factors Influencing the Antioxidant Capacity of Polyphenols
6.6.1 Structure
6.6.2 Stability
6.6.3 Bioavailability
6.6.4 Environmental Factor
6.7 Conclusion
References
7. Heterocyclic Compounds as Anticonvulsants, Antipyretics, Antiallergic Agents, and Antileprosy Agents
Anushka Sharma, Awaneet Kaur, Pranav Gupta, Debashis Paramanick and Abdulsalam Alhalmi
7.1 Introduction
7.2 Heterocyclic Compounds as Anticonvulsant Agents
7.3 Heterocyclic Compounds as Antipyretic Agents
7.4 Heterocyclic Compounds as Antiallergic Agents
7.5 Heterocyclic Compounds as Antileprosy Agents
7.6 Recent Advances and Future Prospects
7.6.1 Novel Synthetic Approaches
7.6.2 Drug Design and Molecular Modeling
7.7 Conclusion
References
8. Heterocyclic Compounds as Antihistamine Agents
Avinash Jha, Saurabh Sharma, Deepika Paliwal, Aman Thakur and Saurabh Srivasatva
8.1 Introduction
8.1.1 Overview of Histamine
8.1.2 Histamine Role in Disease
8.1.3 Antihistamine Agents
8.1.3.1 H1 Antihistamine
8.1.4 Role of Heterocyclic Compound in Drug Development
8.2 Histamine Receptor
8.2.1 H1 Receptor
8.2.2 H2 Receptor
8.2.3 H3 Receptor
8.2.4 H4 Receptor
8.3 Imidazole as Antihistamine Agents
8.4 Piperazine as Antihistamine Agents
8.5 Quinazoline as Antihistamine Agents
8.6 Piperadine as Antihistamine Agents
8.7 Ethanolamines as Antihistamine Agents
8.8 Conclusion
References
9. Heterocyclic Compound Having Herbicides Activity
Niranjan Kaushik, Mridul Singh Sengar, Deepika Paliwal and Nadeem Ahmad Siddique
9.1 Introduction
9.1.1 Historical Background
9.1.2 Herbicides
9.2 Mechanisms of Herbicide Action and Their Role in Plant Growth Inhibition
9.2.1 Inhibitors for Lipid Synthesis
9.2.2 Inhibitors of Amino Acid Synthesis
9.2.3 Photosynthesis Inhibitors
9.2.4 Growth Regulators
9.2.5 Nitrogen Metabolism Inhibitors
9.2.6 Pigment Inhibitors
9.2.7 Cell Membrane Disrupter
9.2.8 Seedling Shoot Growth Inhibitors
9.2.9 Seedling Root Growth Inhibitors
9.2.10 Several Innovative Ways That Herbicides Work
9.3 Heterocyclic Having Herbicides Activity
9.3.1 Triazines
9.3.2 Triazinone
9.3.3 Pyridine
9.3.4 Pyrazole Benzophenone Derivatives
9.3.5 Imidazolines
9.4 Environmental Impact and Resistance Management
9.4.1 Environmental Considerations
9.4.2 Fundamentals of How Weeds React to a Climate with Higher CO2 and Temperature
9.4.3 Resistance Develop in Transgenic Plants
9.5 Field Applications
9.6 Future Prospects of Heterocyclic Herbicides
9.7 Conclusion
References
10. Heterocyclic Compounds as Antihypertensive Agents
Manjot Singh, Deepika Paliwal, Aman Thakur, Manvi Karayat and Saurabh Srivasatva
10.1 Introduction
10.1.1 Marketed Drugs for Hypertension
10.1.2 Significance of Heterocyclic Compounds
10.1.3 Structural Versatility of Heterocyclic Compounds
10.1.4 Pharmacophoric Potential of Heterocyclic Rings
10.1.5 Enhancement of Bioavailability and Stability
10.1.6 Specific Mechanistic Action
10.2 Heterocyclic Moieties against Hypertension
10.2.1 Indole and Indazole Moiety
10.2.2 Imidazole
10.2.3 Furan
