An Introduction to Medicinal Chemistry

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308 Cimetidine—a rational approach to drug design dipole moment
Famotidine and nizatidine 309 • Replacing the sulfur atom with a methylene unit leads to a drop in activity. • Placing the sulfur next to the ring lowers activity. • Replacing the furan ring with more hydrophobic rings such as phenyl or thiophene reduces activity.
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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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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
Page 270 and 271: 258 The opium analgesics R= ——C
Page 272 and 273: 260 The opium analgesics (A) BINDIN
Page 274 and 275: 262 The opium analgesics morphine.
Page 276 and 277: 264 The opium analgesics o N——C
Page 278 and 279: 266 The opium analgesics morphine
Page 281 and 282: Receptor theory
Page 283 and 284: Receptor theory
Page 285: Agonists
Page 289 and 290: e Receptor mechanisms 277
Page 291 and 292: membrane to a second membrane-bound
Page 296 and 297: 284 Cimetidine—a rational approac
Page 299: Searching
Page 305: From partial agonist
Page 309: Development of metiamide 297 the sa
Page 313: Cimetidine
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Page 326 and 327: Appendix
Page 329: a The action of nerves 317
Page 332 and 333: Appendix
Page 334 and 335: 322 Secondary messengers number
Page 337 and 338: Secondary messengers
Page 339 and 340: Haemophilus influenzae Bacteroides
Page 341 and 342: Glossary
Page 343: Index acetylcholine 47-8, 207, 209-
Page 346 and 347: 334 Index intestinal infections
Page 348: 336 Index structure-activity analys
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An Introduction to Medicinal Chemistry

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