Cumulative Chapter Titles Keyword Index

359 -

CUMULATIVE CHAPTER TITLES KEYWORD INDEX

adenylate cyclases, dopamine sensitive, 12, 172 adenylate cyclase, glucagon-sensitive, 6,233 adenylate cyclase, adrenergic SAR, 6 , 227 adenylate cyclases, B -adrenergic, 172 adjuvants, 9 , 244 adrenal steroidogenesis, 2 , 263 8-adrenergic blockers, 107 51; 14,81 affinity labeling, 9, 222 alcohol consumption, drugs and deterrence, 246 alkaloids, 1, 311; 2, 358; k, 322; 5, 323; 6, 274 aminocyclitoi antibiotics, 12, 110 analgesics (analgetic), 1, 40; 2, 33; 2, 36; 4, 37; 5, 31; 34; 7 , 31; 8, 20; 9, 11; 10,1 2 7 g , 23; 12, 20; 13,41; 3, 31; 15,32; 41; 17, 2 1 anestKtics, 1,30; 2, 24; 2, 28; 4, 28; 7 , 39; 8, 29; 10,30 animal models, anxiety, 15,5 1 animal models, memory and learning, 12, 30 anorexigenic agents, 1,51; 2, 44; Z T 4 7 ; 5, 40; 8, 42 antagonists, calcium, 16, 257, 17,7 1 antagonists, GABA, 1 5 , 4 1 , 13,3 1 antagonists, narcotic 7 , 31; 8, 20; 9, 11; 10,12; 11,23 antagonists, non-steroidzl, 1, 191; 3, 184 antagonists, steriodal, 2i3, 2, 208; 2, 207; 4, 199 anthracycline antibiotics, 14,288 antiaging drugs, 9, 214 antiallergy agents, 1, 92; 2, 83; 3, 84; I, 89; 9, 85;S lJ . 80; 11,51; 51;-=, 59717, 51 12, 70; 13,51; antiaGinals, 1,78; 2, 69; 2, 71; 5, 63; 1,69; 8, 63; 2, 67; 12, 39; 17, 7 1 antiaEiety agents, 1, 1; 2, 1; 3, 1; 1; 5, 1; 6 , 1; 7 , 6 ; 8, 1; 9, 1; 10, 2; 2, 13; 10; 13, 21; 14, 22; &, 2 2 7 1 6 , 71; 17; 11 antiarxythmics, 1, 85; 6 , 8 x 8 , 6 3 7 2 , 67; 12, 39 antibacterial agents, synFhetic, 1,118; 2, 112; 3, 105; k, 108; 5, 87; 6 , 108; 17,107 antibibtics, 1, 109; 2, 102, 2, 93; 5, 88; 5, 75; 5, 156; 6, 99; I, 99; 7 , 217; iT 104; 9, 95; 10,109; 11,89; 2, 271; 12,110; 13,103; 14, 103; 15,106 antibiotics, aminocyclitol, 12 , 110 antibiotics, plactam, 12, lm antibiotics, 6-lactam non-classical, 13,149 antibiotics, polyether, 10,246 antibodies, drug carriers and toxicity reversal, 15, 233 antibodies, monoclonal, 16, 243 anticonvulsants, 1, 30; 2, 24; 3, 28; 4, 28; I, 39; 8, 29; 10,30; 1 1, 13; 12, 10;13,2i; g, 22; 1 5 ~ ~ 2 216:; 31; 17, 11 antidepressants, 1, 12; 2, 1 E 3, 14;4, 13; 2, 13; 5, 15; 7,18; 8, 11; 11, 3; 12,l;-s 1; , 14,l;-g1; ,16,1; 17,41 antidzbetics, 1, 164; 2, 176; 3, 156; 5, 164; 6, 192 antifungals, 2 , 1 5 7 ; 2, 145; 5 , 1 3 8 ; 5, 129; 6 , 129; 1,109; 8, 116; 9, 107; 10, i20; 11,101; 2, 113; 15,139; Q, 139 antihyperlipidemics, 15, 162 antihypertensives, 1 , 5 9 ; 2, 48; 3, 53; 5, 47; 2, 49; 6, 52; 7, 59; 8, 52; 9, 57; 11,61; Q, 60; 13,71; 14,61; 15,79; 16,73; 17,6 1 antiiFflammatories, non-steroidal, 1, 224; 2, 217; 2, 215; 5, 207; 5, 225; 6 , 182; L, 208; 5, 214; 9, 193;-g, 172; 13,167; 2,189

g,

A,

a,

g,

A,

g,

G,

ANNUAL REPORTS IN MEDICINALCHEMISTRY-I7

A,

Copyright D 1982 by Academic Press, Inc. All rights of reproduction in any form reserved. ISBN 0-12-040517-2

