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The art of drug synthesis / / edited by Douglas S. Johnson, Jie Jack Li
| The art of drug synthesis / / edited by Douglas S. Johnson, Jie Jack Li |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2007 |
| Descrizione fisica | 1 online resource (xv, 276 pages) : illustrations |
| Disciplina |
615.19
615/.19 |
| Altri autori (Persone) |
JohnsonDouglas S <1968-> (Douglas Scott)
LiJie Jack |
| Collana | Wiley Series on Drug Synthesis |
| Soggetto topico |
Drugs - Design
Pharmaceutical chemistry |
| ISBN |
1-118-67846-X
1-280-91677-X 9786610916771 0-470-13497-6 0-470-13496-8 |
| Formato | Materiale a stampa  |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
THE ART OF DRUG SYNTHESIS; CONTENTS; Foreword; Preface; Contributors; 1 THE ROLE OF MEDICINAL CHEMISTRY IN DRUG DISCOVERY; 1.1 Introduction; 1.2 Hurdles in the Drug Discovery Process; 1.3 The Tools of Medicinal Chemistry; 1.3.1 In Silico Modeling; 1.3.2 Structure-Based Drug Design (SBDD); 1.4 The Role of Synthetic Chemistry in Drug Discovery; References; 2 PROCESS RESEARCH: HOW MUCH? HOW SOON?; 2.1 Introduction; 2.2 Considerations for Successful Scale-up to Tox Batches and Phase I Material; 2.3 Considerations for Phase 2 Material and Beyond; 2.3.1 Reagent Selection; 2.3.2 Solvent Selection
2.3.3 Unit Operations; 2.3.4 Developing Simple, Effective, Efficient Work-ups and Isolations; 2.3.5 The Importance of Physical States; 2.3.6 Route Design and Process Optimization to Minimize COG; 2.4 Summary; References; I CANCER AND INFECTIOUS DISEASES; 3 AROMATASE INHIBITORS FOR BREAST CANCER: EXEMESTANE (AROMASIN®), ANASTROZOLE (ARIMIDEX®), AND LETROZOLE (FEMARA®); 3.1 Introduction; 3.2 Synthesis of Exemestane; 3.3 Synthesis of Anastrozole; 3.4 Synthesis of Letrozole; References 4 QUINOLONE ANTIBIOTICS: LEVOFLOXACIN (LEVAQUIN®), MOXIFLOXACIN (AVELOX®), GEMIFLOXACIN (FACTIVE®), AND GARENOXACIN (T-3811)4.1 Introduction; 4.1.1 Mechanism of Action; 4.1.2 Modes of Resistance; 4.1.3 Structure-Activity Relationship (SAR) and Structure-Toxicity Relationship (STR); 4.1.4 Pharmacokinetics; 4.1.5 Synthetic Approaches; 4.2 Levofloxacin; 4.3 Moxifloxacin; 4.4 Gemifloxacin; 4.5 Garenoxacin (T-3811): A Promising Clinical Candidate; References; 5 TRIAZOLE ANTIFUNGALS: ITRACONAZOLE (SPORANOX®), FLUCONAZOLE (DIFLUCAN®), VORICONAZOLE (VFEND®), AND FOSFLUCONAZOLE (PRODIF®) 5.1 Introduction; 5.2 Synthesis of Itraconazole; 5.3 Synthesis of Fluconazole; 5.4 Synthesis of Voriconazole; 5.5 Synthesis of Fosfluconazole; References; 6 NON-NUCLEOSIDE HIV REVERSE TRANSCRIPTASE INHIBITORS; 6.1 Introduction; 6.2 Synthesis of Nevirapine; 6.3 Synthesis of Efavirenz; 6.4 Synthesis of Delavirdine Mesylate; References; 7 NEURAMINIDASE INHIBITORS FOR INFLUENZA: OSELTAMIVIR PHOSPHATE (TAMIFLU®) AND ZANAMIVIR (RELENZA®); 7.1 Introduction; 7.1.1 Relenza; 7.1.2 Tamiflu; 7.2 Synthesis of Oseltamivir Phosphate (Tamiflu®); 7.3 Synthesis of Zanamivir (Relenza®); References II CARDIOVASCULAR AND METABOLIC DISEASES; 8 PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR (PPAR) AGONISTS FOR TYPE 2 DIABETES; 8.1 Introduction; 8.1.1 Insulin; 8.1.2 Sulfonylurea Drugs; 8.1.3 Meglitinides; 8.1.4 Biguanides; 8.1.5 Alpha-Glucosidase Inhibitors; 8.1.6 Thiazolidinediones; 8.2 Synthesis of Rosiglitazone; 8.3 Synthesis of Pioglitazone; 8.4 Synthesis of Muraglitazar; References; 9 ANGIOTENSIN AT(1) ANTAGONISTS FOR HYPERTENSION; 9.1 Introduction; 9.2 Losartan Potassium; 9.2.1 Introduction to Losartan Potassium; 9.2.2 Synthesis of Losartan Potassium; 9.3 Valsartan; 9.3.1 Introduction to Valsartan |
