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Drug Design and Discovery

X412 (2 semester units in Chemistry)

Designed for individuals working or interested in the pharmaceutical and biotechnology industries, this course is focused on issues related to identifying and optimizing a small molecule or biologic drug candidate for clinical development.

In the first part, the instructor discusses the principles and focuses on the challenges of small molecule or biologic drug discovery. You study such topics as lead identification via high-throughput screening, lead validation, lead optimization via synthetic and parallel chemistry, SAR and QSAR development, pharmacophore generation, the importance of intellectual property, and the role of molecular modeling in drug design. You also learn about pharmacokinetic parameters, toxicological profiling, formulation/solubility considerations, and pre-clinical strategies employed in preparation for clinical development.

In the second part, you examine the underlying chemical principles vital to the discovery of new drugs. The focus is on how the structure of a molecule affects drug function at the level of the receptor. Rather than surveying classes of drugs, you study representative examples that exemplify important principles. The concepts discussed are applicable to understanding many classes of drugs in a variety of therapeutic areas. Students work in small groups solving problems related to drug discovery. For more information go to www.homestead.com/medchem412.

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