360 -

CUMULATIVE CHAPTER TITLES KEYWORD INDEX

anti-ischemic agents, 17,71 antimetabolite concept, drug design, 11, 233 antineoplastics, 2, 166; 3, 150; 4, 1%; 5, 144; 7,129; SY 128, 9, 139; 10, 131; 11, i i o ; g , 1 2 0 ; 13,120, 14,132; 15,130; 16,137; 17,163 antioiGsity agGts, 11,200; 15,172 antiparasitics, 1, 136; 1, 150; 2, 131; 2,147; 2, 126; 3, 140; 4, 126; 130; 5, 116; 7, lz5; 8, 141; 9, 115; 10,154; 11,121; 1 2: 140; 14, 122; 15, 120; 16,125; 17,129 antiparkinsonism drugs, 6, 42; 9, 19 antipsychotics, 1, 1; 2,-1; 2, 1; 4, 1; 5, 1; 5, 1; I_, 6; S , 1; 9, 1; 10, 2; 11,3; " ,1; 13,11; 14,12;15,-12; 16,11 antiradiation agents, 1, 324; 2, 330; 2, 327; 5, 346 antithrombotics, 7, 7878, 73; 9, 75; 10, 99; 12, 80; 14, 71; 17,79 antiviral agents, 1, 129; 2, 122; 3, 116; 4, ln;2, 101; 5, 118; 7,119; 128; 13,i39; 15,149; 16,149 8, 150; 9, 128T10, 161; 2, aporpkne chemistry, k, 331 arachidonate lipoxygenase, 16, 213 arachidonic acid cascade, 182; 14,178 arachidonic acid metabolites, 17, 203 arthritis, new agents, 13, 167716, 189; 17,175 asymmetric synthesis, 1 r 282 atherosclerosis, 1,178;2, 187; 2, 172; 5, 178; 5, 180; 5, 150; 1,169; 8, 183 bacterial resistance, 13, 239; 2, 119 bacterial toxins, 12,211 behavior, serotonin, 7, 47 benzodiazepine receptors, 16, 21 biological factors, 10,39r11, 42 biological membranes , 11,2 2 r biopharmaceutics, 1,331; 2, 340; 2, 337; 4, 302; 5, 313; 5, 264; 7,259; 8, 332 biosynthesis, antibiotics, 2, 130 blood enzymes, 1, 233 bone, metabolic disease, 12, 223; 15,228; 17,261 calcium antagonists, 16,%7; 17, 71 cancer immunotherapy, 2, 166; 3, 150; 5, 154; 5, 144; I_, 129; 8, 128; 9, 139; 9, 151; lo, 131;11,iio; g,120; 13,120; 14,132; 15,130; 16, 137; 17,163 cannabinoids, 9, 253 carboxylic acids, metalated, 12, 278 carcinogenicity, chemicals, 12, 234 cardiotonic agents, 16, 93; 13,92 cardiovascular agents710, 61catalysis, intramolecular, 7,279 cell invasion, 14,229 cell metabolism, 1,267 cell metabolism, cyclic AMP, 2, 286 cellular responses, inflammatory, 12, 152 chemotaxis, 15, 224; 2, 139; 17,253 chronopharmacology, 11,251 complement inhibitors, 15, 193 complement system, 228 conformation, nucleoside, biological activity, 5, 272 conformation, pep tide , biological activity , 2,-227 cyclic AMP, 2, 286; 215; 8, 224; 11,291 cyclic GMP, 11,291 cyclic nucleotides, 9, 203; 10,192; 15, 182 cytochrome P-450 monoxygenases, 9, 2 9 0 DDT-type insecticides, 9, 300 diabetes, 9, 182; 11, 170; 13, 159