10.2.4 Tetrazole
10.2.5 Thiadiazole
10.2.6 Quinazoline
10.2.7 Thiazolidine
10.2.8 Triazole
10.2.9 Pyridine
10.3 Future Prospective
10.4 Conclusion
References
11. In Silico Studies on Heterocyclics as an Active Pharmaceutical Agent
Anurag Paul, Debanjali Adhikary, Abdul Kareem Parchur, Gayatri Sharma and Apoorva Mishra
11.1 Introduction
11.2 In Silico Approaches for Heterocyclic Drug Discovery
11.2.1 Molecular Docking
11.2.2 Molecular Dynamic Simulations
11.2.3 Quantitative Structure–Activity Relationship
11.2.4 Pharmacophore Modeling
11.2.5 ADMET and Toxicity Prediction
11.3 Heterocyclic Compounds as Active Pharmaceutical Agents
11.3.1 Antifungal Activity
11.3.2 Antibacterial Activity
11.3.3 Anticancer Activity
11.3.4 Herbicidal Activity
11.3.5 Anticonvulsant
11.4 Challenges and Future Trends
11.5 Conclusion
References
12. Piperazine Derivatives: Potential Antimicrobial Agents
R. Prathap, Rashmi Dubey, Anjali Gupta and Divya Bajpai Tripathy
12.1 Introduction
12.2 Synthetic Strategies for Piperazine Derivatives
12.2.1 Synthesis of 1-Benzyl-4-Phenylpiperazine
12.2.2 Synthesis of 1-Phenylpiperazine
12.2.3 Synthesis of 1-[(4-Chlorophenyl)sulfonyl]piperazine
12.2.4 Synthesis of Piperazine-Phthalimide Derivatives
12.2.5 Synthesis of Sulfonyl Piperazine
12.2.6 Synthesis of 1-(2,5-Dimethoxyphenyl)piperazine
12.3 Structural Relationship of Piperazine Derivatives
12.4 Antimicrobial Activities of Piperazine Derivatives
12.4.1 Antibacterial Activity
12.4.2 Antifungal Activity
12.4.3 Antiparasitic Activity
12.4.4 Anticancerous Activities of Piperazine Derivatives
12.5 Synergistic Activity of Piperazine Derivatives with Other Antimicrobial Agents, Enhancing Their Effectiveness against Certain Pathogens
12.6 Mechanism of Action
12.6.1 Inhibition of Cell Wall Synthesis
12.6.2 Inhibition of Protein Synthesis
12.6.3 Disruption of Membrane Integrity
12.6.4 Inhibition of Nucleic Acid Synthesis
12.7 Applications of Piperazine Derivatives as Microbial Agents
12.7.1 In human medicine
12.7.2 Treatment of Bacterial Infections
12.7.3 Treatment of Fungal Infections
12.7.4 Treatment of Parasitic Infections
12.7.5 Disinfection and Sanitation
12.7.6 As Anticancerous Agents
12.8 In Veterinary Medicine
12.8.1 Treatment of Bacterial Infections in Livestock
12.8.2 Treatment of Parasitic Infections in Pets
12.8.3 Use as a Disinfectant
12.9 In Agriculture
12.9.1 Control of Plant Pathogens
12.9.2 Preservation of Crops
12.9.3 Control of Nematodes
12.10 Challenges and Future Prospects
12.11 Conclusion
References
13. Synthetic Drug Discovery Strategy of Benzimidazole Derivatives and Their Applications
Prasad Vijay Korake, Diwakar Chauhan and Subhalaxmi Pradhan
Abbreviations
13.1 Introduction
13.2 Benzimidazole as an Antifungal Agent
13.3 Benzimidazole as an Antimicrobial Agent
13.4 Benzimidazole as an Anticancer Agent
13.5 Conclusion
References
14. Synthesis and Biological Evaluation of Thiophene-and Piperazine-Based Active Compounds
