Vardanyan / Hruby Synthesis of Essential Drugs

1. Auflage 2006
ISBN: 978-0-08-046212-7
Verlag: Elsevier Science & Techn.
Format: EPUB
Kopierschutz: 6 - ePub Watermark

E-Book, Englisch, 635 Seiten

Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind - to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO's Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry.* Provides a brief description of methods of synthesis, activity and implementation of all drug types
* Includes synonyms
* Includes over 2300 references

Research Professor, Department of Chemistry and Biochemistry, University of Arizona

Autoren/Hrsg.

Vardanyan, Ruben

Hruby, Victor

Inhaltsverzeichnis

1;front cover;1
2;copyright;5
3;front matter;8
4;Preface;8
5;table of contents;10
6;body;18
7;General Anesthetics;18
7.1;Inhalation Anesthetics;18
7.2;Noninhalation Anesthetics;21
8;Local Anesthetics;26
8.1;Local Anesthetics of the Aminoether Series;29
8.2;Local Anesthetics of the Aminoamide Series;31
8.3;Topical Anesthetics;34
9;Analgesics;36
9.1;Opioid Analgesics;37
9.1.1;Agonists;38
9.1.2;Mixed agonists/antagonists;50
9.1.3;Opioid antagonists;54
9.2;Nonsteroid Anti-Inflammatory Drugs and Anti-Fever Analgesics;55
9.2.1;Salicylic acid derivatives;56
9.2.2;Pyrazolonees;57
9.2.3;p-Aminophenol derivatives;59
9.2.4;Anthranylic acid derivatives;59
9.2.5;Propionic acid derivatives;61
9.2.6;Acetic acid derivatives;63
9.2.7;Indolyl/indeneacetic acids;64
9.2.8;Oxicames;68
10;Soporific Agents (Hypnotics and Sedative Drugs);74
10.1;Barbiturates;75
10.1.1;Long-acting barbiturates;76
10.1.2;Intermediate-acting barbiturates;77
10.1.3;Short-action barbiturates;78
10.1.4;Ultrashort-action barbiturates;79
10.2;Benzodiazepines;79
10.3;Other Hypnotics and Sedative Drugs;82
11;Anxiolytics (Tranquilizers);86
11.1;Benzodiazepines;86
11.2;Anxiolytic of Nonbenzodiazepine Structures;95
12;Antipsychotics (Neuroleptics);100
12.1;Phenothiazine Derivatives;101
12.2;Thioxanthene Derivatives;105
12.3;Butyrophenone Derivatives;108
12.4;Dihydroindolone Derivatives;110
12.5;Dibenzoxazepine and Dibenzdiazepine Derivatives;111
12.6;Diphenylbutylpiperidine Derivatives;113
12.7;Other Neuroleptics;116
12.8;Lithium Derivatives;116
13;Antidepressants;120
13.1;Tricyclic Antidepressants;121
13.1.1;Tertiary amines—representatives of tricyclic antidepressants;121
13.1.2;Secondary amines—representatives of tricyclic antidepressants;124
13.2;Monoaminooxidase Inhibitors;127
13.3;Second-Generation Antidepressants (Atypical Antidepressants);129
13.4;Amphetamines and Other CNS Stimulators;131
14;Central Nervous System Stimulants;134
14.1;Psychomotor Stimulants;134
14.1.1;Methylxanthines;134
14.1.2;Amphetamines, methylphenidate, and pemoline;135
14.2;Respiratory Stimulants or Analeptics;138
14.3;Appetite Suppressants or Anorectics;140
15;Antiepileptic Drugs;142
15.1;Hydantoin Derivatives;143
15.2;Barbiturates;144
15.3;Succinimides;145
15.4;Valproic Acid;146
15.5;Carbamazepine;146
15.6;Benzodiazepines;147
15.7;Acetazolamide;148
15.8;Oxazolidines;148
16;Antiparkinsonian Drugs;152
16.1;Drugs Affecting the Dopaminergic Systems of the Brain;152
16.2;Anticholinergic Drugs (Central Cholinoblockers);155
17;Adrenergic (Sympathomimetic) Drugs;160
17.1;Direct-Acting Agonists;163
17.1.1;Drugs stimulating ?- and ?-adrenoreceptors;163
17.1.2;Drugs stimulating predominantly ?-adrenoreceptors;165
