A receptor-grounded approach to teaching nonsteroidal antiinflammatory drug chemistry and structure-activity relationships

Abstract

Objective: To describe a receptor-based approach to promote learning about nonsteroidal anti-inflammatory drug (NSAID) chemistry, structure-activity relationships, and therapeutic decision-making.

Design: Three lessons on cyclooxygenase (COX) and NSAID chemistry, and NSAID therapeutic utility, were developed using text-based resources and primary medicinal chemistry and pharmacy practice literature. Learning tools were developed to assist students in content mastery.

Assessment: Student learning was evaluated via performance on quizzes and examinations that measured understanding of COX and NSAID chemistry, and the application of that knowledge to therapeutic problem solving.

Conclusion: Student performance on NSAID-focused quizzes and examinations documented the success of this approach.

Keywords: medicinal chemistry; nonsteroidal antiinflammatory drugs.

Figure 1

2D representations of COX-1 and COX-2 NSAID binding sites.

Figure 2

3D model of the COX-1 and COX-2 NSAID binding site residues.

Figure 3

NSAID structures.