This flagship reference for medicinal chemists and pharmaceutical professionals has been thoroughly updated and expanded to incorporate the concepts of drug hunting along with its existing coverage of the entire process of drug discovery and development.
Features thematic volumes or sections on drug discovery, drug development, cardiovascular diseases, metabolic diseases, immunology, cancer, antiinfectives, and CNS disorders
Updates existing chapters and adds 35 new ones, incorporating the concepts of drug hunting
Includes topics like: opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures
Table of contents
PREFACE OF THE EDITOR-IN-CHIEF
PREFACE OF THE CONSULTING EDITOR
PREFACE OF THE VOLUME EDITOR
CONTRIBUTORS
Volume 1 : Methods in Drug Discovery
1 Chirality and Drug Discovery
2 Drug Discovery beyond the Rule of Five
3 Microbes to Man: From Soils and the Depths to Drugs as of early 2019
4 Fragment-Based Lead Discovery
5 Recent Advances in Development, Validation, and Exploitation of QSAR Models
6 Structure-Based Drug Design
7 Docking, Scoring and Virtual Screening in Drug Discovery
8 Computational Chemistry Tools
9 Assay Development and High-Throughput Screening
10 Advances in NMR-based Characterization of Drug Substances, Impurities, Degradants and Drug Metabolites
11 NMR-Based Screening and Drug Discovery
12 Mass Spectrometry and Drug Discovery
13 Cryo Electron Microscopy in Drug Discovery and Development: Opportunities and Challenges
14 Combinatorial Chemistry and Its Associated Technologies
15 Recent Advances in Chemistry Technologies and Applications to Medicinal Chemistry
16 Automated Synthesis
17 Artificial Intelligence in Medicinal Chemistry
18 Medicinal Chemical Biology
Volume 2 : Lead Discovery in Drug Discovery
1 Ion Channels as Therapeutic Drug Targets
2 Drug Transport and Membrane Transport Proteins
3 Structure-Based Drug Design for G Protein-Coupled Receptors
4 Enzymes as Drug Targets
5 Allosterism & Drug Discovery
6 Nuclear Hormone Receptor Medicinal Chemistry
7 ADMET In Vitro Profiling Utility and Applications in Lead Discovery
8 Principles of Drug Metabolism
9 Advances in Multiobjective Optimization for Drug Discovery and Development
10 The Design and Application of Bioisosteres in Drug Design
11 Structure Alerts in Medicinal Chemistry (original chapter: Structural Alerts for Toxicity)
Volume 3 : Development
1 Intellectual Property for Biotechnology and Pharmaceutical Products
2 Experiences in Academic and Industry Partnerships Forging a Path to Translational Drug Discovery
3 Large-Scale Synthesis
4 Preparative Chromatography for Production
5 Translational Pharmaceutics and Early Phase Clinical Development
6 Salt Screening and Selection
7 Polymorphic Crystal Forms in Drug Delivery (Crystal Engineering)
8 Physicochemical Characterization and Oral Dosage Form Design and Selection
9 Prodrugs: Strategic Deployment, Metabolic Considerations, and Chemical Design Principles
10 Provisional BCS Classification of Leading Oral Drugs in Global Market
11 Process Development of Protein Therapeutics
12 Role of Permeability in Drug ADME, PK Interactions and Toxicity
13 Toxicology and Nonclinical Safety Assessment in Pharmaceutical Discovery and Development
14 Quality Assurance
15 The FDA and Drug Regulatory Issues
16 FDA-Approved Medicines
17 Clinical Development - A Primer
18 Global Health Outcomes and Real World Evidence a Primer
19 A Brief Primer on Project Leadership, Project Management and Cross-Functional Teams
Volume 4 : Cardiovascular, Endocrine and Metabolic Diseases
1 Dipeptidyl Peptidase 4 Inhibitors
2 Glucagon Like Peptide 1 Receptor Activators
3 Sodium Glucose Co-Transporter Inhibitors for the Treatment of Diabetes
