An Introduction to Medicinal Chemistry

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144 Quantitative structure-activity relationships (QSAR) + CT 1.0 NO 2 • CN SOjNHj CH3SO2 3 * - 50 . CH 3CO CONH 2 .25 COjH -2.0 -1.6 -1.2 -- 8 '- 4 CH 3CONH C? Br CF 3 •OCF 3 • .4 .8 1.2 1.6 2.0 + + T 7C • OH OCH 3 . .-.50 t-Butyl NMej -.75 - CT . .-1.0 Fig. 9.16 Craig plot. 9.16
The Topliss scheme 145 and electron withdrawing properties (positive IT and positive a), whereas an OH substituent
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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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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
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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
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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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