Medicinal Chemistry-III (eBook)

Front Cover 
1 
Medicinal Chemistry—III 4
Copyright page 5
Table of Contents 6
OPENING REMARKS 8
CHAPTER 1. THE MECHANISMS OF SELECTIVITY AND ACTION 
10 
ABSTRACT 10
THE MECHANISM OF PROTEIN SYNTHESIS 10
SELECTIVITY OF PROTEIN SYNTHESIS INHIBITORS 13
RIBOSOME SUBUNITS AS SPECIFIC TARGETS OF ANTIBIOTIC ACTION 15
INHIBITORS OF THE INITIATION PHASE 16
INHIBITORS OF THE ELONGATION CYCLE 19
REFERENCES 25
CHAPTER 2. THE SIGNIFICANCE OF D-ALANYL-D-ALANINE TERMINI IN THE BIOSYNTHESIS OF BACTERIAL CELL WALLS AND THE ACTION OF PENICILLIN, VANCOMYCIN AND RISTOCETIN 26
ABSTRACT 26
INTRODUCTION 26
PENICILLIN 28
VANCOMYCIN AND RISTOCETIN 29
COMPETITION FOR VANCOMYCIN BINDING SITES 34
CONCLUSION 34
REFERENCES 35
CHAPTER 3. INHIBITORS OF THE TRANSCRIBING ENZYMES 38
ABSTRACT 38
INTRODUCTION 38
TRANSCRIPTASE (DNA-DEPENDENT RNA POLYMERASE): STRUCTURE AND FUNCTION 41
SPECIFIC INHIBITORS OF TRANSCRIPTASE 43
STRUCTURAL MODIFICATIONS OF THE RIFAMYCINS ANDTHEIR EFFECT ON ANTIBACTERIAL ACTIVITY 50
ACTIVITY OF RIFAMYCINS ON VIRAL TRANSCRIPTASES 58
ACKNOWLEDGMENT 63
REFERENCES 63
CHAPTER 4. ANALOGUES OF CYCLIC AMP AND THEIR 
66 
ABSTRACT 66
THE SECOND MESSENGER MODEL 67
THE cAMP-SYSTEM 70
cAMP-ANALOGUES 72
GLYCOGENOLYSIS 77
STEROIDOGENESIS 80
LIPOLYSIS 83
SECRETION OF PITUITARY HORMONES 86
EFFECTS OF cAMP-ANALOGUES ON CONTRACTILE TISSUES 88
PHARMACOLOGICAL ASPECTS 91
REFERENCES 91
CHAPTER 5. PRINCIPLES OF NEUROCHEMISTRY AND DRUG SCREENING PROCEDURES IN 
94 
ABSTRACT 94
INTRODUCTION 94
THE CONCEPT OF POSTSYNAPTIC RECEPTOR IN DRUG DEVELOPMENT 96
REFERENCES 115
CHAPTER 6. ACTIVE POLYPEPTIDES OF THE AMPHIBIAN SKIN 
118 
ABSTRACT 118
INTRODUCTION 118
PHYSALAEMIN-LIKE PEPTIDES 119
BRADYKININ-LIKE PEPTIDES 125
CAERULEIN-LIKE PEPTIDES 126
BOMBESIN-LIKE PEPTIDES 137
MISCELLANEOUS POLYPEPTIDES 144
DISCUSSION 145
ACKNOWLEDGEMENTS 146
REFERENCES 146
CHAPTER 7. SOME BIOLOGICAL APPLICATIONS OF REGULAR 
150 
ABSTRACT 150
INTRODUCTION 150
HISTORICAL FOUNDATIONS 151
MODELS FOR THE ANALYSIS OF BIOLOGICAL ACTIVITIES 154
FORMULATION IN TERMS OF REGULAR SOLUTION THEORY 154
APPLICATION TO STUDIES OF ERYTHROCYTE HAEMOLYSIS 157
CONCLUSIONS 162
REFERENCES 162
CHAPTER 8. THE PREDICTION OF MOLECULAR CONFORMATION AS A BIOLOGICALLY 
164 
ABSTRACT 164
INTRODUCTION 164
EVALUATION OF CONFORMATION 165
MOLECULAR ORBITAL PREDICTION OF CONFORMATION 166
MUSCARINIC AGENTS 167
NICOTINIC AGENTS 168
HISTAMINE 168
SEROTONIN 169
PREGNANE STEROIDS 169
ADRENERGIC AGENTS 170
DOPAMINE 172
CENTRAL INHIBITORY TRANSMITTERS 172
PROSTAGLANDIN 172
PEPTIDE HORMONES 173
SWEET TASTE PHARMACOPHORE 173
CONCLUSION 174
REFERENCES 174
CONCLUDING REMARKS 176