Medicinal Chemistry, Volume 12: Antimalarial Agents: Chemistry and Pharmacology presents the essentials of both biology and chemistry pertinent to the chemotherapy of malaria. This book discusses the nature of the disease, the physiology and biochemistry of the plasmodia, and the mode of action of drugs. Organized into 19 chapters, this volume begins with an overview of the most intensive efforts to develop synthetic antimalarial drugs. This text then examines how drugs are evaluated as well as the specific chemotherapy in malaria. Other chapters consider the diversity of chemical structures exhibiting antimalarial activity with emphasis on structure-activity relationships and methods of synthesis. This book discusses as well the plasmodial effects by quinine in vivo. The final chapter deals with the miscellaneous structures known to have activity against some types of plasmodial infection in animals. This book is a valuable resource for chemists and biologists involved in the development of antimalarial drugs.
Sprache
Verlagsort
Verlagsgruppe
Elsevier Science & Techn.
ISBN-13
978-0-323-15168-9 (9780323151689)
Schweitzer Klassifikation
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.