L z

I,

a,

CUMULATIVE CHAPTER TITLES KEYWORD INDEX

z,

361 -

Diels-Alder reaction, intramolecular, 9, 270 diuretic, 1, 67; 2, 59; 2, 62; 6, 88; 83; 10,71; 2, 71; 2, 61; 15, 105 dopamGe agonists, CNS, 13, 11; 3, 12; 15, 12; 16,11 dopamine agonists, blood f l o w , 16,103 drug abuse, CNS agents, 9, 38 drug allergy, 2, 240 drug carriers, antibodies, 15, 233 drug carriers, liposomes, 14, 250 drug delivery systems, 15,302 drug discovery, natural sources, 17,301 drug disposition, 15, 277 drug metabolism, 3 5, 259; 5, 246; 6, 205; S , 234; 9, 290; 11,190; , 27 ; 12, 201; 13, ig6; 13, 304; 7 1 4 - 188; 319; 17,333 electzsynthesz, 12,309 enantioselectivity, drug metabolism, 13,304 endorphins, 2, 41; 2, 31; 15,32 enzymatic monooxygenation reactions, 15,207 enzymes, blood, 1,233 enzyme inhibitors, 7, 249; 2, 234; 13, 249 enzymes, proteolyticinhibition, 13, 261 fertility control, 10,240; 14,l a free radical pathology, 10,257 GABA, antagonists, 13, 31; 15, 41 gamete biology, fertility control, 10, 240 gastrointestinal agents, 1,99; 2, 91; 4, 56; 5, 68; 8, 93; 10,90; 12, 91 gene therapy, 8, 245 glucocorticosteroids, 2, 179 glycosylation, non-enzymatic, 14, 261 hallucinogens, 1, 12; 2, 11; 3 7 1 4 ; 4, 13; 2, 23; 5, 24 heart disease, ischemic, 15,89; 2,-71 heart failure, 13,92; 16,93 hemorheologic agents, 17,99 herbicides, 17, 311 heterocyclic chemistry, 14,278 hormones, glycoprotein, 12, 211 hormones, non-steroidal, 1, 191; 3, 184 hormones, peptide, 2, 210T1, 194y 8, 204; 10, 202; 2, 158; 16,199 199 hormones, steroid, 1, 213; 2, 208; 7,207; 156host modulation, infKction, 8, 160;-=, 5-hydro~ytryptamine~2, 273;-1, 47 hypersensitivity, delayed, S , 284 hypersensitivity, immediate, 7, 238; 8, 273 hypertension, etiology, 9, 50hypnotics, 1, 30; 2, 24;-2, 28; 4, 28; 7, 39; 29; 10,30; 11,13; 12, lo;-=, 21; 2, 22; g,22 immuncy, cellular mediated, 17,191 immunostimulants, arthritis, 11,138; 14,146 immunosuppressives, arthritis, 2,138 immunotherapy, cancer, 9, 151 4,114 infections, sexually transmitted, 1 inhibitors, complement, 15, 193 inhibitors, connective tissue, 17,175 inhibitors, enzyme, 13, 249 inhibitors, irreversine, 9, 234; 16,289 inhibitors, platelet aggregation, 6, 60 3 : 261 inhibitors, proteolytic enzyme, 1 82 inhibitors, renin-angiotensin, inhibitors, reverse transcription, 8, 251 inhibitors, transition state analogs, 1,249

