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Stomp the Stomach Bug

Designing Norovirus Inhibitors



Author:

Nora S. Green
Department of Chemistry
Randolph-Macon College
ngreen@rmc.edu

Abstract:

Norovirus is one of the most common causes of infectious diarrhea and vomiting, leading to the nickname “winter vomiting disease.” The virus is estimated to be responsible for about half of all food-borne illnesses (CDC) due to its ability to spread rapidly when people are in close quarters, such as in classrooms, on college campuses, and cruise ships. This directed case study is written for an upper-level medicinal chemistry course after students have learned about the basics of drug discovery and design and then apply that knowledge to the development of a variety of different disease states and conditions. Students answer questions and analyze tables of actual data from a research article (Journal of Medicinal Chemistry (2015, 58, 3144–55). The case might also be used with benefit in courses that cover general viral mechanisms and structure (e.g., microbiology and virology) and enzyme kinetics (e.g., biochemistry and cell biology).

Objectives:
  • Describe the potential role of protease inhibitors in the treatment of noroviruses and other viral targets.
  • Explain the differences between IC50 and EC50 values.
  • Interpret inhibition data (IC50, EC50, % inhibition).
  • Apply the concept of structure activity relationships.
  • Explain how the differences in the functional groups and/or structures of different molecules contribute to their therapeutic activity or physicochemical properties.
  • Explain in general terms the advantages of developing analogs of lead compounds in the development of new drugs.
Keywords: Norovirus; drug design; protease inhibitors; IC50; EC50; % inhibition; structure activity relationships; gastroenteritis; therapeutic peptides
Topical Area: N/A
Educational Level: Undergraduate upper division
Formats: PDF
Type/Method: Directed
Language: English
Subject Headings: Medicinal Chemistry   Biochemistry   Cell Biology   Microbiology  
Date Posted: 11/29/2019
Date Modified: N/A
Copyright: Copyright held by the National Center for Case Study Teaching in Science, University at Buffalo, State University of New York. Please see our usage guidelines, which outline our policy concerning permissible reproduction of this work.

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