Medicinal Chemistry of Chemotherapeutic Agents

A Comprehensive Resource of Anti-infective and Anti-cancer Drugs

1st Edition - March 9, 2023
Editors: Pratap Chandra Acharya, Michio Kurosu
Language: English
Paperback ISBN:
9 7 8 - 0 - 3 2 3 - 9 0 5 7 5 - 6
eBook ISBN:
9 7 8 - 0 - 3 2 3 - 9 0 7 0 1 - 9

Medicinal Chemistry of Chemotherapeutic Agents: A Comprehensive Resource of Anti-infective and Anti-cancer Drugs focuses on the basics and fundamentals of chemistry involved… Read more

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Medicinal Chemistry of Chemotherapeutic Agents: A Comprehensive Resource of Anti-infective and Anti-cancer Drugs focuses on the basics and fundamentals of chemistry involved in chemotherapeutic agents. Each chapter comprises distinct chemical classifications that include structure and IUPAC nomenclature, synthetic schemes and routes for each drug, mechanism of the drug action, metabolic pathway and structure–activity relationship (SAR) studies. The book covers current research focused on drug resistance and methods to overcome it, the development of newer drugs belonging to each category of the chemotherapeutic agents, molecules currently under clinical trials, and newly approved drugs, if any.

This book will be a valuable resource for academics and researchers, helping them to understand the fundamentals of the medicinal chemistry of the chemotherapeutic agents.

Cover image
Title page
Table of Contents
Copyright
Dedication
List of contributors
Preface
Acknowledgments
Chapter 1. Introduction to chemotherapy: general and clinical considerations
1.1. Introduction
1.2. Adverse effects and associated drawbacks of the chemotherapeutic agents
1.3. Factors affecting the clinical choice of the chemotherapeutic agents
1.4. Combination therapy and chemotherapeutic regimens
1.5. Current status of the research and development of chemotherapeutic drugs
1.6. Conclusions
Section I. Antibacterial agents
Chapter 2. Sulfonamides, quinolones, antiseptics, and disinfectants
2.1. Sulfonamides
2.2. Quinolones
2.3. Antiseptics and disinfectants
Section II. Antibacterial antibiotics
Chapter 3. β-Lactam antibiotics
3.1. A miracle drug
3.2. The penicillins
3.3. The cephalosporins
3.4. The cephamycins
3.5. The carbapenems
3.6. The penems
3.7. The monobactams and the monosulfactams
3.8. β-Lactam-based β-lactamase inactivators and their β-lactam combinations
3.9. Non-β-lactam-based β-lactamase inactivators and their β-lactam combinations
3.10. The γ-lactams
3.11. Other resistance-breaking strategies
3.12. Future of the β-lactams
Chapter 4. Tetracyclines and chloramphenicol
4.1. Tetracyclines
4.2. Chloramphenicol
4.3. Synthesis of some selected drugs
4.4. Conclusions
Chapter 5. Aminoglycoside antibiotics
5.1. Introduction
5.2. Chemistry and pharmacology of aminoglycosides
5.3. Classification of aminoglycoside antibiotics
5.4. Mechanism of chemical incompatibility of aminoglycosides with beta-lactams
5.5. Recent progress in new aminoglycoside antibiotic discovery
5.6. Conclusions and future prospects
Chapter 6. Macrolide, lincosamide, glycopeptide, and other antibacterial antibiotics
6.1. Introduction
6.2. The ribosome as an antibiotic target
6.3. Ribosome-targeting antibiotics
6.4. Breakthrough ribosome-targeting structures
6.5. Bacterial cell envelope as an antibiotic target
6.6. Cell envelope–targeting antibiotics
6.7. Breakthrough research on cell envelope–targeting antibiotics
Section III. Antimycobacterial agents
Chapter 7. Antitubercular drugs
7.1. Introduction
7.2. Classification of antitubercular drugs
7.3. Drug-resistant tuberculosis
7.4. Recent advancements in antitubercular drug discovery
7.5. Clinical trial status of antitubercular drugs
7.6. Conclusion
Chapter 8. Antileprotic drugs
8.1. Introduction
8.2. Classification of antileprotic drugs
8.3. Recent updates in antileprotic drug discovery
8.4. Clinical trials status of antileprotic drugs
8.5. Conclusion
Section IV. Antifungal agents
Chapter 9. Systemic and topical antifungal drugs
9.1. Introduction
9.2. Antifungal drugs: the evolution
9.3. Systemic antifungal drugs
9.4. Topical antifungal drugs
9.5. Antifungal drug resistance
9.6. Chemistry of antifungal agents
9.7. Conclusions and future prospective
Section V. Antiviral agents
Chapter 10. Antiviral drugs and vaccines
10.1. Introduction
10.2. Antiviral drugs
10.3. Viral vaccines
10.4. Viral adaptation and approaches to overcome
10.5. Outlook and conclusion
Section VI. Antiprotozoal agents
Chapter 11. Antimalarial drugs
11.1. Introduction
11.2. Classical antimalarial drugs
11.3. Recent development in antimalarial agents
11.4. Future directions in antimalarial development
11.5. Approaches for malaria eradication
11.6. Conclusions
Chapter 12. Antiamoebic drugs
12.1. Introduction
12.2. Chemical classifications of antiamoebic drugs
12.3. Drug resistance in amoebiasis
12.4. Newer targets for antiamoebic drug discovery
12.5. Recent progress in antiamoebic drug discovery
12.6. Patents of antiamoebic drugs
12.7. Clinical trials of antiamoebic drugs
12.8. Conclusion
Chapter 13. Drugs for giardiasis, trichomoniasis, and leishmaniasis
13.1. Introduction
13.2. Giardiasis
13.3. Trichomoniasis
13.4. Leishmaniasis
13.5. DNDi: an initiative for discovery of drugs for NTDs
13.6. Vector control programs and vaccine development efforts
13.7. Drug syntheses
13.8. Drug metabolism
13.9. Future directions
Section VII. Anthelmintics
Chapter 14. Vermifuge and vermicide drugs
14.1. Introduction
14.2. Chemical classification and drug profile of anthelmintic drugs
14.3. Recent trends in anthelmintic drug discovery
14.4. Anthelmintic drug leads
14.5. Conclusion
Chapter 15. Synthetic cytotoxic drugs as cancer chemotherapeutic agents
15.1. Introduction
15.2. Classification of the synthetic cytotoxic drugs
15.3. Synthesis of some selected prototypical cytotoxic drugs
15.4. Drug resistance and new chemical classes of cytotoxic drugs
15.5. Tumor targeting approaches for the approved cytotoxic drugs
15.6. Conclusions
Chapter 16. Naturally occurring anticancer drugs
16.1. Introduction
16.2. Chemical classification of natural anticancer drugs
16.3. Total synthesis of some selected natural anticancer drugs
16.4. Resistance to cancer chemotherapy and importance of semisynthetic derivatives
16.5. New antitumor leads from natural sources
16.6. Anticancer natural products in clinical trials
16.7. Conclusions
Chapter 17. Hormones and antihormones in cancer chemotherapy
17.1. Introduction
17.2. Classification of hormones and antihormones used in cancer chemotherapy
17.3. Synthesis of some selected drugs
17.4. New drug discovery approaches for the treatment of hormone-responsive cancers
17.5. Future perspectives and conclusions
Chapter 18. Biologicals and small molecules as target-specific cancer chemotherapeutic agents
18.1. Introduction
18.2. Overview of the elements of the target in targeted cancer therapies
18.3. Classes of targeted cancer therapies
18.4. Synthesis and metabolism of some representative drugs
18.5. Future perspectives
Index

