Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990

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adam_text INTERNATIONAL UNION OF PURE AND APPLIED CHEMISTRY TRENDS IN MEDICINAL CHEMISTRY 90 PROCEEDINGS OF THE XLTH INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY, HELD IN JERUSALEM, ISRAEL, 2-7 SEPTEMBER 1990 EDITED BY SHALOM SAREL DEPARTMENT OF PHARMACEUTICAL CHEMISTRY HEBREW UNIVERSITY SCHOOL OF PHARMACY JERUSALEM, ISRAEL RAPHAEL MECHOULAM DEPARTMENT OF NATURAL PRODUCTS HEBREW UNIVERSITY SCHOOL OF PHARMACY JERUSALEM, ISRAEL ISRAEL AGRANAT DEPARTMENT OF ORGANIC CHEMISTRY THE HEBREW UNIVERSITY OF JERUSALEM JERUSALEM, ISRAEL OXFORD BLACKWELL SCIENTIFIC PUBLICATIONS LONDON EDINBURGH BOSTON MELBOURNE PARIS BERLIN VIENNA CONTENTS PREFACE,X PLENARY LECTURES DESIGNING DRUGS FOR HISTAMINE RECEPTORS, 1 C. R. GANELLIN, T. H. BROWN, D. G. COOPER, G. J. DURANT, R. J. IFE, R. C. MITCHELL, G. S. SACH & R. C. YOUNG CHEMICAL CONVERSION OF VITAMIN D3 TO ITS 1,25-DIHYDROXY METABOLITE, 11 J. KIEGIEL, P. M. WOVKULICH & M. R. USKOKOVIC NMDA RECEPTORS: AGONISTS AND COMPETITIVE ANTAGONISTS, 17 J. C. WATKINS PROTEIN TYROSINE KINASE BLOCKERS (TYRPHOSTINS) AS NOVEL ANTIPROLIFERATIVE DRUGS, 31 A. LEVITZKI NEW METHODS OF DRUG TARGETING, 35 N. BODOR RECENT ADVANCES IN THE FIELD OF MYCOTOXINS, 45 ^ C. TAMM MAIN LECTURES RATIONAL DRUG DESIGN COMPUTER-ASSISTED STRATEGIES STRATEGIES IN COMPUTER-ASSISTED DRUG DESIGN, 51 N. C. COHEN SEMIEMPIRICAL QUANTUM-MECHANICAL APPROACH MODELING OF INHIBITORS FOR HIV-1 PROTEINASE, 65 A. RAYAN, A. FLIESS, M. KOTLER, M. CHOREV & A. GOLDBLUM CHEMICAL STRATEGIES THE PREDICTION OF DRUG-MACROMOLECULE INTERACTIONS, 75 J. L. MARTIN, K. VELURAJA, L. N. JOHNSON, G. W. J. FLEET, N. RAMSDEN, I. BRUCE, N. OIKONOMAKOS, A. PAPAGEORGIOU & D. D. LEONIDAS REACTION-PATH KNOWLEDGE AS A BASIS FOR DESIGN AND SYNTHESIS OF NOVEL PROTEASE INHIBITORS, 79 H. DUTLER, S. A. BIZZOZERO, P. ZBINDEN & B. A. PABSCH CONTENTS PEPTIDE SURROGATES * CHEMISTS TOOLS FOR RECEPTOR MAPPING; THE DESIGN AND ENANTIOSELECTIVE SYNTHESIS OF PHE-ILLE SURROGATES, 87 S. SHATZMILLER, B. Z. DOLITHZKY, A. ABIRI & P. N. CONFALONE DRUGS AFFECTING THE CNS AGONIST/ANTAGONIST RESPONSES TO RECEPTORS OF SEROTONIN, DOPAMINE AND TO THE MUSCARINE SITE OF ACETYLCHOLINE NOVEL APPROACHES TO DRUGS ACTING ON 5-HTJ-LIKE RECEPTORS, 97 M. P. SEILER, J. R. FOZARD, P. FLOERSHEIM, A. HAGENBACH, D. HOYER, H. KALKMAN, A. K. MIR, P. SCHOEFFTER, H. SIEGL & A. STOLL IMIDAZOLYLMETHYL TETRAHYDROCARBAZOLONES AND INDOLYL PROPANONES AS 5-HT 3 ANTAGONISTS, 107 R. BARRETT, D. CAVALLA, I. H. COATES, C. ELDRED, G. B. EWAN, N. GODFREY, D. C. HUMBER, P. C. NORTH & A. W. OXFORD 8-OH DPAT-DERIVED 5-HT 1A -RECEPTOR AGONISTS AND ANTAGONISTS, 113 U. HACKSELL, C. MELL1N, S. E. HILLVER, L. BJORK, L. J. CORNFIELD, D. L. NELSON & T. LEWANDER A NOVEL SERIES OF POTENTIAL ANTIDEPRESSANTS AND SELECTIVE 5-HT UPTAKE INHIBITORS, 121 M. PROTIVA, J. JILEK, K. SINDELAR, M. VALCHAR & J. METYSOVA SUBSTITUTED SALICYLAMIDES AND BENZAMIDES; A VERSATILE POOL OF DOPAMINE D 2 RECEPTOR ANTAGONISTS, 127 T. HOGBERG NOVEL AMINOPYRIDAZINE-DERIVED SELECTIVE MUSCARINIC AGONISTS AS POTENTIAL DRUGS FOR SENILE DEMENTIA, 135 C. G. WERMUTH, J. J. BOURGUIGNON & R. HOFFMANN AGONIST/ANTAGONIST RESPONSES TO RECEPTORS OF EXCITATORY AMINO ACIDS THE DEVELOPMENT OF NMDA RECEPTOR ANTAGONISTS AS USEFUL THERAPEUTIC AGENTS, 145 D. M. ZIMMERMAN, P. L. ORNSTEIN, D. D. SCHOEPP & J. D. LEANDER DESIGN, SYNTHESIS AND MOLECULAR MODELING OF PHOSPHONOALKYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AS COMPETITIVE NMDA ANTAGONISTS, 153 C. F. BIGGE, C. HUMBLET, G. JOHNSON, T. MALONE, D. F. ORTWINE & G. W. PINTER EXCITATORY AMINO ACID ANTAGONISTS, 161 T. HONORE, L. N^ERUM, F. E. NIELSEN & P. JACOBSEN NON-COMPETITIVE A/-METHYL-D-ASPARTATE ANTAGONISTS; STRUCTURE-ACTIVITY RELATIONSHIPS FOR COMPOUNDS ACTING AT THE ION CHANNEL AND GLYCINE SITES, 169 P. D. LEESON, R. W. CARLING, B. J. WILLIAMS, R. BAKER, T. LADDUWAHETTY, K. W. MOORE, M. ROWLEY, A. C. FOSTER, J. A. KEMP & M. D. TRICKLEBANK DESIGN, SYNTHESIS AND EXCITATORY ACTIVITY OF CONFORMATIONALLY RESTRICTED L-GLUTAMATE ANALOGUES IN THE MAMMALIAN CENTRAL NERVOUS SYSTEM, 175 Y. OHFUNE & K. SHIMAMOTO CONTENTS SYNTHESIS AND SOME PHARMACOLOGICAL PROPERTIES OF ODAP ANALOGUES, 183 L. B. PIOTROVSKY, M. A. DUMP1S, A. P. GARYAEV & Y. V. ZAITZEV DRUGS AFFECTING THE ADENYLATE CYCLASE AND THE INOSITOL TRIPHOSPHATE- DIACYLGLYCEROL SYSTEMS CANNABINOID RECEPTOR LIGANDS, 193 A. C. HOWLETT INHIBITOR DESIGN FOR INOSITOL MONOPHOSPHATASE, 199 R. BAKER, J. J. KULAGOWSKI, P. D. LEESON & N. J. LIVERTON AGONIST/ANTAGONIST RESPONSES TO EICOSANOID RECEPTORS LEUKOTRIENE METABOLISM, 209 J. ROKACH & E. G. SPOKAS THROMBOXANE BIOSYNTHESIS AND INHIBITION IN MAN, 215 P. PATRIGNANI & C. PATRONO THE SEARCH FOR PEPTIDOLEUKOTRIENE ANTAGONISTS, 219 A. VON SPRECHER, A. SALLMANN, A. BECK, W. BREITENSTEIN, H. WIESTNER, S. KIMMEL, W. H. ANDERSON, G. P. ANDERSON, N. SUBRAMANIAN & M. A. BRAY DRUGS ASSOCIATED WITH BRADYKININ AND PLATELET ACTIVATING FACTOR NOVEL HIGHLY POTENT BRADYKININ ANTAGONISTS AND THEIR IMPACT ON ALLERGIC DISEASES, 229 S. HENKE, A. ANAGNOSTOPOULOS, G. BREIPOHL, H. GERHARDS, J. KNOLLE, B. SCHOLKENS & F. LEMBECK PAF ANTAGONISTS IN THE HETRAZEPINOIC SERIES, 