An Introduction to Medicinal Chemistry

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198 Antibacterial agents L-LEU — L-DAB / \ D-PHE L-DAB L-DAB L-DAB L-DAB L-THR POLYMYXIN B L-DAB C=0 I (CH 2) 4 CH-CH 3 Fig. 10.69 Polypeptide antibiotic. CH 2 CH 3 such as nucleosides from the cell. The drug is injected intramuscularly and is useful against Pseudomonas strains which are resistant to other antibacterial agents. 10.7 Antibacterial agents which impair protein synthesis Examples of such agents are the rifamycins which act against RNA, and the aminoglycosides, tetracyclines, and chloramphenicol which all act against the ribosomes. Selective toxicity
Antibacterial agents which impair protein synthesis
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An Introduction to Medicinal Chemis
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Preface This text is aimed at under
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Contents Classification of drugs xi
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Contents
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Contents xi 11.16.2 Structure
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Classification of drugs
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1 • Drugs and the medicinal chemi
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Whilst penicillin Drugs and the med
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Drugs
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10 The why and the wherefore Cytopl
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Where do drugs work? 13 Amphoterici
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16 Protein structure [ H O
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The tertiary structure of proteins
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The tertiary structure of proteins
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24 Protein structure H-Bond Peptide
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26 Protein structure again that ter
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Substrate binding
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Substrate binding at an active site
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Substrate binding
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R The catalytic role of enzymes Thy
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I NH 2 CHO (OH Condensation R< The
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Nerve Neurotransmitters
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Receptors
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52 Drug action at receptors Induced
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54 Drug action at receptors MESSENG
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56 Drug action at receptors RECEPTO
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60 Drug action at receptors left-ha
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62 Drug action
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64 Drug action
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66 Drug action at receptors D Neuro
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Structure of DNA 69 NH 2 NHo NHo Ad
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Structure
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Drugs acting
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Drugs acting on DNA 75 CH3—N: MEC
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78 Nucleic acids end AMINO «A/* Ba
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Summary 81
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84 Drug development
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86 Drug development | | Potential I
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88 Drug development bonding or not,
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90 Drug development 7.5.1 Variation
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92 Drug development covered
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94 Drug development avoiding patent
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96 Drug development ,OH OH GLIPINE
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Receptor theories
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Lead compounds
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A case study—oxamniquine
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A case study—oxamniquine
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A case study—oxamniquine 109 CH 3
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112 Pharmacodynamics stream. Thirdl
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Drug dose levels 115 can easily neg
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Drug design for pharmacokinetic pro
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Drug design
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grown Neurotransmitters as drugs? 1
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130 Quantitative structure-activity
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Page 160 and 161: 148 Quantitative structure-activity
Page 162 and 163: 150 Quantitative structure-activity
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Page 170 and 171: 158 Antibacterial agents
Page 173 and 174: others. Antibacterial agents which
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Page 179 and 180: Antibacterial agents which inhibit
Page 183: is tolerated Antibacterial agents w
Page 186 and 187: 174 Antibacterial agents The proble
Page 188 and 189: 176 Antibacterial agents Permeabili
Page 190 and 191: 178 Antibacterial agents H0 2C—C
Page 192 and 193: 180 R
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Page 209: Antibacterial agents which
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Page 215 and 216: Drug resistance 203 10.9 Drug resis
Page 217 and 218: 11- The peripheral nervous system
Page 219 and 220: Motor nerves
Page 221 and 222: Actions
Page 223 and 224: The cholinergic system 211 I j V Ac
Page 225: Agonists
Page 229: Agonists at the cholinergic recepto
Page 232 and 233: 220 The peripheral nervous system
Page 235 and 236: Antagonists
Page 237: Structural analogues based Antagoni
Page 240 and 241: 228 The peripheral nervous system I
Page 242 and 243: 230 The peripheral nervous system p
Page 244 and 245: 232 The peripheral nervous system ;
Page 247: Anticholinesterases
Page 250 and 251: 238 The peripheral nervous system r
Page 253 and 254: Anticholinesterase drugs
Page 255 and 256: Anticholinesterase drugs
Page 257: Pralidoxime—an organophosphate an
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248 The opium analgesics Chinese de
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Morphine
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Development of morphine analogues 2
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258 The opium analgesics R= ——C
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260 The opium analgesics (A) BINDIN
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262 The opium analgesics morphine.
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264 The opium analgesics o N——C
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266 The opium analgesics morphine
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Receptor theory
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Receptor theory
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Agonists
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e Receptor mechanisms 277
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membrane to a second membrane-bound
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284 Cimetidine—a rational approac
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Searching
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From partial agonist
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Development of metiamide 297 the sa
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Cimetidine
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304 Cimetidine — a rational appro
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Appendix
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a The action of nerves 317
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Appendix
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322 Secondary messengers number
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Secondary messengers
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Haemophilus influenzae Bacteroides
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Glossary
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Index acetylcholine 47-8, 207, 209-
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334 Index intestinal infections
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336 Index structure-activity analys
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An Introduction to Medicinal Chemistry

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