A Textbook of Medicinal Chemistry draws together contributions from authoritative practitioners to provide a comprehensive overview of the eld as well as insight into the latest trends and research. An ideal companion for students in medicinal chemistry, drug discovery and drug development, while also communicating core principles, the book places the discipline within the context of the burgeoning platform of new modalities now available to drug discovery. The book also highlights the role chemistry has to play in wider target validation and translational technologies. This is a carefully curated compilation of writing from global experts using their broad experience of medicinal chemistry, project leadership and drug discovery and development from an industry, academic and charity perspective to provide unparalleled insight into the eld.
Marilyn Dunlap is Professor Emerita of Chemistry at Middle Tennessee State University, where she specialized in synthetic organic chemistry and medicinal chemistry. Her research, done primarily with undergraduates and M.S. students, was focused on design and synthesis of bioactive peptidomimetics. She holds a Ph.D. in organic chemistry from the University of Wyoming and was an NIH postdoctoral fellow at the University of Pennsylvania. She began her career as a Senior Research Scientist at Hoffmann-La Roche, in drug discovery. After moving to academia, she was a Lecturer at Vanderbilt University before moving to Middle Tennessee State University. After receiving her undergraduate Chemistry degree (Cornell University) and Ph.D. degree (University of Pennsylvania, Chemistry). Dr. Barbara Frances Westerhaus began her career as a medicinal chemist in the pharmaceutical industry (Hoffmann-La Roche & Wyeth Research), and contributed to drug discovery efforts for HIV, cancer, asthma, and CNS disorders with increasing levels of responsibility. In 2004, she joined academia. She was a Professor at the University of Pittsburgh's School of Pharmacy, and until August 2023, when she was appointed Professor of Practice in the Chemistry Department at the University of Pennsylvania. She is a Fellow of the American Association for the Advancement of Science (AAAS) and the American Chemical Society (ACS), recipient of the ACS Philadelphia Local Section Award, Philip S. Portoghese Lectureship, and Garvan-Olin Medal, and was inducted into the ACS Medicinal Chemistry Division Hall of Fame. She has held a number of elected positions at national levels of the ACS and the AAAS, and in the Organic and Medicinal Chemistry Technical Divisions. She is co-author of the textbook Medicinal Chemistry (CRC Press), and served as an Associate Editor of ACS Medicinal Chemistry Letters from 2014- 2023. In 2019, she co-founded Empowering Women in Organic Chemistry (EWOC), and continues to serve on the organizing committee.
Preface 1. DRUGS: ACTION AND DISCOVERY......................................................................11.1 .Introduction1.2 .What are Drugs and Why Do We Need New Ones?1.3 .Drug Discovery and Design: A Historical Outline1.4 .Leads and Analogues1.5 .Sources of Leads and Drugs1.6 .Methods and Routes of Administration: The Pharmaceutical Phase1.7 .Introduction To Drug Action1.8 . Classification of Drugs 2. DRUG STRUCTURE AND SOLUBILITY..............................................................362. 1. .Introduction2.2. .Importance of Solubility2.3. .Techniques For Solubility Enhancement2.4. .Particle Size Reduction2.5. .Solid Dispersion2.6. .Nanosuspension2.7. .Supercritical Fluid (SCF) Process2.8. .Cryogenic Techniques2.9. .Inclusion Complex Formation-Based Techniques2.10. .Micellar Solubilization2.11. .Hydrotrophy2.12. .Crystal Engineering 3. ACTIVITY AND QUANTITATIVE STRUCTURE RELATIONSHIPS..............................................533.1 .Introduction3.2 .Structure–Activity Relationship (SAR)3.3 .Changing Size and Shape3.4 .Introduction of New Substituents3.5 .Changing The Existing Substituents of A Lead3.6 .Case Study: A Sar Investigation to Discover Potent Geminal Bisphosphonates3.7 .Quantitative Structure–Activity Relationship (QSAR) 4. COMPUTER-AIDED DRUG DESIGN...................................................................864.1 .Introduction Contents 4.2. .Materials4.3. .Methods 5. COMBINATORIAL CHEMISTRY.......................................................................1005.1 .Introduction5.2 .Computational Chemistry For Combinatorial Library Design5.3 .Generation of Combinatorial Libraries5.4 .Screening of Combinatorial Libraries5.5 .Encoding and Decoding of Combinatorial Libraries5.6 .Conclusion and Perspectives 6. DRUGS FROM NATURAL SOURCES................................................................1126.1 .Introduction6.2 .Bioassays6.3 .Dereplication6.4 .Structural Analysis of The Isolated Substance6.5 .Active Compound Development6.6..Extraction Procedures6.7 .Fractionation Methods 7. BIOLOGICAL MEMBRANES..............................................................................1387.1 .Structure and Organization of Membranes7.2 .Membrane Proteins7.3 .Interactions Between Lipids and Proteins In Biological Membranes7.4 .Sending Messages Across Membranes7.5 .Membranes In Health and Disease7.6 .Closing Remarks 8. RECEPTORS AND MESSENGERS....................................................................1688.1 .Introduction8.2 .Cellular Level8.3 .Development8.4 .Organ Systems Involved8.5 .Pathophysiology8.6 . Clinical Significance 9. ENZYMES............................................................................................................1799.1 .Introduction9.2 . Classification and Nomenclature9.3 .Active Sites and Catalytic Action9.4 .Regulation of Enzyme Activity9.5 . The Specific Nature of Enzyme Action9.6 .The Mechanisms of Enzyme Action9.7 . The General Physical Factors Affecting Enzyme Action 9.8 .Enz
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