CHEM 437 Chapter Notes - Chapter 2: Ic50, Pharmacophore, Wyeth
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List and describe the processes in the gut that contribute to a drugs bioavailability. Give examples where possible of how they can be optimized by a chemist. (10) Chemist can optimize the drugs bioavailability to make it easier for passive di usion by: Add more hydrophobic polarizable groups instead of co2h. Decreasing mw helps or decreasing nrot: recall that the key di erence between era and erb has a residue ile373 exactly where era has a residue. Use arguments based on structure, pharmacophores, and weak interactions to explain these observations. Methionine has a sulfur atom, which, interacts favourably with i because they are both polarizable and have similar energies. Methionine doesn"t interact well with cn- because it is negatively charged and s has a lone pair. Methionine is larger than isoleucine and cn is larger than i, therefore more room for cn with isoleucine.
