Bioactive heterocyclic compound classes [2] Pharmaceuticals

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Datensatz im Suchindex

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adam_text IMAGE 1 CONTENTS PREFACE XI LIST OF CONTRIBUTORS XIII INTRODUCTION 1 1 THE SIGNIFICANCE O F HETEROCYDES FOR PHARMACEUTICALS AND AGROCHEMICALS 3 CLEMENS LAMBERTH AND JIIRGEN DINGES 1.1 INTRODUCTION 3 1.2 HETEROCYCLES AS FRAMEWORK OF BIOLOGICALLY ACTIVE COMPOUNDS 4 1.3 FINE-TUNING THE PHYSICOCHEMICAL PROPERTIES WITH HETEROCYCLES 6 1.4 HETEROCYCLES AS PRODRUGS 6 1.5 HETEROCYCLES AS PEPTIDOMIMETICS 7 1.6 HETEROCYCLES AS ISOSTERIC REPLACEMENT O F FUNCTIONAL GROUPS 8 1.7 HETEROCYCLES AS ISOSTERIC REPLACEMENT O F ALICYCLIC RINGS 11 1.8 HETEROCYCLES AS ISOSTERIC REPLACEMENT OF OTHER HETEROCYCLIC RINGS 13 REFERENCES 16 PART I NEUROLOGICAL DISORDERS 21 2 TROPANE-BASED ALKALOIDS AS MUSCARINIC ANTAGONISTS FOR THE TREATMENT OF ASTHMA, OBSTRUCTIVE PULMONARY DISEASE, AND MOTION SICKNESS 23 MICHAEL L. SCHULTE AND CRAIG W. LINDSLEY 2.1 INTRODUCTION 23 2.2 HISTORY 23 2.3 SYNTHESIS 25 2.4 MODE OF ACTION 29 2.5 STRUCTURE-ACTIVITY RELATIONSHIPS 32 REFERENCES 34 HTTP://D-NB.INFO/1020848324 IMAGE 2 VI | CONTENTS 3 MORPHINONE-BASED OPIOID RECEPTOR AGONIST ANALGESICS 37 STEPHANIE M. NG 3.1 INTRODUCTION 37 3.2 HISTORY 37 3.3 SYNTHESIS 40 3.4 MODE O F ACTION 43 3.5 STRUCTURE-ACTIVITY RELATIONSHIP 44 REFERENCES 48 4 BARBITURIC ACID-BASED CABA(A) RECEPTOR MODULATORS FOR THE TREATMENT O F SLEEP DISORDER AND EPILEPSY AND AS ANESTHETICS 51 INGO JANSER AND ROMY JANSER 4.1 INTRODUCTION 51 4.2 HISTORY 52 4.2.1 BARBITURATES IN THE TREATMENT O F SLEEP DISORDERS 55 4.2.2 BARBITURATES IN THE TREATMENT O F EPILEPSY 55 4.2.3 BARBITURATES AS ANESTHETICS 56 4.3 SYNTHESIS 57 4.4 MODE O F ACTION 60 4.5 STRUCTURE-ACTIVITY RELATIONSHIP 62 4.5.1 5,5-DISUBSTITUTION 62 4.5.2 SUBSTITUTION AT THE NITROGENS 63 REFERENCES 63 5 PHENOTHIAZINE-BASED DOPAMINE D 2 ANTAGONISTS FOR THE TREATMENT O F SCHIZOPHRENIA 65 CRISTIANA A. ZAHARIA 5.1 INTRODUCTION 65 5.2 HISTORY 65 5.3 SYNTHESIS 70 5.4 MODE OF ACTION 72 5.5 STRUCTURE-ACTIVITY RELATIONSHIPS 76 REFERENCES 77 6 ARYLPIPERAZINE-BASED 5-HT-|A RECEPTOR PARTIAL AGONISTS AND 5-HT2A ANTAGONISTS FOR THE TREATMENT O F AUTISM, DEPRESSION, ANXIETY, PSYCHOSIS, AND SCHIZOPHRENIA 81 IRINI AKRITOPOULOU-ZANZE 6.1 INTRODUCTION 81 6.2 HISTORY 81 6.3 SYNTHESIS 85 6.4 MODE O F ACTION 88 6.5 STRUCTURE-ACTIVITY RELATIONSHIP 89 REFERENCES 96 IMAGE 3 CONTENTS VIL 7 