17.1.3;Drugs stimulating predominantly ?-adrenoreceptors;170
17.1.4;Antiedema sympathomimetics;170
17.2;Indirect-Acting Agonists;172
17.3;Agonists of Mixed Action;172
18;Adrenoblocking Drugs;178
18.1;?-Adrenoblockers;179
18.2;?-Adrenoblockers;184
18.2.1;Long-lasting noncompetitive antagonists;185
18.2.2;Nonselective, reversible competitive adrenoblockers;186
18.2.3;Reversible, competitive ?1-selective adrenoblockers;187
18.2.4;Ergot alkaloids (alkaloids of ergot);188
18.2.5;Selective ?2-adrenoblockers;189
18.3;Adrenergic Neuron Blockers;189
19;Cholinomimetics;196
19.1;Direct-Acting Cholinomimetics;197
19.1.1;Choline esters;197
19.1.2;Natural muscarinic alkaloids;200
19.1.3;Natural nicotinic alkaloids;202
19.2;Indirect-Acting Cholinomimetics;203
19.2.1;Reversible cholinesterase inhibitors;204
19.2.2;Carbamates;204
19.2.3;Quaternary amines;206
19.2.4;Irreversible cholinesterase inhibitors;207
19.2.5;Other organophosphorous cholinesterase inhibitors;208
20;Anticholinergic Drugs;212
20.1;Antimuscarinic Drugs;212
20.1.1;Alkaloids;213
20.1.2;Anticholinergics of the quaternary amine series;215
20.1.3;Antiparkinsonian drugs of the quaternary amine series;219
20.1.4;Antispasmodics of the tertiary series;219
20.1.5;Mydriatics of the tertiary amine series;221
20.2;Ganglioblocking Substances;222
21;Muscle Relaxants;226
21.1;Neuromuscular Junction Blocking Agents;227
21.1.1;Antidepolarizing neuromuscular junction blockers;227
21.1.2;Depolarizing neuromuscular blockers;230
21.2;Direct-Acting Muscle Relaxants;231
21.3;Centrally Acting Muscle Relaxants;232
22;Antihistamine Drugs;236
22.1;H1 Antihistamine Drugs;238
22.1.1;Aminoalkyl esters;239
22.1.2;Ethylenediamines;241
22.1.3;Alkylamines;242
22.1.4;Piperazines;243
22.1.5;Phenothiazines;244
22.1.6;Piperidines;245
22.2;H2 Receptor Antagonists;247
23;Cardiotonic Drugs;254
23.1;Cardiac Glycosides;255
23.2;Other Positive Inotropic Drugs;258
24;Antiarrhythmic Drugs;262
24.1;Group I Drugs;263
24.1.1;Subgroup IA;263
24.1.2;Subgroup IB;265
24.1.3;Subgroup IC;267
24.2;Group II Drugs;268
24.3;Group III Drugs;269
24.4;Group IV Drugs;270
25;Antianginal Drugs;274
25.1;Nitrates and Nitrites;274
25.2;?-Adrenoblockers;276
25.3;Calcium Channel Blockers;278
25.4;Other Drugs;282
26;Hypolipidemic Agents;286
26.1;Bile Acid Sequesters;287
26.2;Drugs that Inhibit Cholesterol Synthesis;289
26.3;Other Drugs;292
27;Diuretics;294
27.1;Osmotic Diuretics;294
27.2;Carbonic Anhydrase Activity Suppressing Diuretics;295
27.3;Thiazide Diuretics;297
27.3.1;Drugs related to thiazide diuretics;301
27.4;Loop Diuretics;303
27.5;Potassium Sparing Diuretics;305
28;Antihypertensive Drugs;312
28.1;Diuretics;313
28.1.1;Thiazide diuretics;314
28.1.2;Thiazide-related drugs;314
28.1.3;Potassium sparing diuretics;314
28.2;?-Adrenoblockers;315
28.3;Centrally Acting Adrenergic Drugs (Sympatholytics);316
28.4;Peripherally Acting Sympatholytics (?-Adrenoblockers);317
28.4.1;Reversible competitive ?1-selective adrenoblockers;318
28.4.2;Adrenergic neuron blockers;318
28.5;Calcium Channel Blockers;320
28.6;Myotropic Hypotensive Drugs;321
28.7;Angiotensin-Converting Enzyme Inhibitors;322
28.8;Calcium Channel Activators;325
29;Drugs for Treating Respiratory System Illnesses;328
29.1;Antiedema, Vasoconstricting Drugs;328
29.2;Anticough and Expectorant Agents;329
29.2.1;Narcotic anticough drugs;329
29.2.2;Non-narcotic anticough drugs;330