Pratap Chandra Acharya

Dr Pratap Chandra Acharya is presently working as Assistant Professor of Pharmaceutical Chemistry at the Department of Pharmacy, Tripura University (A Central University), Suryamaninagar, Tripura (W) India. He received his PhD in Pharmaceutical Chemistry from Panjab University, Chandigarh and M.Pharm (Pharmaceutical Chemistry) from IIT (BHU), Varanasi, India. He has more than 10 years of teaching and research experience in the field of pharmaceutical chemistry. He has been the member of various learned academic bodies such as IUPAC and APTI and has served as a reviewer to several international journals. His current research work involves various drug discovery projects for the development of anticancer drug candidates especially for colon cancer.

Affiliations and expertise

Assistant Professor, Pharmaceutical Chemistry at the Department of Pharmacy, Tripura University (A Central University), Suryamaninagar, Tripura (W), India

Michio Kurosu

Michio Kurosu has completed his Ph.D. from Osaka University, Japan and postdoctoral studies from Harvard University, Chemistry and Chemical Biology. He is a Professor of Pharmaceutical Science at University of Tennessee Health Science Center (UTHSC), USA. He has been teaching medicinal chemistry courses for pharmacy and Ph. D. students at UTHSC. He has a long-term interest in identifying new drug targets for bacterial infections and cancer chemotherapeutics. His research includes antibacterial and anticancer drug discoveries associated with Gram-negative bacteria, Mycobacterium spp., spore-forming bacteria (e.g. Clostridioides difficile), and solid cancers (e.g., pancreatic, breast, and ovarian cancers). As principal investigator on several NIH- and internally-funded programs, he has studied essential enzymes for growth of Acinetobacter baumannii, Klebsiella pneumoniae, and Mycobacterium tuberculosis, and glycosyl transferases for pancreatic and cervical cancers. He has been serving as editorial board members of several international journals and scientific reviewers of the NIH study sections.

Affiliations and expertise

Professor, Pharmaceutical Science, University of Tennessee Health Science Center (UTHSC), USA

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