An Introduction to Medicinal Chemistry

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The catalytic role of enzymes 37 Fig. 4.16 6-Mercap<strong>to</strong>purine. an example of an allosteric inhibi<strong>to</strong>r. It inhibits the first enzyme involved in the synthesis of purines and therefore blocks purine synthesis. This in turn blocks DNA synthesis. 4.5 The catalytic role of enzymes We
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 and 44: Substrate binding
Page 45 and 46: Substrate binding at an active site
Page 47: Substrate binding
Page 54 and 55: 42 Drug action
Page 56: 44 Drug action at enzymes met in th
Page 60 and 61: 48 Drug action at receptors CH 2 +
Page 62: 50 Drug action at receptors Fig. 5.
Page 65 and 66: How does the message get received?
Page 67 and 68: process whereby How does a receptor
Page 70: 58 Drug action at receptors neurotr
Page 73 and 74: A thorough understanding The design
Page 75 and 76: Partial agonists 63 RECEPTOR RECEPT
Page 77 and 78: Tolerance and dependence 65 5.9 Des
Page 79: Tolerance and dependence 67 level.
Page 82 and 83: 70 Nucleic acids 6.1.2
Page 84 and 85: 72 Nucleic acids able to coil into
Page 86 and 87: 74 Nucleic acids Fig. 6.9 Proflavin
Page 89 and 90: Ribonucleic acid
Page 91: Ribonucleic acid 79 GROWING PROTEIN
Page 95 and 96: the never-ending quest Structure de
Page 97 and 98: Structure-activity relationships
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Structure-activity relationships
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Synthetic analogues
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Synthetic analogues
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Synthetic analogues
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Synthetic analogues
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Receptor theories 97 NH 2 Me BOND R
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102 Drug development Frequently,
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104 Drug development O IIS—NH —
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Et 2NCH 2CH 2 CH 2NEt 2
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108 Drug development Zero Activity
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110 Drug development found
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Drug distribution and 'survival' 11
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116 Pharmacodynamics Drugs
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118 Pharmacodynamics Other common m
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120 Pharmacodynamics
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122 Pharmacodynamics Me AZATHIOPRIN
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124 Pharmacodynamics Many peptides
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126 Pharmacodynamics 8.3.9 Self-des
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Graphs and equations 129 What are t
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Physicochemical properties
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Meta Hydroxyl Group Physicochemical
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Quantifying steric properties Hansc
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log [I] The Craig plot 143
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The Topliss scheme 145 and electron
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The Topliss scheme 147 with a negat
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Planning
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Case study
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156 Antibacterial agents prontosil
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Antibacterial agents which
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162 Antibacterial agents MeO OMe Fi
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164 Antibacterial agents Fig. 10.15
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166 Antibacterial agents drug would
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168 Antibacterial agents -CH2- R—
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170 Antibacterial agents • Ineffe
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Antibacterial agents which inhibit
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groups Antibacterial agents which i
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186 Antibacterial agents = CH 3 C0
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188 Antibacterial agents Second- an
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192 Antibacterial agents
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194 Antibacterial agents [Normal Me
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196 Antibacterial agents L-Valine M
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198 Antibacterial agents L-LEU —
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200 Antibacterial agents which was
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202 Antibacterial agents o ,CO2H HN
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204 Antibacterial agents transferre
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206 The peripheral nervous system y
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208 The peripheral nervous system S
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210 The peripheral nervous system N
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212 The peripheral nervous system 1
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Agonists at the cholinergic recepto
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Water Design of acetylcholine analo
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Design
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224 The peripheral nervous system H
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A large variety Antagonists of the
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Antagonists
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Antagonists
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drug design Other cholinergic antag
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Anticholinesterases
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Anticholinesterase drugs 239 - Pyrr
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242 The peripheral nervous system M
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244 The peripheral nervous system F
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N—CH 3 MeO. R'O* R
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Morphine 249 12.2 Morphine 12.2.1 S
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Morphine 253 To conclude, the 6-hyd
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Development
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Development of morphine analogues 2
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Development
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Development
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270 The opium analgesics analgesic
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272 The opium analgesics acts as a
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Enkephalins
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278 The opium analgesics narcotic a
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280 The opium analgesics O II N —
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Searching
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Searching for a lead—AT-guanylhis
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Developing the lead—a chelation b
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Development of metiamide 295 meanin
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Development
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Further studies—cimetidine analog
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Famotidine and nizatidine 309 • R
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Appendix
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(vesicles) containing The action of
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The action of nerves 319 x Briv "-
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Secondary messengers
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Secondary messengers 323 the proces
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Appendix 4 • Bacteria and bacteri
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Glossary ADDICTION Addiction can be
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Further reading Albert,
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drug addiction 1, 3, 5, 127, 248, 2
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penillic acids 172 pentagastrin Ind
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An Introduction to Medicinal Chemistry

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