ARYLPIPERIDINE-BASED DOPAMINE D 2 ANTAGONISTS/5-HTJ^ ANTAGONISTS FOR THE TREATMENT O F AUTISM, DEPRESSION, SCHIZOPHRENIA, AND BIPOLAR DISORDER 99 YING WANG 7.1 INTRODUCTION 99 7.2 HISTORY 99 7.3 SYNTHESIS 106 7.4 MODE O F ACTION 109 7.5 STRUCTURE-ACTIVITY RELATIONSHIP 111 REFERENCES 113 8 DIBENZAZEPINE-BASED SODIUM CHANNEL BLOCKERS FOR THE TREATMENT O F NEUROPATHIC PAIN 115 DEREK W. NELSON 8.1 INTRODUCTION 115 8.2 HISTORY 115 8.3 SYNTHESIS 119 8.4 MODE O F ACTION 124 8.5 STRUCTURE-ACTIVITY RELATIONSHIPS 128 REFERENCES 130 PART II CARDIOVASCULAR DISEASES 135 9 DIHYDROPYRIDINE-BASED CALCIUM CHANNEL BLOCKERS FOR THE TREATMENT OF ANGINA PECTORIS AND HYPERTENSION 137 MILAN BRUNCKO 9.1 INTRODUCTION 137 9.2 HISTORY 139 9.3 SYNTHESIS 141 9.4 MODE OF ACTION 144 9.5 STRUCTURE-ACTIVITY RELATIONSHIP 148 REFERENCES 149 10 TETRAZOLE-BASED ANGIOTENSIN II TYPE 1 (AT N ) ANTAGONISTS FOR THE TREATMENT OF HEART FAILURE AND CONGESTIVE HYPERTENSION 153 EDWARD C. LAWSON, BRIAN C. SHOOK, AND JAMES C. LANTER 10.1 INTRODUCTION 153 10.2 HISTORY 154 10.3 SYNTHESIS 157 10.4 MODE O F ACTION 159 10.5 STRUCTURE-ACTIVITY RELATIONSHIP 161 REFERENCES 163 IMAGE 4 V I I I I CONTENTS 11 THIAZIDE-BASED DIURETICS FOR THE TREATMENT O F HYPERTENSION AND GENITOURINARY DISORDERS 169 JIIRGEN DINGES 11.1 INTRODUCTION 169 11.2 HISTORY 169 11.3 SYNTHESIS 174 11.4 MODE O F ACTION 177 11.5 STRUCTURE-ACTIVITY RELATIONSHIP 179 REFERENCES 180 12 TETRAHYDROPYRANONE-BASED HMG-COA REDUCTASE INHIBITORS FOR THE TREATMENT O F ARTERIAL HYPERCHOLESTEROLEMIA 183 HONGYU ZHAO 12.1 INTRODUCTION 183 12.2 HISTORY 183 12.3 SYNTHESIS 188 12.4 MODE O F ACTION 191 12.5 STRUCTURE-ACTIVITY RELATIONSHIP 192 12.5.1 THE HYDROPHILIC DIHYDROXYPENTANOIC ACID PORTION 192 12.5.2 THE SAR O F NATURAL STATINS 192 12.5.3 SAR O F SYNTHETIC STATINS 195 12.5.4 LIVER-SELECTIVE HMGCOA INHIBITORS 197 12.5.5 X-RAY CRYSTAL STRUCTURES 197 REFERENCES 198 PART III INFECTIOUS DISEASES 201 13 ADENINE-BASED REVERSE TRANSCRIPTASE INHIBITORS AS ANTI-HIV AGENTS 203 ALASTAIR DONALD 13.1 INTRODUCTION 203 13.2 HISTORY 203 13.3 SYNTHESIS 209 13.4 MODE O F ACTION 212 13.5 STRUCTURE-ACTIVITY RELATIONSHIP 212 REFERENCES 214 14 GUANINE-BASED NUCLEOSIDE ANALOGS AS ANTIVIRAL AGENTS 217 MAURIZIO FRANZINI 14.1 INTRODUCTION 217 14.2 HISTORY 219 14.3 SYNTHESIS 221 14.4 MODE O F ACTION 227 14.5 STRUCTURE-ACTIVITY RELATIONSHIP 229 REFERENCES 232 IMAGE 5 CONTENTS IIX 15 PENICILLIN AND CEPHALOSPORIN ANTIBIOTICS 237 MICHAEL Z. HOEMANN 15.1 INTRODUCTION 237 15.2 HISTORY 