Antimalarial Agents - 1st Edition - ISBN: 9780126889505, 9780323151689

Antimalarial Agents

1st Edition

Chemistry and Pharmacology

Authors: Poul Thompson
eBook ISBN: 9780323151689
Imprint: Academic Press
Published Date: 1st January 1972
Page Count: 408
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Description

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.

Table of Contents


Preface

1 Introduction

Text

References

2 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

References

3 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

References

4 Uses of Drugs in Dealing with Malaria

1. Objectives

2. Methods and Regimens of Drug Administration

References

5 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

References

6 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

References

7 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

References

8 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

References

9 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

References

10 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

References

11 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

References

12 Pyrimidines

1. Introduction

2. Structure-Activity Relationships

3. Synthesis

4. Mode of Action

5. Methods of Estimation

6. Metabolic Disposition

References

13 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

References

14 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

References

15 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

References

16 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

References

17 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

References

18 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

References

19 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

References

Author Index

Subject Index

Details

No. of pages:
408
Language:
English
Copyright:
© Academic Press 1972
Published:
Imprint:
Academic Press
eBook ISBN:
9780323151689

About the Author

Poul Thompson