Recent Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical Diseases

The World Health Organization (WHO) has reported 14 diseases that are occurring exclusively in tropical areas. Most of these diseases are infectious and mainly affect poor populations. Some of these diseases include malaria, dengue fever, leishmaniasis and Chagas disease. Therefore, an acute need for increasing the arsenal of drugs is required to fight against these neglected diseases for the guaranteed recovery and relief of many patients. This E-book gathers important scientific research performed by scientists worldwide showing the state of the art of Medicinal Chemistry dedicated to the synthesis of compounds that are potentially bioactive against the causative agents of neglected diseases. The contents of this book include chapters on recent advances in synthetic organic compounds for the prevention of Chagas disease, recent advances in the discovery of small organic molecules for the prevention and treatment of dengue fever, leishmaniasis, leprosy, therapeutic arsenal and drug discovery for lymphatic filariasis, therapeutic agents for the treatment of malaria, schistosomiasis and synthetic organic compounds as potential antitubercular drugs. This book is intended for undergraduate and graduate students in institutes, colleges, universities and academies who want to specialize in the field of organic synthesis and medicinal chemistry. This book will also be a valuable resource of information for researchers in this field. Cover Recent Advances in the Synthesis of Organic Compounds to Combat Neglected Tropical Diseases Copyright Dedication Contents Foreword Preface List of Contributors 1. CHAGAS DISEASE. An Overview of Recent Advances in the Search for Synthetic Organic Compounds with Trypanocidal Activity Abstract 1. Introductuin 2. New Synthetic Molecules 2.1. Naphthoquinones 2.2. Nitrofuranes and Nitrothiophenes 2.3. Metal Complexes 2.4. Nitrogen Heterocycles 2.5. Nitrogenated Open Chain Compounds 2.6. Sugars, Phosphorus Compounds, Phenolic Derivatives Acknowledgements Conflict of Interest References 2. DENGUE FEVER. Recent Advances in the Discovery of Small Organic Molecules for the Prevention and Treatment of Dengue Fever Abstract 1. Treatment 2. A Medicinal Chemistry Overview of Dengue 2.1. Viral Serine Protease Inhibitors 2.2. Viral Entry Inhibitors 2.3. Inhibitors of RNA Replication 2.4. Other Relevant Compounds Conclusion Acknowledgements Conflict of Interest References 3. LEISHMANIASIS. An Overview of New Synthetic Antileishmanial Candidates Abstract 1. Introduction 1.1. Current Drugs in Use 2. New Synthetic Compounds as Antileishmanial Candidates 2.1. Azole Derivatives 2.1.1. Triazole Derivatives 2.1.2. Imidazole Derivatives 2.1.3. Pyrazole Derivatives 2.1.4. Thiadiazole Derivatives 2.1.5. Oxadiazole Derivatives 2.2. Pyridinone and Dihydropyridine Derivatives 2.3. Pyrimidine and Pyrimidone Derivatives 2.4. Quinoline and Isoquinoline Derivatives 2.5. Quinazoline and Quinoxaline Derivatives 2.6. Indole Derivatives 2.7. Purine, Pyrazolopyrimidine, Pyrazolopyridine and Thienopyridine Derivativ 2.8. Benzimidazole, Benzothiazole, Benzoxadiazole and Benzoxazole Derivatives 2.9. Acridine Derivatives 2.10. Coumarine and Pyrane Derivatives 2.11. Azepine Derivatives 2.12. Porfirine Derivatives 2.13. Biguanidines, Amidines and Diamidines 2.14. Sulfonamide Derivatives 2.15. Hydrazone and Hydrazide Derivatives 2.16. Chalcone Derivatives 2.17. Quinone Derivatives 2.18. Alkylphosphocholine and Bisphosphonate Derivatives 2.19. Trioxane Artemisinin Derivatives 2.20. Miscellaneous Conclusion Acknowledgements Conflict of Interest References 4. LEPROSY. Chasing Potential Antileprotic Compounds Abstract 1. The Diseare 1.1. The Bacteria 1.1.1. Morphology 1.1.2. Biological Properties 1.1.3. Genomic 1.2. Transmission, Immunology and Classifications 1.3. Natural Immunity and Immunology 1.4. Classifications 1.4.1. Resistance to Leprosy: The Lepromin Test 1.5. Clinical Presentations 1.5.1. Tuberculoid Leprosy (TT) 1.5.2. Lepromatous Leprosy (LL) 1.5.3. Borderline Leprosy 1.6. Reactions 2. Synthetic Studies on Antileprotic Compounds 3. Natural Products Bearing Antileprotic Activity 4. Final Considerations Acknowledgements Conflict of Interest References 5. LYMPHATIC FILARIASIS. Therapeutic Arsenal and Drug Discovery for Lymphatic Filariasis from a Synthetic Point of View Abstract 1. Epidemiology 2. Biology 3. LF as an Eradicable Disease 4. Chemical Aspects of LF Pharmacotherapy 4.1. Macrolides 4.1.1. Avermectins 4.1.2. Moxidectin 4.2. Diethylcarbamazine (DEC) 4.3. Albendazole 4.4. Anti-Wolbachia Antibiotics 4.5. Suramin 4.6. Other Filaricidal Agents 5. Concluding Remarks Acknowledgements Conflict of Interest References 6. MALARIA. Synthesis of Hybrid Molecules and Inhibitors of Falcipain for Use as Therapeutic Agents in Treatment of Malaria Abstract 1. Introduction 2. Synthesis of Hybrid Molecules with a Dual Mode of Action 2.1. Endoperoxide-Quinoline Based Hybrids 2.2. Quinoline-Novel Target Based Hybrid 3. Synthesis of Inhibitors of a Cysteine Protease (Falcipain) 3.1. Peptides 3.2. Peptidomimetics 3.3. Chalcones 3.4. Isoquinolines 3.5. Thiosemicarbazones Acknowledgements Conflict of Interest References 7. SCHISTOSOMIASIS. Recent Progresses in Synthesis and Evaluation of Bioactive Compounds with Molluscicidal Activity - Molluscicidal Activity of Synthetic and Natural Products Abstract 1. Introduction 1.1. Drugs to Control Schistosomiasis 2. Strategies to Combat Schistosomiasis Based Upon Molluscicidal Compounds 2.1. Natural Products 2.2. Synthetic Compounds 3. The Structural Diversity of Bioactive Compounds with Molluscicidal Activity 4. Final Remarks Acknowledgements Conflict of Interest References 8. TUBERCULOSIS. Synthetic Organic Compounds as Potential Antitubercular Drugs: A Review of the Progress Made in the Last Five Years Abstract 1. Introduction 2. Search Strategy 2.1. ANTI-Mycobacterium Tuberculosis Drugs Acknowledgements Conflict of Interest References Subject Index