Fundamentals of Medicinal Chemistry

Drug action (Continued)

chain cleaving agents, 154–155

distribution, 50, 159

drugs that disrupt cell membranes and walls,

131–131–138

drugs that target nucleic acids, 147–155

drugs that target receptors, 144 –147

elimination, 51, 75, 159, 161, 165, 167, 171,

174, 175, 176, 177

enzymes, 138–144

host cell viral penetration inhibitors, 156

ionophores, 135–136

intercalation, 147, 150, 151–152

metabolism (see alsometabolism), 51, 159,

172

pharmacodynamic phase, 49, 53

pharmacokinetic phase, 49

phenols, 135

nucleic acid synthesis inhibitors, 155

viral protein synthesis inhibition, 157

Drug administration, 46, 47, 167, (see also

Pharmacokinetics)

dosage regimen, 48, 177

dosage form, 46, 172, 178, 235

enteral administration, 47

excipients, 46, 235

extravascular administration, 171

intravascular, 162–171

intravenous infusion, 169–171

IV bolus, 162, 171

IV infusion, 171

loading dose, 177

oral administration, 171

parenteral administration, 48

plateau value, 48

prodrugs, (seeprodrugs)

therapeutic window, 48, 170, 174, 176

Drug development and production,

223–238

chemical development, 224 –229

chemical engineering issues, 225

critical path, 223

formulation, 235

health and safety, 226–227

market authorisation (application), 224, 231,

235

patent protection, (seePatents)

pilot plant, 224, 225

quality control, 235

reaction vessel, 225

regulation, 237–238

toxicological testing, 231

Drug design and discovery, 57

general route, 58

stereochemistry (seeStereochemistry of drug

design)

solubility (seeSolubility and drug design)

Drug synthesis, 203–220

adverse drug reactions, 233

asymmetric synthesis methods, 208–214

asymmetry in synthesis, 204–214

books and databases, 215

case study, 228–231

chiral auxilary, 211, 212

chiral building blocks, 211, 212

convergent routes, 204, 217, 224

design, 203–4, 214–220

disconnection, 205, 214–220

diastereoisomeric, 207, 208

efluent load factor (ELF), 227

enantiomeric excess, 207, 208

functional group interconversions, 216, 217,

220

linear synthesis/routes, 204, 217, 224

non-stereoselective reactions, 205,

206–207

partial routes, 203

quality control, 227–228

Sharpless-Katsuki catalysts, 211

stereoselective reactions, 206, 207

synthetic routes, 220

synthons, 214

telescoping, 228

Dyphylline, 69

Econazole, 133

Elastin, 4

Elimination (seedrug action)

Ellipticine, 150

Enalapril, 212

Enalaprilat analogues, 72

Endogenous species, 1, 57, 145, 147

b-Endorphin, 7

Enzymes, 131, 132, 138–144, 255–257

active site, 256

activation energy, 256

allosteric activation, 257

allosteric control, 257

allosteric site, 257

apoenzymes, 255

278 INDEX