Essentials of Medicinal Chemistry and Pharmacology

Course Code: EMCP

Overview

This course is for chemical scientists who have little or no formal training in physiology, pharmacology, or medicinal chemistry. It reviews key concepts and principles of those sciences, including:

• Modern concepts of drug action, drug-receptor interactions, and pharmacophore analysis
• Molecular basis for the mechanism of action of drugs
• Concepts in PK and PD, drug efficacy and potency, physiological effects, and structure/function relationships
• Modern drug design approaches, including structure-based and ligand-based drug design
• ADME/tox

When and Where

Key Topics

• Key concepts and principles that serve as the basis of medicinal chemistry and pharmacology.
• Modern concepts of drug action, drug-receptor interactions, and pharmacophore analysis.
• Molecular basis for the mechanism of action of drugs.
• Concepts in pharmacodynamics and pharmacokinetices.
• Drug efficacy and potency, physiological effects, structure-function relationships
• Physiological and pharmacological effects that guide the design of new therapeutic agents.
• Survey of selected drug classes to highlight general principles.
• Modern drug design approaches, including structure-based and ligand-based drug design.
• Absorption, distribution, metabolism, elimination and toxicity (ADME/tox).

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Course Instructor

Dr. J. Phillip Bowen (Course Director) is Professor of Chemistry & Biochemistry and Director of the Center for Drug Discovery at the University of North Carolina at Greensboro. Dr. Bowen is also an Adjunct Professor in the Division of Medicinal Chemistry and Natural Products, School of Pharmacy, at the University of North Carolina at Chapel Hill. If you have technical questions about the course, contact Professor Bowen at (336) 334-4257 or at jpbowen@uncg.edu.

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Who Should Attend?

Chemical scientists who have little or no formal training in physiology, pharmacology, or medicinal chemistry. Registrants should have a firm grasp of organic chemistry and the equivalent of an introductory course in physical chemistry and biochemistry.

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How You'll Benefit from This Course

• Consult with an expert about your research concerns.
• Learn the vocabulary used in the fields of medicinal chemistry and pharmacology. Learn the general principles underlying the mechanism of action of various drugs.
• Learn structure-function relationships and their influence on drug design strategies.
• Understand the chemical and pharmacological basis for the current therapeutic agents.
• Trace the development of selected drugs from the bench to the market.
• Understand pharmacological principles of drug action.
• See how the chemical sciences influence pharmacology and drug design.
• Review various drug classes and therapeutic strategies.
• Improve your ability to interact with pharmacologists and computational scientists in team-oriented research pursuits.
• Be exposed to state-of-the art molecular modeling methods for drug design, including QSAR, 3D-QSAR, docking, pharmacophore perception, computer-assisted drug design, and database searching.

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Agenda

General Concepts and Principles of Pharmacology:

• Definitions, references, and literature of medicinal chemistry and pharmacology--drug classifications, drug names, sources of drugs.
• Drug approval process, clinical trials, double-blind studies, placebo effect, FDA approval process.
• Overview of the drug discovery history.
• Physiological considerations--membrane models, ion channels, G-coupled protein receptors, blood-brain barrier, etc.
• Basis of drug action in the human body, sites of action, drug targets--drug-receptor binding, chemical forces, structurally specific and nonspecific drugs; receptor theories, occupation theory, signaling pathways, dose-response curves; desensitization and sensitization, tolerance and dependence, drug allergies.
• Drug-receptor interactions, concentration-response curves, receptor data plots--agonists, partial agonists, antagonists, inverse agonists.
• Organic functional groups in drug molecules, stereochemistry, and structure-function relationships.
• Drug-like and lead-like physicochemical properties.
• Pharmacophore definition and examples, pharmacophore development, drug design concepts.
• Pharmacokinetics overview and implications in medicinal chemistry and pharmacology--drug doses, routes of administration, routes of elimination, protein binding and its effects on drugs; key pharmacology concepts: apparent volume, drug clearance, rate of elimination, drug half-life, bioavailability, protein plasma binding, drug stability, drug formulations.
• Drug solubility, dissolution, absorption, and distribution of drugs (active transport and passive diffusion)--case studies, predictive solubility models, Lipinski’s rules.
• Drug metabolism (Phases I and II), first pass metabolism, and excretion.
• Toxicity testing, side effects, drug interactions, pharmacogenetics.
• Property-based drug design.
• Physicochemical properties--electronic effects, steric effects, hydrophobic effects, pKa, pH.
• Introduction to classical QSAR and 3D-QSAR.
• Enzymes and enzyme inhibitors--examples, case studies, structure-based drug design.
• Computer-Assisted Drug Design.

Survey of selected drug classes, including a discussion of physiology and anatomy, mechanism of action, drug development, case histories:

• Antihistamines
• Antimicrobials
• Antiviral agents
• Antiulcer agents
• Antineoplastic agents
• Anti-inflammatory agents
• Central Nervous System drugs
• Adrenergic agents
• Cholingeric agents
• Antidepressants

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Course Fees

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