Over the past 50 years a wide variety of antibacterial substances have been discovered and synthesised, and their use in treating bacterial infection has been spectacularly successful. Today there are several general classes of antibacterial drugs, each having a well established set of uses, and together they form the mainstay of modern antibacterial chemotherapy. In search for new and improved agents, the pharmaceutical researcher needs to be well informed on many topics, including existing agents, their modes of action and pharmacology, and possible synthetic approaches. In this new book the…mehr
Over the past 50 years a wide variety of antibacterial substances have been discovered and synthesised, and their use in treating bacterial infection has been spectacularly successful. Today there are several general classes of antibacterial drugs, each having a well established set of uses, and together they form the mainstay of modern antibacterial chemotherapy. In search for new and improved agents, the pharmaceutical researcher needs to be well informed on many topics, including existing agents, their modes of action and pharmacology, and possible synthetic approaches. In this new book the author has brought together a wide range of information on the principal classes of antibacterial agents, and he covers, for each group, their history, mode of action, key structural features, synthesis and bacterial resistance. The result is a compact and concise overview of these very important classes of antibacterial agents.
1 Introduction.- 1.1 History and overview of anti-infective chemotherapy.- 1.2 Infectious disease outbreaks and plagues.- 1.3 Common bacterial species.- 1.4 Sources of chemotherapeutic antibacterial agents and the impact of organic chemistry.- 1.5 Resistance.- 1.6 Current status and trends in antibacterial chemotherapy.- Further reading.- 2 Sulfa antibacterials and arylpyrimidine antifolates.- 2.1 History and overview.- 2.2 Mode of action: inhibition of bacterial folate metabolism.- 2.3 Structural features and structure-activity relationships of the sulfa antibacterials and arylpyrimidine antifolates.- 2.4 Synthetic approaches to sulfa antibacterials and arylpyrimidine antifolate antibacterial agents.- 2.5 Bacterial resistance to the sulfa antibacterials and arylpyrimidine antifolates.- 2.6 New agents.- 2.7 Summary.- Further reading.- 3 ß-Lactam antibiotics.- 3.1 History and overview.- 3.2 Mode of action: penicillin-binding proteins and inhibition of transpeptidation.- 3.3 Structural features and structure-activity relationships of the ß-lactam antibacterials.- 3.4 Synthesis of ß-lactam antibacterials.- 3.5 Bacterial resistance to the ß-lactam antibacterial agents.- 3.6 Recent advances.- 3.7 Summary.- Further reading.- 4 Tetracycline antibiotics.- 4.1 History and overview.- 4.2 Mode of action: bacterial protein synthesis inhibition.- 4.3 Structural features and structure-activity relationships of the tetracycline antibacterials.- 4.4 Synthetic approaches to tetracycline antibacterial agents.- 4.5 Uptake and bacterial resistance to tetracycline antibacterial agents.- 4.6 Recent advances.- 4.7 Summary.- Further reading.- 5 Aminoglycoside antibiotics.- 5.1 History and overview.- 5.2 Mode of action: bacterial protein synthesis inhibition.- 5.3 Structural features andstructure-activity relationships of the aminoglycoside antibacterials.- 5.4 Synthetic approaches to aminoglycoside antibacterial agents.- 5.5 Bacterial resistance to aminoglycoside antibacterials.- 5.6 Recent advances.- 5.7 Summary.- Further reading.- 6 The non-peptidic macrocyclic antibacterials.- 6.1 History and overview.- 6.2 Mode of action of the non-peptidic antibacterials.- 6.3 Structural features and structure-activity relationships of the macrocyclic antibacterials.- 6.4 Synthetic approaches to the non-peptidic macrocyclic antibacterials.- 6.5 Bacterial resistance to non-peptidic macrocyclic antibacterial agents.- 6.6 Recent advances.- 6.7 Summary.- Further reading.- 7 Quinolone antibacterials.- 7.1 History and overview.- 7.2 Mode of action: bacterial DNA gyrase inhibition.- 7.3 Structural features and structure-activity relationships of quinolone antibacterials.- 7.4 Synthetic approaches to quinolone antibacterial agents.- 7.5 Bacterial resistance to quinolone antibacterials.- 7.6 Recent advances.- 7.7 Summary.- Further reading.- 8 Peptidic antibacterial agents.- 8.1 Introduction.- 8.2 Individual peptidic antibacterial compounds.- 8.3 General comments.- Further reading.- 9 Miscellaneous antibacterial agents.- 9.1 Chloramphenicol.- 9.2 Lincosamides.- 9.3 Nitrofurans and nitroimidazoles.- 9.4 Vancomycin and teicoplanin.- 9.4.1 Mode of action.- 9.5 Isoniazid and other antituberculosis agents.- Further reading.
