Antimalarial Agents

Preface1 Introduction Text References2 Malaria Parasites and Life Cycles with Reference to Chemotherapy 1. Malaria Parasites 2. Life Cycle of Plasmodia 3. Classes of Drugs Based on Life Cycle Stage Affected References3 Biochemistry, Metabolism, and Cultivation of Malaria Parasites A. Biochemistry and Metabolism 1. Inorganic Substances 2. Carbohydrates and Respiration 3. Proteins and Nucleic Acids 4. Lipids B. Cultivation of Malaria Parasites 1. Cultivation of Asexual Blood Forms in Erythrocytes 2. Cultivation of Plasmodia Freed from Erythrocytes 3. Cultivation of Exoerythrocytic Forms and Mosquito Stages of Plasmodia References4 Uses of Drugs in Dealing with Malaria 1. Objectives 2. Methods and Regimens of Drug Administration References5 Drug Resistance in Malaria 1. Introduction 2. Geographic Distribution and General Types of Drug Resistance 3. Relations Among Drugs Based on Tests for Cross Resistance 4. Possible Factors Accounting for Drug Resistance 5. Mechanisms of Resistance References6 Evaluation of Antimalarial Activity 1. Asexual Blood Forms in vitro 2. Exoerythrocytic Forms in vitro 3. Evaluation of Drugs in Experimental Animals 4. General Principles in Chemotherapy and Selection of Test Infections in Animals 5. Primary Tests for Suppressive Activity Against Asexual Blood Forms in Animals 6. Primary Tests for Activity Against Exoerythrocytic Forms in Animals 7. Secondary Tests for Activity Against Asexual Blood Forms in Animals 8. Secondary Tests for Activity Against Exoerythrocytic Forms in Animals 9. Miscellaneous Antimalarial Tests in Animals 10. Preclinical Toxicity and Physiological Disposition Studies in Animals and Evaluation of Antimalarial Drugs in Man References7 Quinine and Related Alkaloids 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Antimalarial Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects of Quinine 8. Antimalarial Activity and Clinical Uses References8 Quinolinemethanols and Related Compounds 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Antimalarial Activity 5. Mode of Action 6. Methods of Estimation 7. Metabolic Disposition 8. Toxicity and Side Effects References9 8-Aminoquinolines 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects of Primaquine 8. Antimalarial Activity and Clinical Uses of Primaquine References10 Acridines 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects of Quinacrine 8. Antimalarial Activity and Clinical Uses of Quinacrine References11 4-Aminoquinolines 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects of Major 4-Aminoquinolines 8. Antimalarial Activity and Clinical Uses of Major 4-Aminoquinolines References12 Pyrimidines 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition References13 Pyrimidines: Pyrimethamine Type 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation of Pyrimethamine and Trimethoprim 6. Metabolic Disposition of Pyrimethamine and Trimethoprim 7. Toxicity and Side Effects of Pyrimethamine and Trimethoprim 8. Antimalarial Activity and Clinical Uses References14 Biguanides 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects 8. Antimalarial Activity and Clinical Uses References15 Dihydrotriazines 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects of Cycloguanil 8. Antimalarial Activity and Clinical Uses of Cycloguanil Pamoate References16 Sulfonamides 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects 8. Antimalarial Activity and Clinical Uses References17 Sulfones 1. Introduction 2. Structure-Activity Relationships 3. Synthesis 4. Mode of Action 5. Methods of Estimation 6. Metabolic Disposition 7. Toxicity and Side Effects 8. Antimalarial Activity and Clinical Uses References18 Other Compounds of Interest 1. Bis(Alkylaminomethyl)Dihydroxynaphthalenes-377C54 2. Endochin 3. Pteridines and Related Structures 4. [2-(Chlorophenyl)Tetrahydro-2-Furyl]Piperidines 5. Tetrahydrohomopteroic Acid 6. 6-Aminoquinolines 7. Antibiotics and Lincomycin Derivatives 8. 5,5-Bis(Benzyl)-2-(Aryl and Heterocyclic)-l,4,5,6-Tetrahydropyrimidines 9. l,4-Bis(Trichloromethyl)Benzene (Hetol) and Related Polyhalogenated Aromatics 10. Febrifugine and Related Structures 11. Naphthoquinones 12. Quinazolines 13. RC-12 and Other Pyrocatechol Amines 14. Substituted 2-(Aminoalkylamino)-4-(Trichloromethyl)-S-Triazines References19 Miscellaneous Structures A. Types Investigated Moderately 1. Organometallic Compounds 2. Amidines 3. 3-Amino-1,2,4-Benzotriazines 4. Dithiocarbamates 5. ?-Dithiosemicarbazones 6. Guanylhydrazones 7. Pentadienamides 8. Pantothenates 9. B-663 Phenazines 10. 3-Piperonylsydnone 11. Quinoline Disulfides 12. Quinoxalines B. Compounds Investigated Briefly 1. Alloxan 2. 1-Aminocyclopentanecarboxylic Acid 3. Aminothiazole Derivatives 4. Colchicine 5. 7,10-Ethano-1-Thia-4,7-Deazaspiro [4,5] Decane 6. Ethylenimines 7. Forbisen 8. Hydrazines 9. 1-Methyl-3-Nitro-1-Nitrosoguanidine 10. Prodigiosin 11. ß-Resorcylic Acid 12. Tropolone Derivatives ReferencesAuthor IndexSubject Index