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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5648_Библиотеки_им_академика_М_И_Перельмана.pdf
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- •Preface
- •Contents
- •1.1 Introduction
- •1.3 Drug Discovery: A Historical Perspective
- •1.4 Drug Discovery and Development Processes
- •1.5 Modern Approach of Research and Development Strategies
- •Questions
- •2.1 Introduction
- •2.2 Retrosynthetic Analysis: The Concepts
- •1.6 Role of Natural Products in Target Identification
- •1.7 Bioisosterism
- •1.8 Role of Stereochemistry in Drug Discovery
- •2.3 Basic Synthetic Strategies: General Approaches Used for Synthesis Problems
- •2.4 Retrosynthetic Analysis: Other Simplification Rules
- •2.5 Retrosynthetic Analysis: Synthetic Impropriety to Avoid
- •Questions
- •3.1 Introduction
- •3.2 Classification
- •3.3 Mechanism of Action
- •3.4 Analgesic Agents
- •3.5 Anti-Inflammatory Drugs
- •3.6 Opioid Receptor Discovery
- •3.7 Aspirin
- •3.8 Ibuprofen
- •3.9 Paracetamol
- •3.10 Diclofenac
- •Questions
- •4.1 Introduction
- •4.2 Antibacterial Agents
- •4.3 Antifungal Agents
- •4.4 Chloramphenicol
- •4.5 Sulfonamides
- •4.6 Sulfamethoxazole
- •4.7 Sulfacetamide
- •4.8 Trimethoprim
- •Questions
- •5.1 Introduction
- •5.2 Drugs Acting on CNS and Peripheral Nervous System (PNS)
- •5.3 Barbiturates
- •Questions
- •6.1 Introduction
- •6.2 Cardiovascular Drugs
- •6.3 Organic Nitrates
- •Questions
- •7.1 Introduction
- •7.2 The Organism
- •7.3 Drug Testing Systems
- •7.4 Chemotherapy
- •7.5 Classification of Leprosy and the Clinical Symptoms
- •7.6 Leprosy Co-existing Factors
- •7.7 Dapsone
- •7.8 Clofazimine (Lamprene)
- •7.9 Solapsone (Sulphetrone)
- •7.10 Ethionamide (Ethionamidum)
- •7.11 Rifampicin (Rifampin)
- •7.12 Clarithromycin
- •7.13 Minocycline
- •7.14 Other Sulfone Derivatives Active Against Leprosy
- •7.15 Treatment of Leprosy Using Chaulmoogra Oil
- •7.16 WHO Recommended Chemotherapeutic Regimens
- •Questions
- •8.1 Introduction
- •8.2 Structure of Viruses
- •8.3 Life Cycle of Viruses
- •8.4 Antiviral Drug Targets
- •8.5 Antiviral Drugs Acting Against RNA Viruses: HIV
- •8.6 Acquired Immune Deficiency Syndrome (AIDS)
- •Questions
- •9.1 Introduction
- •9.2 Life Cycle of the Malaria Parasite
- •9.3 Antimalarial Drugs
- •9.4 National Drug Policy on Malaria
- •9.5 WHO Guidelines for the Treatment of Malaria
- •Questions
- •10.1 Introduction
- •10.2 Production of Ethyl Alcohol and Citric Acid
- •10.3 Production of Antibiotics
- •10.4 Production of Lysine
- •10.5 Production of Glutamic Acid
- •10.6 Production of Vitamin B2 (Riboflavin)
- •10.7 Microbial Production of Vitamin B12
- •10.8 Production of Vitamin C (Ascorbic Acid)
- •Questions
- •11.1 Medicinal Importance of Haldi or Curcumin (Curcuma longa)
- •11.2 Medicinal Importance of Neem (Azadirachta indica)
- •11.3 Medicinal Value of Vitamin C (Ascorbic acid)
- •11.4 Medicinal Importance of Ranitidine
- •11.5 Medicinal Importance of Ginger (Zingiber officinale)
- •11.6 Medicinal Importance of Tulsi (Ocimum tenuiflorum)
- •11.7 Medicinal Importance of Garlic (Allium sativum)
- •11.8 Medicinal Importance of Ajwain (Trachyspermum ammi)
- •Questions
- •Abbreviations
- •Bibliography
- •Index


Index
4,4,6-Trimethyl-tetrahydro-pyran-2-one,
synthesis of 51
5,5-disubstituted barbiturates 119
