Identify likely Phase I metabolites for each of the following compounds, indicat
ID: 714201 • Letter: I
Question
Identify likely Phase I metabolites for each of the following compounds, indicating the class of enzyme carrying out the process.
Q4 Identify likely Phase I metabolites for each of the following compounds, indicating the class of enzyme carrying out the process CH3 CH3 CO2CH3 SCH3 NThioridazine (6 marks) Outline, by means of general equations, how conjugation with glycine is used to metabolise aromatic acids. Suggest a chemical reason for the product of this proces:s being readily excreted by the kidney (4 marks) Q6 Phenols are antiseptics. Consider a series of 4- substitued phenols OH (a)Using the tables found at the end of this assignment, calculate log P for the compounds where R= Me-, n-propyl-and MeO-( NB. log Pbenze ne-2.13) Show your working (b)The activity of these compounds appears to increase as they become more lipophilic. Propose at least two structural analogues of this compound that could be used to gain more insight into the relative importance of lipophilicity versus steric properties of the R groupExplanation / Answer
4. Thioridazine is a racemic compound with two enantiomers, by CYP2D6 into (S)- and (R)-thioridazine-2-sulfoxide, better known as mesoridazine,and into (S)- and (R)-thioridazine-5-sulfoxide. Mesoridazine is in turn metabolized into sulforidazine. Thioridazine is an inhibitor of CYP1A2 and CYP3A2
5. Glycine conjugation is a detoxification mechanisms by which it increases water solubility of acids, hence it will increase urinary excreation from the kidneys. Systemic levels of amino acids is regulated by amino acids conjugation particularly glycine conjugation. Glycine conjugation doesn’t increase water solubility to much extent in aromatic acids.
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