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Justification - Justification Sulfonamides The history of...

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Justification – Sulfonamides The history of the use of the Sulfonamides started with the discovery of prontosil and extended based on its antibacterial properties. Prontosil was metabolised by bacteria in small intestines to give these sulphonamides. This is demonstrated in figure one below. Figure 1. The mechanistic action of drugs competes with the enzyme inhibitors of dihydropleroate synthetise and blocks the biosynthesis of tetrahyfrofolate in bacteria cells. The sulfonamides themselves do not kill the bacteria cells but instead prevent the cells from growing/multiplying allowing the body to react naturally with its own defence system. They mimic p-aminobenzoic acid (PABA) to compete. This reaction is reversible. Structure activity relationship is an important parameter to the development of medicine. This experiment takes the molecule in figure two and alternates the R groups to assess the biological activity of the derivatives. Figure 2. The p-amino group in figure two is essential for the activity of the molecule. It must be unsubstituted (H) unless when substituted for an acyl group so that a reaction can occur in the stomach. The core
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