| Record Nr. | UNINA-9910143402603321 |
| Hoboken, N.J., : Wiley-Interscience, c2007 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Modern drug synthesis [[electronic resource] /] / edited by Jie Jack Li and Douglas S. Johnson
| Modern drug synthesis [[electronic resource] /] / edited by Jie Jack Li and Douglas S. Johnson |
| Pubbl/distr/stampa | Hoboken, NJ, : Wiley, c2010 |
| Descrizione fisica | xiv, 355 p. : ill |
| Disciplina | 615/.19 |
| Altri autori (Persone) |
LiJie Jack
JohnsonDouglas S <1968-> (Douglas Scott) |
| Soggetto topico |
Drugs - Design
Pharmaceutical chemistry |
| ISBN |
0-470-76859-2
1-299-18617-3 0-470-76858-4 1-118-70124-0 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Record Nr. | UNINA-9910208846603321 |
| Hoboken, NJ, : Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||
Modern drug synthesis / / edited by Jie Jack Li and Douglas S. Johnson
| Modern drug synthesis / / edited by Jie Jack Li and Douglas S. Johnson |
| Edizione | [1st ed.] |
| Pubbl/distr/stampa | Hoboken, NJ, : Wiley, c2010 |
| Descrizione fisica | xiv, 355 p. : ill |
| Disciplina | 615/.19 |
| Altri autori (Persone) |
LiJie Jack
JohnsonDouglas S <1968-> (Douglas Scott) |
| Soggetto topico |
Drugs - Design
Pharmaceutical chemistry |
| ISBN |
0-470-76859-2
1-299-18617-3 0-470-76858-4 1-118-70124-0 |
| Formato | Materiale a stampa |
| Livello bibliografico | Monografia |
| Lingua di pubblicazione | eng |
| Nota di contenuto |
Intro -- Modern Drug Synthesis -- Contents -- Preface -- Contributors -- I. Infectious Diseases -- Chapter 1. Raltegravir (Isentress): The First-in-Class HIV-1 Integrase Inhibitor -- 1.1 Background -- 1.2 Pharmacology -- 1.3 Structure-Activity Relationship (SAR) -- 1.4 Pharmacokinetics and Drug Metabolism -- 1.5 Efficacy and Safety -- 1.6 Syntheses -- 1.7 References -- Chapter 2. Maraviroc (Selzentry): The First-in-Class CCR5 Antagonist for the Treatment of HIV -- 2.1 Background -- 2.2 Structure-Activity Relationship (SAR) -- 2.3 Pharmacokinetics and Safety -- 2.4 Syntheses -- 2.5 References -- Chapter 3. Darunavir (Prezista): A HIV-1 Protease Inhibitor for Treatment of Multidrug Resistant HIV -- 3.1 Background -- 3.2 Pharmacology -- 3.3 Structure-Activity Relationship (SAR) -- 3.4 Pharmacokinetics and Drug Metabolism -- 3.5 Efficacy and Safety -- 3.6 Syntheses -- 3.7 References -- II. Cancer -- Chapter 4. Decitabine (Dacogen): A DNA Methyltransferase Inhibitor for Cancer -- 4.1 Background -- 4.2 Pharmacology -- 4.3 Structure-Activity Relationship (SAR) -- 4.4 Pharmacokinetics and Drug Metabolism -- 4.5 Efficacy and Safety -- 4.6 Syntheses -- 4.7 References -- Chapter 5. Capecitabine (Xeloda): An Oral Chemotherapy Agent -- 5.1 Background -- 5.2 Pharmacology -- 5.3 Structure-Activity Relationship (SAR) -- 5.4 Pharmacokinetics and Efficacy -- 5.5 Syntheses -- 5.6 References -- Chapter 6. Sorafenib (Nexavar): A Multikinase Inhibitor for Advanced Renal Cell Carcinoma and Unresectable Hepatocellular Carcinoma -- 6.1 Background -- 6.2 Pharmacology -- 6.3 Structure-Activity Relationship (SAR) -- 6.4 Pharmacokinetics and Drug Metabolism -- 6.5 Efficacy and Safety -- 6.6 Syntheses -- 6.7 References -- Chapter 7. Sunitinib (Sutent): An Angiogenesis Inhibitor -- 7.1 Background -- 7.2 Discovery and Development -- 7.3 Syntheses -- 7.3.1 Discovery Route.