5-HT antagonists 144
A
Acetylcholine 22
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syndrome (AIDS) 181, 200
Acquired resistance 86
Acyclovir 188
Adrenoceptor blocking agents 140
Aerobic fermentation 235
Ajwain, medicinal importance of 278
Allium sativum 275
Alternative MDT regimens 179
Anaerobic fermentation 234
Anaesthesia, drugs used in 113
Analgesic agents 61, 110
Aniline 59
Anion antagonists 137
Antianginal agents 138
Antiarrhythmic agents 133
Antibacterial action, mechanisms of 89
Antibacterial agents 87
Antibacterial drugs 89, 90
Antibiotics 85, 86
production of 239
Anticoagulants 145
Anticonvulsants 109
mechanisms of 117
Antidepressant drugs 112
Anti-epileptic drugs 113
Antiepileptic drugs 118
Antifungal agents 89, 93
adverse effects of 93
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Antihyperlipidemic agents 149
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Antihypertensive agents 139
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Anti-leprosy drugs 158
Antimalarial agents 208
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Antimalarial drugs 211
Antimicrobial action 85
Antimicrobial drugs 85
Anti-parkinsonian drugs 110
Antiplatelets 145
Antipsychotic drugs 112
Antipyretic analgesics 59
Antipyretics 57, 63
mechanism of action 60
Antiviral drug targets 185
Artemisinin 220
Arterial and venous dilatators 149
Arterial vasodilators 148
Ascorbic acid 265
Aspirin 68
Aspirin, preparation of 283
Atom mapping 35

394 Index
B
Bacteria 185
Barbiturates 116, 118
Basic synthetic strategies 34
Benzodiazepam derivatives 126
Benzodiazepines 117, 124
Benzoyl glycine, preparation of 289
Bioisosterism 24
Blood schizonticidal agents 211
C
Ca-ion channel blockers 137
Captodiamine, synthesis of 48
Captopril, synthesis of 52
Cardiac glycosides 131
Cardiovascular drugs 130
categories 131
Central nervous system agents 109
Cephalosporin 242
Chaulmoogra oil 177
Chemotherapeutic regimens 178
Chemotherapy 160
Chloramine-T, preparation of 295
Chloramphenicol 94, 244
retrosynthetic analysis approach of 31
Chloromycetin 244
Chloroquine 214
mechanism of resistance 215
Citric acid 236
Clarithromycin 174
Class-I antiarrhythmic drugs 134
Clofazimine (lamprene) 166
Clotrimazole, preparation of 299
CNS stimulants 109, 113
Codeine, metabolism of 67
Convergent synthesis 30
Coronary vasodilators 139
Curcumin (Curcuma longa) 259
D
Dapsone 162
Dermophytic infections 90
Diabetes, types of 153
Diazepam 125
Dichloramine-T, preparation of 297
Diclofenac 80
Diclofenac sodium, preparation of 291
Dicoumarol (dicouman) 146
Diels-Alder reaction 29
Disconnection approach 30
Diuretics 144
DNA viruses 183
Drug development process 18
Drug discovery 1
and development processes 8
historical perspective 5
process 16
revolutions in 3
role of stereochemistry in 25
stages 9
success in 11
Drug testing systems 159
Drug-like properties, detection of 12
Drugs
and developmental programmes 9
generations of 5
E
Ethanol fermentation 236
Ethionamide (ethionamidum) 171
Ethyl alcohol 236
F
Fermentation, types of 233
Fluconazole, synthesis of 47
Fungal cell wall 91
G
Garlic, medicinal importance of 275
General anaesthesia 113
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Ginger
bioactive compounds of 272
medicinal importance of 269

Index 395
Glutamic acid 247
Glyceryl trinitrite 155