Ayyagari Subramanya Sharma, Subhalaxmi Pradhan and Prashant Kumar
14.1 Introduction
14.2 Chemistry of Thiophene and Synthesis of Its Derivative
14.2.1 Metal-Catalyzed Synthetic Approaches
14.2.2 Metal-Free Synthetic Approaches
14.2.3 Multicomponent Synthetic Approaches
14.3 Biological Application of Thiophene and Its Derivatives
14.3.1 Mono-Substituted Thiophene Derivatives as Anticancer Agents
14.3.2 Di-Substituted Thiophene Derivatives as Anticancer Agents
14.3.3 Tri-Substituted Thiophene Derivatives as Anticancer Agents
14.3.4 Biological Application of Thiophene Derivatives as Antimalarial Agent
14.3.5 Biological Application of Thiophene-Based Compounds as Anti-nflammatory Agent
14.3.6 Biological Applications Thiophene-Based Compounds as Antidepressant
14.3.7 Biological Applications of Thiophene Analogs as Anti-Inflammatory and Analgesic
14.3.8 Biological Applications of Thiophene Analogs as Anticonvulsant
14.3.9 Biological Applications of Thiophene-Based Compound as Antidiabetic Agent
14.4 Biological Application of Piperazine-Based Compounds
14.4.1 Piperazine as an Antimicrobial Agent
14.4.2 Anticancer Activity of Piperazine
14.4.3 Antioxidant Activity of Piperazine
14.4.4 Antitumor Activity of Piperazine
14.4.5 Piperazine: Insecticidal Activity
14.4.6 Piperazine: Antidiabetic Activity
14.4.7 Piperazine Derivatives as Anti-Inflammatory and Analgesic Agents
14.5 Conclusion
References
15. Heterocyclic Compounds as Antileprotic Agents
Sanjita Das, Anjali Singh, Shalini Gautam and Gyas Khan
15.1 Introduction
15.2 Historical Perspectives
15.3 Pathophysiology
15.4 Classification of Heterocyclic Antileprotic Drugs
15.4.1 Characteristics of Structure
15.4.2 Heterocyclic Ring’s Role in Mechanism of Action
15.5 Important Heterocyclic Antileprotic Drugs
15.5.1 Clofazimine
15.5.2 Rifampin
15.5.3 Ethionamide
15.5.4 Dapsone or Di-Amino-Diphenyl-Sulfone
15.5.5 Fluoroquinolones
15.5.6 Minocycline
15.5.7 Clarithromycin
15.6 Advances in Antileprotic Agents
15.7 Obstacles and Prospects for the Development of Heterocyclic Antileprotic Drugs
References
16. Bromodomains: Biomedical Applications of Active Ingredients
Sweta Raj, Anjan Kumar Nayak, Harsh Vardhan and Divya Bajpai Tripathy
16.1 Introduction
16.1.1 Significance in Medical Researches
16.2 History and Discovery of BRDs
16.2.1 Evolution of BRD Research
16.2.2 Structure of BRDs
16 2.3 Interaction with Acetylated Lysines
16.3 BRDs as Drug Targets
16.3.1 Drug Design Strategies Targeting BRDs
16.4 BRD Inhibitors
16.5 Next-Generation BRDs Inhibitors
16.5.1 Two Classes of BET Inhibitors
16.6 BET Inhibitors in Clinical Trials
16.6.1 Key Insights on Selectivity between BRD4 (BRD1) and BRD3 (BRD2)
16.6.2 BD2 Selectivity (Why Target Selective Compounds?)
16.7 Resistance toward BET Inhibitors
16.8 Toxicity of BET Inhibitors Used Clinically
16.9 BRD Inhibition and Human Diseases
16.9.1 Cancer
16.9.2 Cardiovascular Disease
16.10 Conclusion and Future Perspectives
References
Index
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