Fundamentals of Medicinal Chemistry

design for specific purposes, 197

improving absorption, 197

improving patients acceptance, 198

improving transport through membranes,

197

minimising side effects, 200

prontosil, 51, 195

site specific, 198–200

slow release, 198

tripartate prodrug, 196

Progesterone, 203, 204

Prokaryotes, 131, 132, 245

Proline, 2, 212

Propranolol, 169, 185

Prostaglandins, 141, 258

Prostaglandins synthase, 141

Prostanoic acid, 258

Prosthetic groups, 6

Proteins, 4 –10

analysis, 9

anti-parallelb-pleated sheet, 8, 9

conformations, 6

conjugated, 6

C-terminal group, 5, 7

examples of the biological functions of, 4

fibrous, 8

globular, 8

glycoproteins, 6

haemoproteins, 6

a-helix, 8, 9

hydrogen bonding, 9

lipoproteins, 6

N-terminal group, 5, 7

order of structure, 8

parallelb-pleated sheet, 8, 9

peptide link, 4, 5

polypeptides, 5

primary structure, 7, 8

salt bridges, 8, 10

S-S bridges, 6, 7

secondary structure, 8–9

simple, 5

structure (general), 4 –6

tertiary structure, 8

triple helix, 8, 9

water solubility, 9

Proflavine, 151

5-(Propnyl)uracil, 154

Protofibril, 9

Prunasin, 16

Pseudocholinesterases, 189

Pyranose, 11, 15

Pyrantel embonate, 63

2-(2-Pyridyl)ethylamine

Pyrrole, 108

Quantitative structure-activity relationship

(QSAR), 40, 42, 78–91

Charton’s steric parameter, 84

Craig plots, 88

electronic effects, 78, 81–83

Hammettsconstants, 78, 82–83, 84, 88

Hansch analysis, 85–88

Hansch equations, 86, 87

inductive constants, 83

lipophilicity, 78, 79–81,

lipophilicity substituent constant, 79, 80–81,

88

molar refractivity, 84–85

partition constants, 78, 79, 172

physicolchemical parameters, 78

regression constant, 81, 87, 253

steric effects, 83–85

standard deviation, 81, 87, 253–254

Swain and Lupton constants, 83

TaftMssteric constants, 78, 83

Taft steric parameter, 84

Verloop’s steric parameter, 84

quinine, 43, 151

Ranitidine, 40, 41, 168

Receptors, 41, 131, 132, 145, 147, 242, 247–249

b-adrenergic, 144

allosteric site, 146

domain, 247

down regulation, 38

drugs that target, 144 –147

histamine, 144

ligands, 247

secondary messengers, 247

signal transduction, 247

superfamilies, 247, 248

Regression analysis, (seeQuantative structure-

activity relationships)

Resolution, 206, 207

Resting potentials, 246

Reverse transcriptases, 155, 156

5-(b-D-Ribofuranosyl)uracil, 16

Ribbonstructures, 99

Ribonuclease A, 10

INDEX 283