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ERIC Number: EJ1079219
Record Type: Journal
Publication Date: 2015-Oct
Pages: 6
Abstractor: As Provided
Reference Count: 19
ISBN: N/A
ISSN: ISSN-0021-9584
Hands-On Approach to Structure Activity Relationships: The Synthesis, Testing, and Hansch Analysis of a Series of Acetylcholineesterase Inhibitors
Locock, Katherine; Tran, Hue; Codd, Rachel; Allan, Robin
Journal of Chemical Education, v92 n10 p1745-1750 Oct 2015
This series of three practical sessions centers on drugs that inhibit the enzyme acetylcholineesterase. This enzyme is responsible for the inactivation of acetylcholine and has been the target of drugs to treat glaucoma and Alzheimer's disease and for a number of insecticides and warfare agents. These sessions relate to a series of carbamate inhibitors that are classed as slowly reversible anticholinesterases and show how structure-activity relationships can guide the development of drug molecules. In Practical 1, each student group synthesizes one carbamate inhibitor of acetylcholinesterase. In Practical 2, students measure the activity of their inhibitor to derive an IC[subscript 50] value suitable for comparison with the other derivatives made by the class. In Practical 3, students gain firsthand experience with structure-activity methods, such as a Hansch analysis, to investigate whether these can be used to make predictions of the activity of related compounds based on structural properties. This series gives students a rare insight into a number of the important aspects of drug discovery, that of drug synthesis, activity testing, and the construction of subsequent quantitative structure-activity relationships (QSARs).
Division of Chemical Education, Inc and ACS Publications Division of the American Chemical Society. 1155 Sixteenth Street NW, Washington, DC 20036. Tel: 800-227-5558; Tel: 202-872-4600; e-mail: eic@jce.acs.org; Web site: http://pubs.acs.org/jchemeduc
Publication Type: Journal Articles; Reports - Descriptive
Education Level: Higher Education; Postsecondary Education
Audience: N/A
Language: English
Sponsor: N/A
Authoring Institution: N/A