Chapter 8: Problem 15

The thiazole ring of 12 is metabolized to a toxic metabolite. Suggest two approaches you would take to prevent this toxicity.

Short Answer

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The two approaches to prevent the toxicity of the thiazole ring in compound 12 can be: 1) Modifying the thiazole ring in compound 12 to a safer substitute and 2) designing a competitive inhibitor that binds to the metabolizing enzyme instead of the drug to prevent its toxic metabolism.

Step by step solution

Understanding Toxic Metabolites

While metabolizing a drug, our body may convert it into different forms. Some of these might be toxic. This is the case for the thiazole ring in compound 12. Hence, we need to identify how we can prevent the production of such a toxic metabolite.

Identifying Strategy 1: Structural Modification

One common approach to prevent the production of toxic metabolites from the drug is by structural modifications of the drug. This can be achieved by replacing or modifying the thiazole ring in compound 12 to a safer substitute that either cannot form the toxic metabolite or is metabolized to a non-toxic product.

Identifying Strategy 2: Enzyme Inhibition

Another approach involves identifying the specific enzyme that metabolizes the thiazole ring into its toxic form and then designing a competitive inhibitor that can bind to this enzyme instead of the drug thus preventing its metabolism.

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The thiazole ring of 12 is metabolized to a toxic metabolite. Suggest two approaches you would take to prevent this toxicity.

Short Answer

Step by step solution

Understanding Toxic Metabolites

Identifying Strategy 1: Structural Modification

Identifying Strategy 2: Enzyme Inhibition

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