237 15.3 SYNTHESIS 239 15.3.1 TOTAL SYNTHESES 239 15.3.2 CORE MODIFICATIONS 243 15.4 MODE OF ACTION 248 15.5 STRUCTURE-ACTIVITY RELATIONSHIPS 250 REFERENCES 251 PART IV ONCOLOGY 255 16 PYRIMIDINE-BASED KINASE INHIBITORS IN CANCER CHEMOTHERAPY 257 ROBERT MAH 16.1 INTRODUCTION 257 16.2 HISTORY 257 16.3 SYNTHESIS 261 16.4 MODE O F ACTION 264 16.5 STRUCTURE-ACTIVITY RELATIONSHIP 266 REFERENCES 269 17 BENZYL TRIAZOLE-BASED AROMATASE INHIBITORS FOR THE TREATMENT O F BREAST CANCER 275 DAWN GEORGE AND STACY VAN EPPS 17.1 INTRODUCTION 275 17.2 HISTORY 275 17.3 SYNTHESIS 277 17.4 MODE O F ACTION 281 17.5 STRUCTURE-ACTIVITY RELATIONSHIP 282 REFERENCES 286 PARTV INFLAMMATION AND GASTROINTESTINAL DISEASES 289 18 ACETONIDE-BASED GLUCOCORTICOIDS FOR THE TREATMENT O F ASTHMA, SKIN INFLAMMATION, AND DISEASES O F THE EYE 291 KEVIN P. CUSACK, VIKRAM G. KALTHOD, RAJARATHNAM E. REDDY, AND SANJAY R. CHEMBURKAR 18.1 INTRODUCTION 291 18.2 HISTORY 293 18.3 SYNTHESIS 297 18.4 MODE O F ACTION 304 18.4.1 ASTHMA 306 18.4.2 SKIN INFLAMMATION 307 18.4.3 EYE DISEASE 307 IMAGE 6 X | CONTENTS 18.5 STRUCTURE-ACTIVITY RELATIONSHIP 308 REFERENCES 311 19 BENZIMIDAZOLE-BASED H + /K + -ATPASE INHIBITORS FOR THE TREATMENT O F GASTROESOPHAGEAL REFLUX DISEASE 313 STEVE SWANN 19.1 INTRODUCTION 313 19.2 HISTORY 313 19.3 SYNTHESIS 316 19.4 MODE O F ACTION 319 19.5 STRUCTURE-ACTIVITY RELATIONSHIPS 320 REFERENCES 324 PART VI METABOLIC DISEASES 327 20 THIAZOLIDINEDIONE-BASED INSULIN SENSITIZERS:PPAR-Y AGONISTS FOR THE TREATMENT O F TYPE 2 DIABETES 329 STEVEN RICHARDS 20.1 INTRODUCTION 329 20.2 HISTORY 329 20.3 SYNTHESIS 337 20.4 MODE O F ACTION 343 20.5 STRUCTURE-ACTIVITY RELATIONSHIP 344 REFERENCES 345 INDEX 349
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spellingShingle Bioactive heterocyclic compound classes
title Bioactive heterocyclic compound classes
title_auth Bioactive heterocyclic compound classes
title_exact_search Bioactive heterocyclic compound classes
title_full Bioactive heterocyclic compound classes [2] Pharmaceuticals ed. by Clemens Lamberth and Jürgen Dinges
title_fullStr Bioactive heterocyclic compound classes [2] Pharmaceuticals ed. by Clemens Lamberth and Jürgen Dinges
title_full_unstemmed Bioactive heterocyclic compound classes [2] Pharmaceuticals ed. by Clemens Lamberth and Jürgen Dinges
title_short Bioactive heterocyclic compound classes
title_sort bioactive heterocyclic compound classes pharmaceuticals
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