16,

s,

Lx

362 -

CUMULATIVE CHAPTER TITLES KEYWORD INDEX

inorganic chemistry, medicinal, S, 294 insect control agents, 17,311 insecticides, 9, 300 interferon, 8,150; 12, 211; 16,229; 17,151 interoceptivediscriminative stimuli, animal model of anxiety , 11,5 1 intramolecular catalysis, I , 279 ionophores, monocarboxylic acid, l&,246 iron chelation therapy, 13,219 isotopes, stable, in medicinal chemistry, 12, 319 B-lactam antibiotics, 12, 101 @-lactam antibiotics, non-classical, 13, 149 B-lactam antibiotics, synthesis, 11,271 B-lactamases, 13, 239; 17,119 learning, 3, 2%; 16,51 leukocyte mztility, 17,181 leukotrienes, synthesis structure, 17, 291 180; 12, 191; 13,184; 14, 198; lipid metabolism, 9, 172; 10,182; 15, 162 liposomes, 14,250 lipoxygenase, 16, 213; 17,203 lymphocytes, decyed hypersensitivity, 8, 284 magnetic resonance, drug binding, 11,3il mechanism, drug allergy, 3, 240 mechanisms of antibiotic resistance, 1,217; 13, 239; 17,119 membrane function, 10,317 membrane regulators, 11,210 membranes, active transport, 11, 222 memory, 2, 279; 2, 30; 16,5 1 metabolism, cell, 1,267; 2, 286 metabolism, drug, 2, 227; 4, 259; 5, 246; 6, 205; 8, 234; 2, 290; 11,190; 12, 201; 13,196; 13,304; 14,188 metabxism, lipid, 9, 172; 10, 182; 11,180; 2, 191; 14,198 metabolism, mineral , l2, 22?metal carbonyls, S, 322 metals, disease, 3, 321 monoclonal antibodies, 16, 243 monoxygenases, cytochromrP-450, 9 290 37 muscle relaxants, 1,30; 2, 24, 2; 28; 4, 28; muscular disorders, 12, 260 mutagenicity, 12, 2 3 r mutagens, 12,234 narcotic antagonists, 7, 31; S, 20 9, 11; 10, 12; 11,23; 13,41 natural products, 6, 274; 15,255; 17,301 neoplasia, 8, 160;-10, 142 neuroleptic, 12, 2 4 y neurotensin, 31 neurotransmitters, 5, 270 neurotransmitters, amino acid, 14,42 neurotransmitters, brain receptor, 3, 264; 2, 249 non-enzymatic glycosylation, 14, 26i non-nutritive, sweeteners, 177323 non-steroidal antiinflamato~es, 1, 224; 2, 217; 3, 215; 4, 207; 5, 225; 6, 182; I , 208; 8, 214; 9, 193710, 172; 13,167; 16,189 nucleic acid-drug interactions, 13, 316 nucleic acid, sequencing, 16,2 9 9 nucleic acid, synthesis, 16,299 nucleoside conformation, 5, 272 nucleosides, 1,299; 2, 354; 2, 297; 5, 333 nucleotides, 1,299; 2, 3 0 4 ; 2, 297; 5, 333 nucleotides, cyclic , 9, 203; 10,192;-g, 182

11,

a,

L c

363 -

CUMULATIVE CHAPTER T I T L E S KEYWORD INDEX

obesity, 1,5 1 ; 2, 4 4 ; 3 , 4 7 ; 5, 4 0 ; 8, 4 2 ; 11,200 opioid receptor, 11,3 3 7 1 2 , 2 0 ; 1 3 , 4 1 ; 16,3 1 ; 2, 3 2 ; 16,4 1 ; 17,2 1 1 2 , 20; 1 6 , 41 opioids, endogenous, organocopper reagents, 10, 3 2 7 PAF, platelet activatingTactor, 17,243 parasite biochemistry, 16,269 pathophysiology, plasma membrane, 10, 2 1 3 peptic ulcer, _1, 9 9 ; 8 , 93; 10, 9 0 ; 12, 91; 16,8 3 ; 2 , 91; 4 , 5 6 ;6 , 68; 1 7 , 89 peptiz conformation, 1 3 , 227 peptide hormones, 5, 2 1 0 ; 1 9 4 ; 8 , 2 0 4 ; 2, 2 0 2 ; 11,158 8 , 7 0 4 ; 10,2 0 2 ; 16,199 peptide, hypothalamus, 7 , 1 9 4 ; peptide, neurotensin, 31 peptide, SAR, 5 , 266 peptide, synthesis, 5, 3 0 7 ; 7 , 2 8 9 ; 16,309 peptide, synthetic, 1,2 8 9 , 296 peptide, thyrotropin, 1 7 , 3 1 periodontal disease, l c 228 pharmaceutics, 1, 3 3 1 r 2 , 3 4 0 ; 2, 3 3 7 ; 4 , 3 0 2 ; 5, 3 1 3 ; 5, 2 5 4 ; 5, 2 6 4 ; 7 , 2 5 9 ; 8, 7 3 2 3 , 2 2 7 ; 3 , 3 3 7 ; 6,2 5 9 ; A, 302; 5, 2 4 6 ; 5, 3 1 3 ; 6 , 2 0 5 ; pharm&okinetics, 8 , 2 3 4 ; 2, 290; 11, 195; 12, 2 0 1 ; 13,1 9 6 ; 13,3 0 4 ; 14,1 8 8 ; 309; 1 6 , 3 1 9 ; IJ, 333pharmacophore identification, 15,267 pharmacophoric pattern searching, 1 4 , 299 physicochemical parameters, drug dexgn, 3 , 3 4 8 ; 4, 3 1 4 ; 5, 285 pituitary hormones, 7 , 1 9 4 ; 8, 2 0 4 ; 10,202 plasma membrane pathophysiology, 10,213 platelet activating factor (PAF), 17,, 2 4 3 platelet aggregation, 5, 6 0 polyether antibiotics, 10, 246 polyamine metabolism, l c 253 polymeric reagents, 11s-281 prodrug approach, druFdesign, 10,306 prolactin secretion, 1 5 , 202 prostacyclin, 2, 178prostaglandins, 5 , 170; 6, 1 3 7 ; 7, 1 5 7 ; 8, 1 7 2 ; 9, 1 6 2 prostaglandins, S%, 3, 2 9 0 ; 11,80 protein growth factors, 17,219 proteinases, arthritis, 14,219 psoriasis, 1 2 , 1 6 2 psychiatric disorders , 11, 42 psychoses, biological factors, 10,39 psychotomimetic agents, 9 , 27 pulmonary agents, 1 , 92;-2, 8 3 ; 2, 8 4 ; 4, 6 7 ; 5, 5 5 ; 7, 8 9 ; 9, 8 5 ; 10,8 0 ; 11, 5 1 ; g, 7 0 7 1 3 , 5 i ; 14,51; g, 5 9 ; 17,51 2 4 5 ; 8 , 3 1 3 ; 11,3 0 1 ; 13,2 9 2 ; 17,2 8 1 quantitative SAR, radioimmunoassays, 10,284radioisotope labeled drugs, 7, 296 receptor binding, 12, 249 receptor mapping, 1 4 , 2 9 9 ; 15,267 receptors, adrenergz, 15,217 receptors, 6-adrenergic blockers, 3, 81 receptors, benzodiazepine, 1 6 , 2 1 receptors, cell surface, 12,211 receptors, drug, 1, 2 3 6 ; 2, 2 2 7 ; 8, 262 receptors, histamize, 1 4 , 9 1 receptors, neurotransmitters, 3 , 2 6 4 ; 1 2 , 249 receptors, opioid, 11, 3 3 ; g , - 2 0 ; 13,41; 14,3 1 ; 15,3 2 ; 16,4 1 ; 17,2 1 recombinant DNA, 1 7 , 2 2 9