233 K. H. WEBER, F. BIRKE & H. KOPPEN DRUGS TARGETED AT THE CARDIOVASCULAR SYSTEM CHEMICAL APPROACHES TO THE TREATMENT OF ATHEROSCLEROSIS, 243 D. T. WITIAK, D. R. FELLER & H. A. I. NEWMAN SPECIFIC BRADYCARDIC AGENTS * A NOVEL APPROACH TO THE TREATMENT OF MYOCARDIAL ISCHEMIA, 257 B. WETZEL PROGRESS IN THE SYNTHESIS AND DESIGN OF RENIN INHIBITORS, 265 Q. BRANCA, J. P. CLOZEL, W. FISCHLI, W. NEIDHART, H. STADLER & W. WOSTL STRUCTURE ACTIVITY STUDIES AND RECEPTOR BINDING MODEL OF L-BENZAZEPIN-2-ONE CALCIUM ANTAGONISTS, 271 S. D. KIMBALL, D. M. FLOYD, J. C. BARRISH, J. DAS, J. T. HUNT, J. KRAPCHO, G. ROVNYAK, K. J. DUFF, M. LAGO, V. G. LEE, R. V. MOQUIN, S. SPERGEL, J. Z. GOUGOUTAS, M. MALLEY, A. PUDZIANOWSKI, S. F. FLAIM, S. MORELAND, A. HEDBERG & R. E. WHITE CONTENTS SYNTHESIS OF CARDIOACTIVE STEROIDS, 277 P. WELZEL, B. JANSSEN, H. STEIN, T. MILKOWA, H. W. HOPPE, U. WERNER, U. MOLLER, B. STAMMEN, D. BOTTGER, A. PONTY, M. KAISER, P. WAGNER & D. MULLER NOVEL POTASSIUM CHANNEL OPENERS, 285 J. SOMBROEK, R. BERGMANN, R. GERICKE & 1. LUES DRUGS ASSOCIATED WITH BONE FORMATION AND METABOLISM METABOLIC BONE DISEASE; CURRENT THERAPIES AND FUTURE PROSPECTS WITH BISPHOSPHONATES AND OTHER AGENTS, 293 F. H. EBETINO & R. G. G. RUSSELL NOVEL VITAMIN D ANALOGUES IN THE CALCIPOTRIOL (MC 903) SERIES: SYNTHESIS AND EFFECT OF SIDE CHAIN STRUCTURE ON THE SELECTIVE BIOLOGICAL ACTIONS, 299 M. J. CALVERLEY AN EFFICIENT, NON-PHOTOCHEMICAL SYNTHETIC APPROACH TO VITAMIN D METABOLITES AND ANALOGUES, 307 J. STERLING, D. BARASCH, E. SLOVIN, D. HIRSCH, D. LEONOV, A. SCHWARTZ & B. WEINER AGENTS AGAINST INFECTIOUS DISEASES AND CANCER DESIGN AND SYNTHESIS OF NOVEL DNA-GYRASE INHIBITORS, 315 C. HUBSCHWERLEN, P. PFLIEGER & I. KOMPIS HYPERICIN, A POTENTIAL ANTI-AIDS DRUG, 321 D. LAVIE, D. FREEMAN, H. BOCK, J. FLEISCHER, K. VAN KRANENBERG, Y. ITTAH, Y. MAZUR, G. LAVIE, L. LIEBES & D. MERUELO AS-101 [AMMONIUM TRICHLORO(DIOXOETHYLENE-O,O -)TELLURATE] A NEW IMMUNOMODULATOR FOR USE IN TREATMENT OF MALIGNANCIES AND AIDS, 329 M. ALBECK & B. SREDNI CYTOTOXIC GROUPS LINKED TO SYNTHETIC ESTROGENS, 333 K. KROHN, K. KULIKOWSKI, H. MULLER, M. PREISS & G. LECLERCQ MEDICINAL PLANTS FROM CHINA CHINESE TRADITIONAL MEDICINE * A VALUABLE FIELD TO BE EXPLORED, 343 H. LIANG CHEMICAL DRUG DELIVERY SYSTEMS, BIOTRANSFORMATIONS AND PHARMACODYNAMICS DEVELOPMENT OF A LUNG-SELECTIVE BRONCHODILATOR PRODRUG: BAMBUTEROL, 357 L. A. SVENSSON SITE- AND STEREOSPECIFIC DRUG DELIVERY TO THE EYE, 361 A. SIMAY & N. BODOR CONTENTS EVALUATION OF A NOVEL REDOX-BASED ESTROGEN CHEMICAL DELIVERY SYSTEM FOR THE BRAIN, 369 M. H. RAHIMY, N. BODOR & J. W. SIMPKINS