Burger's Medicinal Chemistry, Drug Discovery and Development

Donald J. Abraham is Emeritus Professor of Medicinal Chemistry and Emeritus Director of the Institute for Structural Biology and Drug Discovery at Virginia Commonwealth University. He is a member of 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 worked in drug discovery and development for over 30 years. He holds over 35 patents and has led efforts in evaluating new lead generation technologies and processes in early drug discovery, predictive ADMET, and computational chemistry.

Kent D. Stewart, PhD (Volume Editor) is Associate Professor of Basic Pharmaceutical Sciences at High Point University. Previously, he worked for over 25 years in the industry at Burroughs Wellcome, AbbVie, and Abbott Laboratories.

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 -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