An Introduction to Medicinal Chemistry

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142 Quantitative structure-activity relationships (QSAR) activity is related to only one such property, a simple equation can be drawn up. However, the biological activity of most drugs is related to a combination of physicochemical properties. In such cases, simple equations involving only one parameter are relevant only if the other parameters are kept constant. In reality, this is not easy to achieve and equations which relate biological activity to more than one parameter are more common. These equations are known as Hansch equations and they usually relate biological activity
log [I] The Craig plot 143
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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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Page 106 and 107: 94 Drug development avoiding patent
Page 108 and 109: 96 Drug development ,OH OH GLIPINE
Page 111: Receptor theories
Page 115 and 116: Lead compounds
Page 117 and 118: A case study—oxamniquine
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Page 121 and 122: A case study—oxamniquine 109 CH 3
Page 124 and 125: 112 Pharmacodynamics stream. Thirdl
Page 127 and 128: Drug dose levels 115 can easily neg
Page 129 and 130: Drug design for pharmacokinetic pro
Page 131 and 132: Drug design
Page 139: grown Neurotransmitters as drugs? 1
Page 142 and 143: 130 Quantitative structure-activity
Page 164: 152 Quantitative structure-activity
Page 170 and 171: 158 Antibacterial agents
Page 173 and 174: others. Antibacterial agents which
Page 175 and 176: Antibacterial agents which act agai
Page 177 and 178: Antibacterial agents which
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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Antibacterial agents which inhibit
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Antibacterial agents which
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Antibacterial agents which
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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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