| Description |
1 online resource : illustrations |
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text txt rdacontent |
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computer c rdamedia |
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online resource cr rdacarrier |
| Series |
Heterocyclic drug discovery series |
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Heterocyclic drug discovery series.
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| Bibliography |
Includes bibliographical references and index. |
| Note |
Online resource; title from PDF title page (EBSCO, viewed June 26, 2017). |
| Summary |
Piperidine-Based Drug Discovery outlines the complexities of Piperidine scaffold use in drug discovery, including derivative chemistry, structural properties, methods of synthesis and practical implementations. Piperidine scaffolds are the cornerstones of over 70 commercialized drugs (including multiple blockbusters). Designed as a guide for both experts and students working in this and related areas, it is hoped that this volume will encourage and inspire the continued design and development of novel pharmaceuticals based on Piperidine and its derivatives. Heterocyclic compounds are of central importance to medicinal chemistry, as demonstrated by the high percentage of marketable drugs that feature heterocyclic fragments in their structures. As starting points for drug discovery they offer a broad range of attractive properties, and a detailed understanding of the particular characteristics of each is of great benefit to researchers. The most commonly used heterocycle among US FDA approved pharmaceuticals, Piperidine is an extremely important building block in the synthesis of medicinal agents. This heterocycle and its derivatives exhibit a number of important functionalities and have been employed variously as CNS modulators, antiaggregants, anticoagulants, antihistamines, anti-cancer drugs and analgesics. |
| Contents |
Synthesis of Piperidin-4-Ones by Dieckmann CondensationSynthesis of Piperidin-4-Ones by Miscellaneous Methods; Nucleophilic Addition Reactions to the Carbonyl Group of Piperidin-4-Ones; Nucleophilic Substitution Reactions Involving [alpha]-Carbon of Piperidin-4-Ones; Piperidin-3-Ones; Piperidin-2-Ones; 4-Cyano-4-Phenylpiperidines; References; 2. 1-Substituted Piperidines; 2.1 Derivatives of 1-Phenyl-3-(Piperidin-1-yl)Propan-1-ol; Trihexyphenidyl (2226); Biperiden (1329); Pridinol (157); Cycrimine (82); 2.2 Derivatives of 1-Phenyl-4-(Piperidin-1-yl)Butan-1-ol; Diphenidol (323); Pirmenol (234). |
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Front Cover; Piperidine-Based Drug Discovery; Copyright Page; Contents; 1. Introduction; 1.1 The Scope of the Material Under Consideration; 1.2 General Methods of the Synthesis of Piperidine Compounds; Nucleophilic Substitution Reactions; Intermolecular Michael Reactions; Catalyzed Hydroamination Reactions; Aza-Diels-Alder Reactions; Intramolecular Ene Reactions; Ring-Closing Metathesis Reactions; Synthesis of Piperidin-4-Ones; The Synthesis of 2,2,6,6-Tetramethyl-4-Oxopiperidine; Petrenko-Kritschenko Reaction for the Synthesis of 2,6-Disubstituted Piperidin-4-Ones. |
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2.3 Derivatives of 2-(Piperidin-1-yl)Ethan-1-ol and 3-(Piperidin-1-yl)Propan-1-olCloperastine (199); Benproperine (140); Pipazethate (98); Raloxifene (7685); Flavoxate (452); Piperocaine (266); 2.4 Derivatives of 3-(Piperidin-1-yl)Propane-1,2-Diol and 3-(Piperidin-1-yl)Propane-1,1-Diol; Diperodon (147); Pipoxolan (25); 2.5 Derivatives of 1-Phenyl-3-(Piperidin-1-yl)Propan-1-One; Dyclonine (584); 2.6 Derivatives of 2,2-Diphenyl-4-(Piperidin-1-yl)Butanamide; Fenpiverinium Bromide (83); References; 3. 2-Substituted and 1,2-Disubstituted Piperidines; 3.1 Methylphenidate (11968). |
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3.2 Perhexiline (1216)3.3 Pipradrol (259); 3.4 Mefloquine (5370); 3.5 Mepivacaine (4176); 3.6 Ropivacaine (6847); 3.7 Bupivacaine (21293) and Levobupivacaine (1976); 3.8 Flecainide (3638); 3.9 Encainide (682); 3.10 Thioridazine (6558); 3.11 Rimiterol (219); 3.12 Lobeline (1914); 3.13 Argatroban (2627); 3.14 Ascomycin (752), Pimecrolimus (1645), Tacrolimus (32436), Sirolimus (22468), Everolimus (8972), and Temsirolimus (2859); References; 4. 3-Substituted and 1,3-Disubstituted Piperidines; 4.1 Methixene (92); 4.2 Tipepidine (132); 4.3 Timepidium (83); 4.4 Tiagabine (2008). |
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4.5 Piperidolate (72)4.6 Mepenzolate (137); 4.7 Pipenzolate (109); 4.8 Benidipine (927); 4.9 Paroxetine (12203) and Femoxetine (270); 4.10 Troxipide (110); 4.11 Linagliptin (1133); 4.12 Tofacitinib (1130); References; 5. 4-Substituted and 1,4-Disubstituted Piperidines; 5.1 4-Piperidinols and Their Derivatives; Periciazine (112); Diphenylpyraline (453); Ebastine (990); Bepotastine (236); Lamifiban (257); Eucatropine (90); Propiverine (664); Pentapiperide (22); 5.2 4-Phenylpiperidin-4-ols and Their Derivatives; Haloperidol (41140); Bromperidol (515); Moperone (218); Trifluperidol (613). |
| Subject |
Drugs -- Design.
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Drug development.
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Piperidine.
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Drug Discovery |
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Drug Design |
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Piperidines |
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Médicaments -- Conception.
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Médicaments -- Développement.
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Pipéridine.
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MEDICAL -- Pharmacology.
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Drug development
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Drugs -- Design
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Piperidine
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| Other Form: |
Print version: Vardanyan, R.S. (Ruben S.). Piperidine-based drug discovery. Amsterdam, Netherlands : Elsevier, [2017] 0128051574 9780128051573 (OCoLC)978696429 |
| ISBN |
9780128134283 (electronic bk.) |
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0128134283 (electronic bk.) |
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9780128051573 |
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0128051574 |
| Standard No. |
GBVCP 892971649 |
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CHVBK 499792114 |
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CHBIS 011069410 |
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AU@ 000061157004 |
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AU@ 000066136092 |
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UKMGB 018377372 |
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