I,

17,

z,

14,

a,

364 -

CUMULATIVE CHAPTER T I T L E S KEYWORD INDEX

renal blood flow, 16,103 renin-angiotensin system, 13, 82 reproduction, 1, 205; 2, 1%; 2, 200; 4, 189 reverse transcryption, 8, 251 rheumatoid arthritis, 17, 138; 3, 219 SAR, adrenergic, 6, 2 2 F SAR, non-classical-$ -lactams, 17, 291 SAR, peptides, 5, 266 SAR, prostaglandins, l l , 80 SAR, quantitative, 5, 245; 8, 313; 11, 301; 13,292; 17, 291 sedative-hypnotics, 1,39; - 29; 13; 12, 10; 13,21; l4, 22; 15, 22; 16, 31; 17, 11 sedatGes, 1730; 2, 24; 3, 28; 5, 28; 1,39; 8, 29; 10,30; 2,13; 12, 10;-13, 21; 3, 2T; 15, 22 serotzin, beEvior, 2, 273;7, 47 serum lipoproteins, re&lation, 13,184 sexually-transmitted infections, 3, 114 silicon, in biology medicine, 10, 265 skeletal muscle relaxants, 8, 37 slow-reacting substances, 17, 69; l6, 213; 17, 203; 17, 291 solute active transport, li-; 222 somatostatin, 14, 209 SRS, 15,69; 16, 213; 17, 203; 17, 291 2, 20872, 207; 4, 199 steroid hormones, 1, 213; steroidogenesis, adFenal, 2, 263 steroids, 2, 312, 2, 307; 4, 281; 2, 296; 5, 192; 6, 162; 1,182; 8, 194; 11, 197 stimuKnts, 1, 12; 2, 11; 3, 14; 4, 13; 2, 13; 6, 15; 1,18; 8, 11 substance P, 17, 271 substituent constants, 2, 347 suicide enzyme inhibitors, 16, 289 superoxide dismutases, 10, 257 superoxide radical, 10,257 sweeteners, non-nutrizve, 17, 323 synthesis, asymmetric, 13, 282 synthesis, computer-assized, 12,288; 16, 281 thrombosis, 5, 237 thromboxanes, 14, 178 thyrotropin, 1 T 31 toxicity reverzl, 15,233 toxicology, comparative, 11, 242 toxins, bacterial, 3, 21itranscription, reverse, 8, 251 vasoconstrictors, 4, 77 vasodilators, 4, 77 vasodilators, cerebral, 12, 49 veterinary drugs, 16,1 6 1 viruses, 14,238 vitamin D, 10, 295; 15, 288; 12,261 waking functions, x i 2 1 water, structured, 5, 256 xenobiotics, 15,182

r,

Lc