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Pharmaceutical Chemistry 1

Course Description

The design of new drug structures is a challenging and multidisciplinary process. It involves a multistep process of identifying the target structure, an initial lead structure, optimization of the lead to a drug structure. This process requires knowledge of chemistry, biology, pharmacology, and translation of principles of various other disciplines to develop a feasible drug candidate. This course will incorporate principles of drug design, recognition of potential metabolic vulnerabilities, screening for toxicities and in vitro disease models, and development of formulations for administration in animal testing.

This course incorporates early cross-sectional and competency concepts essential to the drug design & development process:

  • Demonstrate the interactions between a target and a drug compound based on functional groups and physicochemical properties
  • Design a pharmacophore lead structure based on properties of the target, its physiological role, and the intended route of administration
  • Summarize synthesis strategies for designing drugs with specific functional groups
  • Assess metabolic liability of functional groups and predict routes of metabolism based on a given drug structure

Course Goal

Despite an active pharmaceutical development and research market, few new drug candidates have entered the pipeline in recent years and made it to market. With a growing demand for both new small molecular weight drugs with fewer adverse effects and new biological drugs with a more targeted mechanism of action, research is focused on rational drug design or modification of existing structures that help to improve characteristics and binding affinity. This course will use a number of available drugs to illustrate the drug design and development process.


PHA 6432 Fundamentals of Pharmaceutical Chemistry


Module Topic
Module 1 Target structures and their identification
Module 2 From hit to lead, initial optimization and design of drug structures
Module 3 Protein therapeutics (biologicals), similarities & differences
Module 4 Modeling of drug-target interactions
Module 5 Lead and analogue synthesis approaches
Module 6 Metabolic screening, vulnerabilities & solutions
Module 7 Suitable disease in vitro screening models & limitations
Module 8 Drug Metabolism & Pharmacokinetics (DMPK) in early drug design
Module 9 Toxicity evaluation & testing
Module 10 Prodrugs & formulation for preclinical testing

Course Structure

Group discussion forums, online chat sessions, asynchronous mini-lectures, online timed quizzes, interactive animations, and individual e-mail contact between student and instructor. Students will be required to submit written essay assignments, record asynchronous presentations, as well as complete timed quizzes. The instructor will also be frequently available for one-on-one virtual office hours.

Recommended Materials

There is no single recommended text for this course. Helpful textbooks include:

  • Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization
    Author: Li Di, Edward H Kerns
    Publisher: Academic Press; 2nd edition (2016)
    ISBN: 978-0128010761
  • Basic Principles of Drug Discovery and Development
    Author: Benjamin Blass
    Publisher: Academic Press; 1st edition (2015)
    ISBN: 978-0124115088
  • Early Drug Development: Strategies and Routes to First-in-Human Trials
    Author: Mitchell N. Cayen
    Publisher: Wiley; 1st edition (2010)
    ISBN: 978-0470170861
  • Goodman & Gilman’s The Pharmacological Basis of Therapeutics
    Author: Laurence L. Brunton, Bruce A. Chabner, Bjorn Christian Knollmann
    Publisher: McGraw-Hill Professional; 12th edition (2010)
    ISBN: 978-0071624428
  • Foye’s Principles of Medicinal Chemistry
    Author: Thomas L. Lemke, David A. Williams, Victoria F. Roche, S. William Zito
    Publisher: Wolters Kluwer, Lippincott Williams & Wilkins; 6th edition (2008)
    ISBN: 9780781768795

Library Access

Distance Education and UF Online Students enjoy the same library privileges as on-campus students. To utilize the University of Florida Library System, click here!

At a Glance