An Introduction to Medicinal Chemistry

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32 Drug action at enzymes Fig.
Substrate binding at an active site 33 unable to accept any more substrate. Therefore, the bonding interactions between substrate and enzyme have to be properly balanced such that they are strong enough to keep
Page 1 and 2: An Introduction to Medicinal Chemis
Page 3 and 4: Preface This text is aimed at under
Page 5 and 6: Contents Classification of drugs xi
Page 7 and 8: Contents
Page 9 and 10: Contents xi 11.16.2 Structure
Page 11 and 12: Classification of drugs
Page 13 and 14: 1 • Drugs and the medicinal chemi
Page 15 and 16: Whilst penicillin Drugs and the med
Page 17: Drugs
Page 22 and 23: 10 The why and the wherefore Cytopl
Page 25: Where do drugs work? 13 Amphoterici
Page 28: 16 Protein structure [ H O
Page 31 and 32: The tertiary structure of proteins
Page 33 and 34: The tertiary structure of proteins
Page 36 and 37: 24 Protein structure H-Bond Peptide
Page 38: 26 Protein structure again that ter
Page 43: Substrate binding
Page 47: Substrate binding
Page 53 and 54: R The catalytic role of enzymes Thy
Page 55 and 56: I NH 2 CHO (OH Condensation R< The
Page 59 and 60: Nerve Neurotransmitters
Page 61 and 62: Receptors
Page 64 and 65: 52 Drug action at receptors Induced
Page 66 and 67: 54 Drug action at receptors MESSENG
Page 68: 56 Drug action at receptors RECEPTO
Page 72 and 73: 60 Drug action at receptors left-ha
Page 74 and 75: 62 Drug action
Page 76 and 77: 64 Drug action
Page 78 and 79: 66 Drug action at receptors D Neuro
Page 81 and 82: Structure of DNA 69 NH 2 NHo NHo Ad
Page 83 and 84: Structure
Page 85 and 86: Drugs acting
Page 87: Drugs acting on DNA 75 CH3—N: MEC
Page 90 and 91: 78 Nucleic acids end AMINO «A/* Ba
Page 93: 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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158 Antibacterial agents
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others. Antibacterial agents which
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Antibacterial agents which act agai
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Antibacterial agents which
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Antibacterial agents which inhibit
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is tolerated Antibacterial agents w
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174 Antibacterial agents The proble
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176 Antibacterial agents Permeabili
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178 Antibacterial agents H0 2C—C
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180 R
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Antibacterial agents which impair p
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Agents which
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Drug resistance 203 10.9 Drug resis
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11- The peripheral nervous system
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Motor nerves
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Actions
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The cholinergic system 211 I j V Ac
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Agonists
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Agonists at the cholinergic recepto
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220 The peripheral nervous system
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Antagonists
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Structural analogues based Antagoni
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228 The peripheral nervous system I
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230 The peripheral nervous system p
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232 The peripheral nervous system ;
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Anticholinesterases
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238 The peripheral nervous system r
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Anticholinesterase drugs
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Anticholinesterase drugs
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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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