An Introduction to Medicinal Chemistry

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58 Drug action at receptors neurotransmitter. The binding forces must be strong enough to bind the neurotransmitter effectively such that the receptor changes shape. However, the binding forces cannot be too strong, or else the neurotransmitter would not be able to leave and the receptor would not be able to return to its original shape. Therefore, it is reasonable to assume that
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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
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 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 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
Page 99 and 100: Structure-activity relationships
Page 101 and 102: Synthetic analogues
Page 109: Receptor theories 97 NH 2 Me BOND R
Page 114 and 115: 102 Drug development Frequently,
Page 116 and 117: 104 Drug development O IIS—NH —
Page 118 and 119: 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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