Posted: December 21st, 2015

For each transformation name the enzyme system(s) likely to have mediated the transformation, their subcellular location and co-factor requirements.

Question 2:

Drug X, structure shown below, has a molecular weight of 257, a calculated Log P value of 2.4 and a pKa of 9.5, undergoes hepatic metabolism to yield a variety of Phase I and II metabolites.

• Draw the chemical structures of five potential metabolites of drug.

• Name the type of metabolic transformation that the drug, or a metabolite of the drug, has undergone for each metabolic route you have indicated.

(20% Marks)

• For each transformation name the enzyme system(s) likely to have mediated the transformation, their subcellular location and co-factor requirements.

(20% Marks)

• Comment on the alteration in the physicochemical properties of the metabolites compared to the drug and explain how the structural modifications involved influence the excretion of drug related material from the body.