7.3.2 Process Route -- 7.4 References -- Chapter 8. Bortezomib (Velcade): A First-in-Class Proteasome Inhibitor -- 8.1 Background -- 8.2 Pharmacology -- 8.3 Structure-Activity Relationship (SAR) -- 8.4 Pharmacokinetics and Drug Metabolism -- 8.5 Efficacy and Safety -- 8.6 Syntheses -- 8.7 References -- Chapter 9. Pazopanib (Votrient): A VEGFR Tyrosine Kinase Inhibitor for Cancer -- 9.1 Background -- 9.2 Pharmacology -- 9.3 Structure-Activity Relationship (SAR) -- 9.4 Pharmacokinetics and Drug Metabolism -- 9.5 Efficacy and Safety -- 9.6 Syntheses -- 9.7 Other VEGFR Inhibitors in Development: Vandetanib and Cediranib -- 9.8 References -- III. Cardiovascular and Metabolic Diseases -- Chapter 10. Sitagliptin (Januvia): A Treatment for Type 2 Diabetes -- 10.1 Background -- 10.2 Pharmacology -- 10.3 Structure-Activity Relationship (SAR) -- 10.4 Pharmacokinetics and Drug Metabolism -- 10.5 Efficacy and Safety -- 10.6 Syntheses -- 10.7 References -- Chapter 11. Aliskiren (Tekturna), The First-in-Class Renin Inhibitor for Hypertension -- 11.1 Background -- 11.2 Pharmacology -- 11.3 Structure-Activity Relationship (SAR) -- 11.4 Pharmacokinetics and Drug Metabolism -- 11.5 Efficacy and Safety -- 11.6 Syntheses -- 11.7 References -- Chapter 12. Vernakalant (Kynapid): An Investigational Drug for the Treatment of Atrial Fibrillation -- 12.1 Background -- 12.2 Pharmacology -- 12.3 Structure-Activity Relationship (SAR) -- 12.4 Pharmacokinetics and Drug Metabolism -- 12.5 Efficacy and Safety -- 12.6 Syntheses -- 12.7 References -- Chapter 13. Conivaptan (Vaprisol), Vasopressin Via and V2 Antagonist for Hyponatremia -- 13.1 Background -- 13.2 Pharmacology -- 13.3 Structure-Activity Relationship (SAR) -- 13.4 Pharmacokinetics and Drug Metabolism -- 13.5 Efficacy and Safety -- 13.6 Syntheses -- 13.7 References. Chapter 14. Rivaroxaban (Xarelto): A Factor Xa Inhibitor for the Treatment of Thrombotic Events -- 14.1 Background -- 14.2 Pharmacology -- 14.3 Structure-Activity Relationship (SAR) -- 14.4 Pharmacokinetics and Drug Metabolism -- 14.5 Efficacy and Safety -- 14.6 Syntheses -- 14.7 Compounds in Development: Apixaban and Otamixaban -- 14.8 References -- Chapter 15. Endothelin Antagonists for the Treatment of Pulmonary Arterial Hypertension -- 15.1 Background -- 15.2 Treatment of PAH -- 15.3 Endothelin Antagonists -- 15.4 Synthesis of Bosentan -- 15.5 Synthesis of Sitaxsentan -- 15.6 Synthesis of Ambrisentan -- 15.7 Conclusion -- 15.8 References -- III. Central Nervous System Diseases -- Chapter 16. Varenicline (Chantix), An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation -- 16.1 Background -- 16.2 Discovery Chemistry Program -- 16.3 Pharmacology -- 16.4 Pharmacokinetics and Drug Metabolism -- 16.5 Efficacy and Safety -- 16.6 Syntheses -- 16.7 References -- Chapter 17. Donepezil, Rivastigmine, and Galantamine: Cholinesterase Inhibitors for Alzheimer Disease -- 17.1 Background -- 17.2 Pharmacology -- 17.3 Structure-Activity Relationship (SAR) -- 17.4 Pharmacokinetics and Drug Metabolism -- 17.5 Efficacy and Safety -- 17.6 Synthesis of Donepezil -- 17.7 Synthesis of Rivastigmine -- 17.8 Synthesis of Galantamine -- 17.9 References -- Chapter 18. Aprepitant (Emend): A NK1 Receptor Antagonist for the Treatment of Postchemotherapy Emesis -- 18.1 Background -- 18.2 In Vitro Pharmacology and Structure-Activity Relationships -- 18.3 In Vivo Pharmacology -- 18.4 Pharmacokinetics and Drug Metabolism -- 18.5 Efficacy and Safety -- 18.6 Syntheses -- 18.7 References -- Chapter 19. Armodafinil (Nuvigil): A Psychostimulant for the Treatment of Narcolepsy -- 19.1 Background -- 19.2 Pharmacology -- 19.3 Pharmacokinetics and Drug Metabolism. 19.4 Efficacy and Safety -- 19.5 Synthesis -- 19.6 References -- V. Miscellaneous -- Chapter 20. Raloxifene (Evista): A Selective Estrogen Receptor Modulator (SERM) -- 20.1 Background -- 20.2 Mechanism of Action -- 20.3 Pharmacokinetics and Drug Metabolism -- 20.4 Efficacy and Safety -- 20.5 Syntheses -- 20.6 References -- Chapter 21. Latanoprost (Xalatan): A Prostanoid FP Agonist for Glaucoma -- 21.1 Background -- 21.2 Syntheses -- 21.3 References -- Index. |
| Record Nr. | UNINA-9910816237503321 |
| Hoboken, NJ, : Wiley, c2010 | ||
| Materiale a stampa | ||
| Lo trovi qui: Univ. Federico II | ||
| ||