PRODRUGS OF VALPROIC ACID, 377 M. BIALER FROM HANSCH TO HILDEBRAND: AN ALTERNATIVE APPROACH TO PHARMACODYNAMICS, 383 S. COHEN TRANSMEMBRANE DRUG TRANSPORT LIPOSOMES IN CANCER CHEMOTHERAPY: EXPERIMENTAL STRATEGIES, 393 Y. BARENHOLZ & A. GABIZON IMPORTANCE OF BIOLOGICAL MEMBRANES IN DRUG ACTION AND DEVELOPMENT, 397 J. K. SEYDEL, H. P. CORDES, M. WIESE, M. KANSY & B. KUNZ SPECIAL TOPICS DISSOCIATION OF PHARMACOLOGICAL EFFECTS IN CHIRAL DRUGS, 405 V. TORTORELLA RECENT ADVANCES IN THE FIELD OF SATIETINS, 411 J. KNOLL NEW RETINOIDS FOR THE TREATMENT OF DISORDERS OF EPIDERMAL DIFFERENTIATION, 419 B. SHROOT, J. EUSTACHE, J. M. BERNARDON & W. R. PILGRIM INDEX, 425 ;
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spellingShingle Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990
Chemistry, Pharmaceutical Congresses
Drug Design Congresses
Drug Therapy Congresses
Drugs Design Congresses
Pharmaceutical chemistry Congresses
Pharmazeutische Chemie (DE-588)4132158-3 gnd
Pharmakologie (DE-588)4045687-0 gnd
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(DE-588)4045687-0
(DE-588)1071861417
title Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990
title_auth Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990
title_exact_search Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990
title_full Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990 International Union of Pure and Applied Chemistry. Ed. by Shalom Sarel ...
title_fullStr Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990 International Union of Pure and Applied Chemistry. Ed. by Shalom Sarel ...
title_full_unstemmed Trends in medicinal chemistry '90 proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990 International Union of Pure and Applied Chemistry. Ed. by Shalom Sarel ...
title_short Trends in medicinal chemistry '90
title_sort trends in medicinal chemistry 90 proceedings of the xith international symposium on medicinal chemistry held in jerusalem israel 2 7 september 1990
title_sub proceedings of the XIth International Symposium on Medicinal Chemistry, held in Jerusalem, Israel, 2 - 7 September 1990
topic Chemistry, Pharmaceutical Congresses
Drug Design Congresses
Drug Therapy Congresses
Drugs Design Congresses
Pharmaceutical chemistry Congresses
Pharmazeutische Chemie (DE-588)4132158-3 gnd
Pharmakologie (DE-588)4045687-0 gnd
topic_facet Chemistry, Pharmaceutical Congresses
Drug Design Congresses
Drug Therapy Congresses
Drugs Design Congresses
Pharmaceutical chemistry Congresses
Pharmazeutische Chemie
Pharmakologie
Konferenzschrift 1990 Jerusalem
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