Question

Activity of aromatic ring with CYP450:

2. (2.3 points) Each of the drugs below contain 3 aromatic rings. (a) For ONE of the compounds, rank each ring as 1, 2, and 3, in order of their likelihood of undergoing a CYP-450 mediated oxidation, and briefly explain your answers. (b) Then draw an arrow to show the most likely site of oxidation in the most reactive ring. gorac -NO2 Br enclomiphene (antiestrogen) HO celecoxib-like (anti-inflammatory) CO2Na ОН CF3 IZ O=D=0 N iPr tripranavir (anticancer) atorvastatin-like (cholesterol lowerer)

Answer 1

Cytochrome P450 enzymes is a super family of enzymes involved in a drug metabolism and bioactivation. The most important role of this super family of enzymes is the breakdown of xenobiotics in humans. Xenobiotics are substances that we introduce in our body such as medicines and drugs that we intake.

Biggest role of cytochrome P450 enzyme is to turn the drugs into soluble molecules so that it can be excreted out properly.

The active site of cytochrome P450 contains the heme centre, specifically Heme B.

Heme B is the most abudant heme. It is also present in hemoglobins and myglobins.

Enclomiphene is used to treat female infertility. It binds the estrogen receptor and prevents binding of estrogen.