Antibacterial Agents Chemistry, Mode of Action, Mechanisms of Resistance and Clinical Applications

by Anderson, Rosaleen; Groundwater, Paul W.; Todd, Adam; Worsley, Alan

• ISBN13: 9780470972458
• ISBN10: 0470972459
• Edition: 1st
• Format: Paperback
• Copyright: 2012-07-23
• Publisher: Wiley

Summary

Antibacterial agents act against bacterial infection either by killing the bacterium or by arresting its growth. They do this by targeting bacterial DNA and its associated processes, attacking bacterial metabolic processes including protein synthesis, or interfering with bacterial cell wall synthesis and function. Antibacterial Agents is an essential guide to this important class of chemotherapeutic drugs. Compounds are organised according to their target, which helps the reader understand the mechanism of action of these drugs and how resistance can arise. The book uses an integrated "lab-to-clinic" approach which covers drug discovery, source or synthesis, mode of action, mechanisms of resistance, clinical aspects (including links to current guidelines, significant drug interactions, cautions and contraindications), prodrugs and future improvements. Agents covered include: agents targeting DNA - quinolone, rifamycin, and nitroimidazole antibacterial agents agents targeting metabolic processes - sulfonamide antibacterial agents and trimethoprim agents targeting protein synthesis - aminoglycoside, macrolide and tetracycline antibiotics, chloramphenicol, and oxazolidinones agents targeting cell wall synthesis - β-Lactam and glycopeptide antibiotics, cycloserine, isonaizid, and daptomycin Antibacterial Agents will find a place on the bookshelves of students of pharmacy, pharmacology, pharmaceutical sciences, drug design/discovery, and medicinal chemistry, and as a bench reference for pharmacists and pharmaceutical researchers in academia and industry.

Author Biography

Rosaleen J. Anderson, Sunderland Pharmacy School, University of Sunderland, UK Paul W. Groundwater, Faculty of Pharmacy, University of Sydney, Australia Adam Todd, Sunderland Pharmacy School, University of Sunderland, UK Alan J. Worsley, Department of Pharmacology and Pharmacy, The University of Hong Kong, Hong Kong SAR

