The art of drug synthesis / / edited by Douglas S. Johnson, Jie Jack Li

• Pubblicazione: Hoboken, N.J., : Wiley-Interscience, c2007
• Edizione: 1st ed.
• Descrizione fisica: 1 online resource (xv, 276 pages) : illustrations
• Disciplina: 615.19; 615/.19
• Soggetto topico: Drugs - Design; Pharmaceutical chemistry
• Altri autori: JohnsonDouglas S <1968-> (Douglas Scott) LiJie Jack
• Nota di bibliografia: Includes bibliographical references and index.
• 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
• Sommario/riassunto: The Art of Drug Synthesis illustrates how chemistry, biology, pharmacokinetics, and a host of other disciplines come together to produce successful medicines. The authors have compiled a collection of 21 representative categories of drugs, from which they have selected as examples many of the best-selling drugs on the market today. An introduction to each drug is provided, as well as background to the biology, pharmacology, pharmacokinetics, and drug metabolism, followed by a detailed account of the drug synthesis.Edited by prominent scientists working in drug discovery for PfizerM
• Titolo autorizzato: The art of drug synthesis
• 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: Inglese
• Record Nr.: 9910143402603321
• Lo trovi qui: Univ. Federico II
• Serie: Wiley Series on Drug Synthesis