Fighting Tuberculosis in an Undergraduate Laboratory: Synthesizing, Evaluating and Analyzing Inhibitors

• David Daniels ^[1] ; Charlotte Berkes ^[1] ; Arjan Nekoie ^[1] ; Jimmy Franco ^[1]
  1. [1] Merrimack College

     Merrimack College

     Town of North Andover, Estados Unidos

     
• Localización: Journal of chemical education, ISSN 0021-9584, Vol. 92, Nº 5, 2015, págs. 928-931
• Idioma: inglés
• Texto completo no disponible (Saber más ...)
• Resumen

  • A drug discovery project has been successfully implemented in a first-year general, organic, and biochemistry (GOB) health science course and second-year organic undergraduate chemistry course. This project allows students to apply the fundamental principles of chemistry and biology to a problem of medical significance, practice basic laboratory skills, and understand the interdisciplinary aspect of the drug discovery platform. Students collectively synthesize a small library of antituberculosis compounds and subsequently screen them using a Kirby–Bauer disc diffusion assay for inhibitory activity against Mycobacterium smegmatis, a known safe surrogate of Mycobacterium tuberculosis, the causative agent of tuberculosis. The last unit of the project involves students using PyMOL, a free computer program, to examine a cocrystal structure of the activated inhibitor–enzyme complex, allowing students to identify the molecular interactions responsible for the binding affinity.