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Methods and Principles in Medicinal Chemistry - Mannhold R.

Mannhold R., Kubinyi H., Timmerman H. Methods and Principles in Medicinal Chemistry - Wiley-VCH, 2001. - 155 p.
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molecular lipophilicity potential 10 molecular modelling 138 molecular size 45, 48 molecular surface area 8 absorption 8 bile excretion 8 molecular weight 43 moricizine 118 morphine 91, 95 myeloperoxidase 106 myosin 48
n
napsagatran 131 N-dealkylation 82, 111
Index 147
N-demethylation 82, 84 necrosis 102 nephron 67
neural network 115, 136, 138 nifedipine 53, 54 nitrenium ion 109, 119 nitrofurantoin 37 NMR spectroscopy 137 no-effect doses 100 nomifensine 107 non-linearity 137
non-steroidal anti-inflammatory drugs 80 nucleophilicity 91
o
occupancy theory 25 octanol 5, 8
alternative lipophilicity scales 8 H-bonding 5
model of a biological membrane 5 olanzapine 119 opioid analgesic 95 organic cation transporter 62 ototoxicity 100 oxcarbazepine 104 oxidation 76 oxidative stress 116 oxygen rebound 76
P
P450 enzyme inhibition 138 P450 inhibitor 61 pafenolol 43 PAPS 91
paracellular absorption 38 paracellular pathway 47, 71 paracellular route 64 parallel synthesis 133 paroxetine 92 partition coefficient 2, 9, 10
absence of dissociation or ionization 3 artificial membranes 9 basic drugs 11 calculation 9
chromatographic techniques 9 intrinsic lipophilicity 3 ionic interactions 11 liposomes 9 membrane systems 10 phospholipids 10 shake-flask 9 unilamellar vesicles 10 unionized form 3 passive diffusion 68, 136
peak-to-trough variations 56 peptidic renin inhibitors 8 permeability 136 peroxisome proliferator-activated receptor y 120 PET scanning 28 P-glycoprotein 41, 42, 43, 137 pharmacokinetic modelling 139 pharmacokinetic phase 26 phase II conjugation 90 phenacetin 104 phenol 90, 91, 94 phenolate anion 91 phenytoin 37, 80, 103, 118, 128 pholcodine 55 phospholipid 52, 54 phospholipidosis 102 physiological models 139 physiological time 127 pindolol 51 pirenzepine 30 pKa 136
plasma protein binding 32, 69, 125, 129
polar surface area 45, 136
polyethylene glycol 36
polypharmacology 100
poor absorption 23
poor metabolizers 79
practolol 106
predictive methods 115
pre-systemic metabolism 22
procainamide 109
pro-drug design 43
pro-drug 89
pro-moiety 43
propafenone 79
propranolol 27, 38, 42, 51, 64, 88
protein binding 137
proxicromil 102
proximal tubule 67
pulsed ultrafiltration-mass spectrometry 138
q
QSAR 115, 138
quantitative structure-pharmacokinetic relationships 138
quantitiative structure-metabolism relationships 138
quinone imine 104, 111 r
radical stability 84 Raevsky 40 rash 106
148 Index
reabsorption 68
reactive metabolite 103, 104, 105,
110, 113
real-time SAR 135 receptor occupancy 26, 28, 51 receptor occupation 25 receptor-ligand complex 25 relative metabolic stability 129 remifentanil 89 remoxipride 28 renal clearance 62, 63, 126, 127 renal injury 113 rifabutin 52 rifampicin 52 rifamycin SV 52 rosiglitazone 119 rule-of-five 40
s
salbutamol 30 salmeterol 30 SAM 92
SCH 48461 83, 85 screening sequences 134 secondary amines 84 sensitization period 119 serine esterases 87 side-effects 56, 88, 89 sinusoidal carrier systems 60 skin rash 103 slow offset 29, 30 pharmacodynamic action 30 SM-10888 63, 75 small intestine 38 soft-drug 89 solubility 45, 136
species-specific differences 127, 129 steady state concentration 21 clearance 21 half-life 21
intravenous infusion 21 steady state 24, 26, 33, 88 steroid receptors 29 (S)-warfarin 80 Stevens-Johnson syndrome 112 structure-activity relationships 26 structure-toxicity relationships 115 substrate radical 76 sulphamethoxazole 111 sulphate transferases 91 sulphate 93, 95 sulphonamide 107 sulphotransferases 91, 95 phenol-sulphotransferase 91
sulpiride 28, 49 suprofen 112
t
tacrine 105 talinolol 42 telenzepine 30 tenidap 113 teratogenicity 100, 103 terfenadine 82 tertiary amine 82 thalidomide 100 thioether adducts 109 thiolate anion 93 thiophene ring 112 thiophene S-oxide 112 thiophene 113 thioridazine 28 thiourea 114
thromboxane A2 receptor antagonists 61 thromboxane receptor antagonists 130 thromboxane synthase inhibitors 61 ticlopidine 112 tienilic acid 112, 127 tissue half-life 54 Tmax 56 tocainide 109 tolbutamide 80, 107, 127 topical administration 88 toxicity 99, 101, 102 idiosyncratic 102 metabolism 102 pharmacology 99 physiochemical properties 101 structure 101 toxicogenomics 116 toxicology 118 toxicophore 108, 115 transcellular diffusion 38 transport proteins 41, 67, 69 transport systems 60 transporter proteins 129, 130, 137 transporter 60, 61, 137 canalicular 60 sinusoid 60 triamterene 37 triazole 72 troglitazone 119 tubular carrier systems 62 tubular pH 69
tubular reabsorption 70, 72, 126 tubular secretion 69, 70 turbidimetry 136
Index 149
u
UDP-a-glucuronic acid 90 unbound drug concentration 50 unbound drug 24, 125 GABA uptake inhibitors 6 histamine Hj-receptor antagonists 6 uptake of drugs in the brain 6 urea 42 urine 62, 67
v
variability 124 verapamil 68 vesnarinone 111
volume of distribution 17, 32, 51, 64, 124, 136
apparent free volume 32 extracellular water volume 17 plasma volume 17 tissue affinity 17 total body water volume 17
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