1 Introduction.- 1.1 History and overview of anti-infective chemotherapy.- 1.2 Infectious disease outbreaks and plagues.- 1.3 Common bacterial species.- 1.4 Sources of chemotherapeutic antibacterial agents and the impact of organic chemistry.- 1.5 Resistance.- 1.6 Current status and trends in antibacterial chemotherapy.- Further reading.- 2 Sulfa antibacterials and arylpyrimidine antifolates.- 2.1 History and overview.- 2.2 Mode of action: inhibition of bacterial folate metabolism.- 2.3 Structural features and structure-activity relationships of the sulfa antibacterials and arylpyrimidine antifolates.- 2.4 Synthetic approaches to sulfa antibacterials and arylpyrimidine antifolate antibacterial agents.- 2.5 Bacterial resistance to the sulfa antibacterials and arylpyrimidine antifolates.- 2.6 New agents.- 2.7 Summary.- Further reading.- 3 ß-Lactam antibiotics.- 3.1 History and overview.- 3.2 Mode of action: penicillin-binding proteins and inhibition of transpeptidation.- 3.3 Structural features and structure-activity relationships of the ß-lactam antibacterials.- 3.4 Synthesis of ß-lactam antibacterials.- 3.5 Bacterial resistance to the ß-lactam antibacterial agents.- 3.6 Recent advances.- 3.7 Summary.- Further reading.- 4 Tetracycline antibiotics.- 4.1 History and overview.- 4.2 Mode of action: bacterial protein synthesis inhibition.- 4.3 Structural features and structure-activity relationships of the tetracycline antibacterials.- 4.4 Synthetic approaches to tetracycline antibacterial agents.- 4.5 Uptake and bacterial resistance to tetracycline antibacterial agents.- 4.6 Recent advances.- 4.7 Summary.- Further reading.- 5 Aminoglycoside antibiotics.- 5.1 History and overview.- 5.2 Mode of action: bacterial protein synthesis inhibition.- 5.3 Structural features andstructure-activity relationships of the aminoglycoside antibacterials.- 5.4 Synthetic approaches to aminoglycoside antibacterial agents.- 5.5 Bacterial resistance to aminoglycoside antibacterials.- 5.6 Recent advances.- 5.7 Summary.- Further reading.- 6 The non-peptidic macrocyclic antibacterials.- 6.1 History and overview.- 6.2 Mode of action of the non-peptidic antibacterials.- 6.3 Structural features and structure-activity relationships of the macrocyclic antibacterials.- 6.4 Synthetic approaches to the non-peptidic macrocyclic antibacterials.- 6.5 Bacterial resistance to non-peptidic macrocyclic antibacterial agents.- 6.6 Recent advances.- 6.7 Summary.- Further reading.- 7 Quinolone antibacterials.- 7.1 History and overview.- 7.2 Mode of action: bacterial DNA gyrase inhibition.- 7.3 Structural features and structure-activity relationships of quinolone antibacterials.- 7.4 Synthetic approaches to quinolone antibacterial agents.- 7.5 Bacterial resistance to quinolone antibacterials.- 7.6 Recent advances.- 7.7 Summary.- Further reading.- 8 Peptidic antibacterial agents.- 8.1 Introduction.- 8.2 Individual peptidic antibacterial compounds.- 8.3 General comments.- Further reading.- 9 Miscellaneous antibacterial agents.- 9.1 Chloramphenicol.- 9.2 Lincosamides.- 9.3 Nitrofurans and nitroimidazoles.- 9.4 Vancomycin and teicoplanin.- 9.4.1 Mode of action.- 9.5 Isoniazid and other antituberculosis agents.- Further reading.
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