Table of Contents

Preface	p. xiii
Introduction to Microorganisms and Antibacterial Chemotherapy	p. 1
Microorganisms	p. 3
Key points	p. 3
Classification	p. 3
Structure	p. 4
Antibacterial targets	p. 6
Bacterial detection and identification	p. 17
Other than its mode of action, what factors determine the antibacterial activity of a drug?	p. 25
Bacterial resistance	p. 27
The 'post-antibiotic age'?	p. 29
References	p. 31
Questions	p. 33
Agents Targeting DNA	p. 35
Quinolone antibacterial agents	p. 37
Key points	p. 37
Discovery	p. 37
Synthesis	p. 39
Bioavailability	p. 41
Mode of action and selectivity	p. 44
Bacterial resistance	p. 45
Clinical applications	p. 47
Adverse drug reactions	p. 50
Drug interactions	p. 55
Recent developments	p. 56
References	p. 60
Rifamycin antibacterial agents	p. 63
Key points	p. 63
Discovery	p. 63
Synthesis	p. 65
Bioavailability	p. 68
Mode of action and selectivity	p. 69
Bacterial resistance	p. 71
Clinical applications	p. 71
Adverse drug reactions	p. 77
Drug interactions	p. 78
Recent developments	p. 81
References	p. 81
Nitroimidazole antibacterial agents	p. 85
Key points	p. 85
Discovery	p. 85
Synthesis	p. 86
Bioavailability	p. 86
Mode of action and selectivity	p. 87
Mechanisms of resistance	p. 89
Clinical applications	p. 90
Adverse drug reactions	p. 94
Drug interactions	p. 95
Recent developments	p. 96
References	p. 97
Questions	p. 101
Agents Targeting Metabolic Processes	p. 103
Sulfonamide antibacterial agents	p. 105
Key points	p. 105
Discovery	p. 105
Synthesis	p. 107
Bioavailability	p. 108
Mode of action and selectivity	p. 111
Bacterial resistance	p. 114
Clinical applications	p. 115
Adverse drug reactions	p. 119
Drug interactions	p. 121
Recent developments	p. 123
References	p. 124
Trimethoprim	p. 127
Key points	p. 127
Discovery	p. 127
Synthesis	p. 128
Bioavailability	p. 130
Mode of action and selectivity	p. 130
Bacterial resistance	p. 136
Clinical applications	p. 136
Adverse drug reactions	p. 138
Drug interactions	p. 138
Recent developments	p. 139
References	p. 140
Questions	p. 145
Agents Targeting Protein Synthesis	p. 147
Aminoglycoside antibiotics	p. 149
Key points	p. 149
Discovery	p. 149
Synthesis	p. 152
Bioavailability	p. 156
Mode of action and selectivity	p. 158
Bacterial resistance	p. 160
Clinical applications	p. 161
Adverse drug reactions	p. 165
Drug interactions	p. 167
Recent developments	p. 168
References	p. 168
Macrolide antibiotics	p. 173
Key points	p. 173
Discovery	p. 173
Synthesis	p. 175
Bioavailability	p. 177
Mode of action and selectivity	p. 180
Bacterial resistance	p. 181
Clinical applications	p. 182
Adverse drug reactions	p. 187
Drug interactions	p. 189
Recent developments	p. 191
References	p. 193
Tetracycline antibiotics	p. 197
Key points	p. 197
Discovery	p. 197
Synthesis	p. 200
Bioavailability	p. 205
Mode of action and selectivity	p. 210
Bacterial resistance	p. 213
Clinical applications	p. 217
Adverse drug reactions	p. 223
Drug interactions	p. 224
Recent developments	p. 224
References	p. 225
Chloramphenicol	p. 231
Key points	p. 231
Discovery	p. 231
Synthesis	p. 231
Bioavailability	p. 232
Mode of action and selectivity	p. 235
Bacterial resistance	p. 235
Clinical applications	p. 236
Adverse drug reactions	p. 239
Drug interactions	p. 239
Recent developments	p. 240
References	p. 241
Oxazolidinones	p. 243
Key points	p. 243
Discovery	p. 243
Synthesis	p. 245
Bioavailability	p. 247
Mode of action and selectivity	p. 248
Bacterial resistance	p. 249
Clinical applications	p. 251
Adverse drug reactions	p. 252
Drug interactions	p. 253
Recent developments	p. 254
References	p. 254
Questions	p. 259
Agents Targeting Cell-Wall Synthesis	p. 261
ß-Lactam antibiotics	p. 263
Key points	p. 263
Discovery	p. 263
Synthesis	p. 272
Bioavailability	p. 277
Mode of action and selectivity	p. 284
Bacterial resistance	p. 285
Clinical applications	p. 290
Adverse drug reactions	p. 296
Drug interactions	p. 298
Recent developments	p. 300
References	p. 301
Glycopeptide antibiotics	p. 305
Key points	p. 305
Discovery	p. 305
Synthesis	p. 306
Bioavailability	p. 307
Mode of action and selectivity	p. 308
Bacterial resistance	p. 309
Clinical applications	p. 313
Adverse drug reactions	p. 314
Drug interactions	p. 316
Recent developments	p. 316
References	p. 317
Cycloserine	p. 319
Key points	p. 319
Discovery	p. 319
Synthesis	p. 320
Bioavailability	p. 320
Mode of action and selectivity	p. 321
Bacterial resistance	p. 323
Clinical applications	p. 323
Adverse drug reactions	p. 325
Drug interactions	p. 325
Recent developments	p. 325
References	p. 325
Isoniazid	p. 327
Key points	p. 327
Discovery	p. 327
Synthesis	p. 328
Bioavailability	p. 329
Mode of action and selectivity	p. 329
Bacterial resistance	p. 330
Clinical applications	p. 331
Adverse drug reactions	p. 333
Drug interactions	p. 334
Recent developments	p. 335
References	p. 335
Daptomycin	p. 339
Key points	p. 339
Discovery	p. 339
Synthesis	p. 340
Bioavailability	p. 341
Mode of action and selectivity	p. 341
Bacterial resistance	p. 343
Clinical applications	p. 343
Adverse drug reactions	p. 344
Draw interactions	p. 345
Recent developments	p. 345
References	p. 346
Questions	p. 349
Index	p. 351
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