Guanine nucleoside 194
H
Haldi, medicinal importance of 259
Heparin 145
HIV 181
life cycle of 198
Hypoglycaemic agents 153
I
Ibuprofen 71
Imidazobenzodiazepines 117
Immobilized cell bioreactors 235
Indanedione 147
Insulin dependent diabetes mellitus 154
Internal resistance 86
K
Nj-subtype of opiate receptors 23
Koji process 238
L
Leprosy
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clinical symptoms 161
co-existing factors 162
treatment of 177
Linear synthesis 30
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Lipinski’s rules 12
Lysine 246
M
Magnesium silicate, preparation of 302
Malaria
drug schedule for treatment of 228
WHO guidelines for treatment of 230
Malaria parasite, life cycle of 209
Metronidazole, preparation of 293
Minocycline 175
Miscellaneous antihyperlipidemic agents 153
Morphine, metabolism of 67
Multibacillary leprosy 178
N
Narcotic analgesics 110
Narcotic opioid analgesics 62
N-arylanthranilic acids 60
Neem, medicinal importance of 261
Non-insulin dependent diabetes mellitus 154
Non-narcotic analgesics 62
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(NSAIDs) 63
chemical classes of 64
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Opioid analgesia, mechanisms of 66
Opioid receptor discovery 64
Opportunistic infections 91
Organic nitrates 154
P
p-aminophenol analogues 59
Paracetamol 76
Paracetamol, preparation of 287
Parkinsonism, drugs used in 110
Paucibacillary leprosy 179
Penicillin 86, 241
Peripheral nervous system (PNS) 115
Peripheral opioid mechanisms 66
Pharmaceutical balance 11
Phenobarbital 120
Primaquine 224
Prontosil 96
Propranolol, synthesis of 49
Prostaglandin, synthesis of 74
Pyrazolodiones 60
Pyrazolones 60
Q
Quantitative structure-activity relationships 21
Quinine 217
Quinoline analogues 59

396 Index
R
Ranitidine, medicinal importance of 268
Renin-angiotensin system, agents acting on 142
Retron 38
Retrosynthetic (antithetic) analysis 30
Retrosynthetic analysis 29, 30, 31
and synthetic planning 32
backward approach 35
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synthetic impropriety to 41
Retrosynthetic approaches 28
Reverse synthetic reaction process 30
Rifampicin (rifampin) 172
RNA viruses 184
antiviral drugs acting against 196
S
Salicyclic acid analogues 59
SAR paradox 21
Sedative-hypnotic drugs 111
6HGDWLYHVDQGK\SQRWLFVFODVVLÀFDWLRQRI
Solapsone (sulphetrone) 169
Solid state fermentation 234, 238
Sorbic acid, preparation of 300
Streptomycin 244
Structure-activity relationships (SARs) 19, 20
Submerged fermentation 234, 238
Sulfacetamide 103
Sulfamethoxazole 102
Sulfonamides 95
Sulfone derivatives active against 176
Sumatriptan
retrosynthesis of 53
synthesis of 53, 54
Surface fermentation 238
Systemic infections 91
T
7DUJHWLGHQWLÀFDWLRQUROHRIQDWXUDO
products in 22
Therapeutic targets 1, 16
molecular approach 17
systems approach 17
Thrombolytics 145
Tissue schizonticidal agents 211
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Transient insomnia 114
Triazolobenzodiazepines 117
Trimethoprim 105
Tulsi, medicinal importance of 273
V
Vasodilators 143, 148
Veber rules 14
Viruses
life cycle of 182
structure of 181
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microbial production of 252
Vitamin C (ascorbic acid) 253
medicinal value of 265
Z
Zidovudine 200
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