Advances in the Medicinal Chemistry of Neglected Tropical Disease and Related Infectious Diseases offers an in-depth overview of recent progress in drug discovery targeting some of the world’s most persistent and under-researched diseases. With a focus on medicinal chemistry and target-based drug design, this book explores critical pharmacological targets and innovative compounds aimed at combating neglected tropical diseases (NTDs) and related infections.Spread across ten chapters, the book examines the current state and future directions of therapeutic research for diseases such as leishmaniasis, Chagas disease, sleeping sickness, malaria, schistosomiasis, dengue, Zika virus, tuberculosis, and fascioliasis. Each chapter provides details about disease-specific targets, structural activity relationships (SAR), and developments in promising lead compounds over the past decade.
Key Features:
- Focuses on pharmacological targets and medicinal chemistry strategies
- Covers both parasitic and viral diseases with global health impact
- Underlines emerging therapeutic approaches and SAR-guided design
- Explains compound screening, optimization, and preclinical research
Table of Contents
Chapter 1 Medicinal Chemistry of Neglected Tropical Diseases (Ntds):- From Targets to Drugs
- Introduction
- Neglected Tropical Diseases: a Constant Threat
- Epidemiology
- Consequences on the Health System
- Pharmacological Intervention and Prevention
- Research in Drug Design and Development Focuses on New Targets
- Some Explored Drug Targets and Pathways
- N-Myristoyltransferase (Nmt)
- Nitroreductases
- Topoisomerases and Dna
- Pyrimidine Synthesis Pathway
- Mitochondrial Alterations
- Conclusion
- Acknowledgments
- References
- Targeting Druggable Pathways and Overcoming Treatment Challenges
- Introduction
- Life Cycle
- Forms of the Disease
- Cutaneous Leishmaniasis (Localized Cutaneous Leishmaniasis)
- Mucocutaneous Leishmaniasis (Mcl)
- Visceral or Kala-Azar (Vl)
- Post Kala-Azar Dermal Leishmaniasis (Pkdl)
- Current Treatment
- Pentavalent Antimonials
- Amphotericin B
- Miltefosine
- Paromomycin
- Pentamidine
- Herbal Antileishmanial Agents
- Flavonoids and Chalcones
- Naphthoquinones and Iridoids
- Saponins
- Quinolines
- Lignans
- Terpenes and Terpenoids
- Synthesized Antileishmanial Agents
- Furans
- Pyrazoles
- Chromenes and Coumarins
- Pyridines
- Indoles
- Quinolines
- Isoquinolines and Oxoisoaporphines
- Quinazolines and Its Derivatives
- Triazine
- Drug Candidates Targeting Metabolic Pathways of Leishmania
- Resistance
- Vaccination
- Concluding Remarks
- References
- Introduction
- T. Cruzi Transmission
- Pathogenesis of Chagas Disease
- Signs and Symptoms
- Cd Associated Cardiomyopathies
- Parasitological Diagnosis
- Pharmacological Treatment of Cd
- Novel Therapeutic Approaches
- Prevention
- Conclusion
- References
- Updates on Medicinal Chemistry and Target Identification
- Introduction
- Current Diagnosis and Treatment Strategies for Hat
- Target-Based Drug Design Strategies for Hat
- Novel Anti-Hat Targets
- Protein Tyrosine Kinases (Ptks)
- Mitogen-Activated Protein Kinases (Mapks)
- Heat Shock Proteins (Hsps)
- Kinetoplastid Proteasome
- Tb Cathepsin L (Tbcatl)
- Tb Udp-Glucose 4’-Epimerase (Tbgale)
- Phosphofructokinase (Pfk)
- Inositol Polyphosphate Multikinase (Ipmk)
- Rna-Editing Ligase (Rel1)
- S-Adenosylmethionine Decarboxylase (Adometdc)
- Conclusion
- References
- Introduction
- The Life Cycle of Schistosoma
- Clinical Manifestations of Human Schistosomiasis
- Acute Schistosomiasis
- Cercarial Dermatitis or Swimmer’S Itch
- Katayama Fever or Syndrome
- Chronic Schistosomiasis
- Current Antischistosomal Drugs
- Praziquantel
- Oxamniquine
- Drug Repurposing and Treatment of Schistosomiasis
- Antimalarial Agents
- Antibiotics
- Anti-Inflammatory Agents
- Anticancer Drugs
- Statins
- Organometallics
- Potential Molecular Targets in Schistosomiasis
- Epigenetic Regulators
- Histone Modifying Enzymes
- Protein Kinases Inhibitors
- Protease Inhibitors
- Cyp450 Inhibitors
- Transporters Inhibitors
- Specific Targets
- Drug Resistance
- Vaccination
- Schistosoma Mansoni 14-Kda Fatty Acid-Binding Protein (Sm14)
- Schistosoma Mansoni 29 Kilodalton Protein Sm29
- Concluding Remarks
- References
- Introduction
- Targets for Dengue
- Ns2B/Ns3 Protease
- Ns5 Protein
- E Protein
- Other Non-Structural Proteins
- Protease
- Rdrp
- Pdb Id: 5F3Z
- Methyltransferase
- Pdb Id: 3P8Z
- 2.4E Protein
- Pdb Id: 1Oan
- Inhibitors Targeting Protease
- Inhibitors Targeting Rdrp
- Inhibitors Targeting Ns5 Methyl Transferase
- Inhibitors Targeting E Protein
- Miscellaneous
- Conclusion
- References
- Introduction
- Chemotherapeutic Targets for Antimalarial Therapy
- The Need for New Target for Anti-Malarial Drugs
- Targets for Malaria Parasite
- Targeting the Processes in the Parasite Membrane
- Targeting Channels/Transporters
- Aquaporin Channel
- Plasmodial Surface Anion Channel
- Hexose Transporter
- Choline Transporter
- Targeting the Apicoplast
- Focusing on Cyclin-Dependent Protein Kinases (Cdks) Found in Parasites
- Targeting Nucleic Acid Metabolism
- The Purine Pathway
- The Pyrimidine Pathway
- Targeting Parasite Transporters
- Targeting the Mitochondrial System
- Targeting the Redox System
- Targeting the Shikimate Pathway
- Targeting Isoprenoid Biosynthesis
- Targeting Parasite Proteases
- Targeting Parasite Membrane Biosynthesis
- Targeting the Pftbp-Pftfiib Interface
- Novel 5-Imidazopyrazole Incorporated Fused Pyrans
- 2-Amidobenzimidazole Derivatives
- Phenoxyaryl-4(1H)-Pyridones
- Sar of Hydroxyferroquine Derivatives
- Novel Indoleamide Derivatives
- Chromano-Chalcones and Chromeno-Chalcones Derivatives
- Structural Activity Relationship of Chromano-Chalcones Derivatives
- Sar of Chromeno-Chalcone’S Antimalarial Activity
- Novel Benzoxaboroles Derivatives
- Curcumins
- 4-Oxo-3-Carboxyl Quinolones
- Β-Carboline Derivative
- Quinazoline-Chalcone Hybrids
- Conclusion
- References
Author
- Igor Jose dos Santos Nascimento
- Ricardo Olimpio de Moura