29.2.3;Expectorant drugs;330
29.3;Bronchodilators (Broncholytics);331
29.3.1;Methylxanthines;331
29.3.2;Anticholinergic drugs;333
29.3.3;Inhibitors of allergy mediator release;333
29.3.4;Corticosteroids;334
29.3.5;Adrenergic drugs (?2-receptor agonists, sympathomimetics);335
30;Anticoagulants, Antiaggregants, Thrombolytics, and Hemostatics;340
30.1;Anticoagulants;341
30.1.1;Direct-acting coagulants or parenteral anticoagulants;341
30.1.2;Direct-acting coagulants, or enteral anticoagulants;342
30.2;Antiaggregants;345
30.3;Fibrinolytics (Thrombolytics);347
30.4;Hemostatics (Procoagulants);349
30.4.1;Systemic hemostatics;349
30.4.2;Local procoagulants;350
31;Thyroid Hormone and Antithyroid Drugs;354
31.1;Drugs for Treating Hypothyroidism;355
31.2;Drugs for Treating Hyperthyroidism;356
32;Insulin and Synthetic Hypoglycemic Agents;360
32.1;Insulin;360
32.2;Synthetic Hypoglycemic Drugs;361
33;Corticosteroids;366
33.1;Glucocorticoids;367
33.2;Mineralocorticoids;377
34;Female Sex Hormones;382
34.1;Estrogens;382
34.2;Antiestrogens;388
34.3;Progestins;390
35;Male Sex Hormones and Anabolic Steroids;398
35.1;Androgens;398
35.2;Androgen Antagonists;400
35.3;Anabolics;402
36;Antineoplastics;406
36.1;Antimetabolites;407
36.1.1;Folic acid antagonists;407
36.1.2;Purine derivatives;409
36.1.3;Pyrimidine derivatives;410
36.2;Alkylating Agents;412
36.2.1;Nitro-containing mustard derivatives;413
36.2.2;Ethylenimine derivatives;415
36.2.3;Alkyl sulfonates;416
36.2.4;Nitrosoureas;416
36.3;Antibiotics;419
36.3.1;Dactinomycines;419
36.3.2;Bleomycins;419
36.3.3;Anthracyclines;420
36.4;Compounds Isolated from Plants;422
36.4.1;Epipodophyllotoxins;423
36.5;Hormonal Drugs;425
36.5.1;Androgens;425
36.5.2;Estrogens;426
36.5.3;Progestins;426
36.5.4;Corticosteroids;426
36.5.5;Nonhormonal drugs;427
36.6;Other Antineoplastic Drugs;429
37;Immunopharmacological Drugs;436
37.1;Immunostimulants;437
37.2;Immunodepressants;438
37.2.1;Glucocorticoids;438
37.2.2;Cytotoxic drugs;439
38;Antibiotics;442
38.1;Beta-Lactam Antibiotics;444
38.1.1;Penicillins;447
38.1.2;Cephalosporins;458
38.1.3;Penems and carbapenems;480
38.1.4;Monobactams;482
38.2;Macrolide Antibiotics;484
38.3;Tetracyclines;487
38.4;Aminoglycosides;492
38.5;Lincosamides;499
38.6;Chloramphenicol;500
38.7;Other Antibiotics;502
39;Antimicrobial Drugs;516
39.1;Sulfonamide Drugs and Trimethoprim;516
39.1.1;Diaminopyrimidines (trimethoprim, pyrimethamine, and trimethoprim-sulfamethoxazole);526
39.2;Quinolones;530
39.3;Nitrofuranes;536
40;Antimycobacterial Drugs;542
40.1;Antituberculosis Drugs;542
40.1.1;Drugs of the first group;543
40.1.2;Drugs of the second group;546
40.2;Drugs for Treating Leprosy;549
41;Antifungal Drugs;552
41.1;Polyene Antifungal Drugs;553
41.2;Imidazoles (Triazoles);554
41.3;Allylamines;560
41.4;Others;560
42;Antiviral Drugs;566
43;Drugs for Treating Protozoan Infections;576
43.1;Antimalarial Drugs;576
43.1.1;Drugs effective against the erythrocyte stage of plasmodia infection;577
43.1.2;Drugs effective against the hepatic (exoerythrocyte) stage of plasmodia infection;587
43.1.3;Drugs effective against hepatic and erythrocyte forms of plasmodia infection;587
43.2;Drugs for Treating Amebiasis;590
43.3;Drugs for Treating Leishmaniasis;594
43.4;Drugs for Treating Trypanosomiasis;595
43.5;Drugs for Treating Other Protozoan Infections;597
44;Antihelmintic Drugs;600
45;Index;612