4 Treatments for Non-Alcoholic Steatohepatitis (NASH)
5 Therapeutic Strategies for Sickle Cell Disease
6 Hematopoietic Agents
7 Anticoagulants
8 Antiplatelet Agents (needs proofreading, few minor changes needs to be done by the author.
9 Atherosclerosis: Cholesterol Management (original: Atherosclerosis I: LDL Cholesterol Lowering)
10 Recent Advances Toward New Small Molecule Therapies for Heart Failure
11 ACE Inhibitors
Volume 5 : Inflammation, Pulmonary, Bone, Immunology Agents and Vitamins
1 Fundamentals of Steroid Chemistry and Biochemistry
2 Estrogen Receptor Modulators (original chapter: Female Sex Hormones, Contraceptives, And Fertility Drugs by Peter C. Ruenitz)
3 Modulation of the Androgen Receptor Axis bmc055 (original chapter: Male Sex Hormones, Analogs, and Antagonists)
4 Essential Micronutrients: Vitamins and Essential Fatty Acids
5 Current and Emerging Therapies in Pulmonary Disease
6 Anti-Inflammatory Glucocorticoids and Receptors
7 Osteoporosis Therapy: Mechanistic Antiresorptives
8 Osteoporosis: Current and Future Anabolic Therapy
9 Drug Discovery in Erectile Dysfunction and Sleep Disorders (original chapter: Drug Discovery in Non-Life-Threatening Disorders: Erectile Dysfunction, Insomnia, and Smoking)
10 Multiple Sclerosis
11 JAK Inhibitors for Autoimmune Diseases
12 Eicosanoid Pathway Modulators: Prostaglandins, Prostacyclins and Thromboxanes
Volume 6 : Cancer
1 Synthetic DNA Target Therapeutics
2 USFDA-Approved Small-Molecule Kinase Inhibitors for Cancer Therapy (original chapter: Kinase Inhibitors: Approved Drugs and Clinical Candidates)
3 Cancer Drug Resistance: Targets and Therapies
4 Natural Products as Cytotoxic Agents
5 Tumor Metabolism: Focused on Tumor Glycolysis, Progress and Prospects in Cancer Therapy
6 Small-Molecule Effectors of DNA Repair Proteins: applications for development of cancer therapeutics and research
7 Angiogenesis Inhibitors
8 Cancer Targets Involving the Ubiquitin Proteasome System
9 Immuno-oncology
10 The Design and Development of Antibody-Drug Conjugates (ADCs) for the Treatment of Cancer
11 Hsp90 Inhibitors
12 Gene Therapy with Plasmid DNA
Volume 7 : Antiinfectives
1 Confronting the COVID-19 Pandemic: December 2019 – May 2020
2 Medicinal Chemistry of β-Lactam Antibiotics
3 2010 to 2020: ten years of malaria drug discovery
4 Drug Discovery and Development for Kinetoplastid Diseases
5 Anti-DNA Virus Agents
6 Polymyxins as Antibacterials and Antibiotic Potentiators
7 Antifungal Drugs
8 The Gut Microbiome
9 Antitubercular Agents
10 Bacterial Efflux Pumps and Their Inhibitors
11 Current Status of Approaches to Eradicate HIV Infection
12 Antiinfective Case Histories
Volume 8 : CNS
1 Cholinergics/Anticholinergics
2 Therapeutic and Diagnostic Agents for Parkinson’s Disease
3 Opioid Receptor Ligands
4 Antipsychotic Agents
5 Antidepressants
6 PET and SPECT in Drug Development
7 New and Emerging Antiepileptic Drugs
8 Cognition
9 The Blood-brain Barrier and CNS Drug Delivery
INDEX
Donald Abraham is an Emeritus Professor of Medicinal Chemistry and Emeritus Director of the Institute for Structural Biology and Drug Discovery at Virginia Commonwealth University. He was edited both previous editions of Burger's. In 2010, Dr. Abraham was elected to the Hall of Fame of the American Chemical Society's Medicinal Chemistry Division.
Michael Myers, PhD is Senior Director of Due Diligence at Lilly Research Labs. He has over 30 years of experience with drug discovery and development targeting various disease areas. Dr. Myers has over 35 patents and led efforts in evaluating new lead generation technologies and processes in early drug discovery, predictive ADMET, and computational chemistry approaches
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