a- Identify promising properties of a as a lead compound. b- What was the benefi

Question

a- Identify promising properties of a as a lead compound. b- What was the benefit of adding the amide? c- What might the function of the methyl group added in c be? d- What physical property and pharmacokinetic advantage would you achieve by adding the group shown in d? a- Identify promising properties of a as a lead compound. b- What was the benefit of adding the amide? c- What might the function of the methyl group added in c be? d- What physical property and pharmacokinetic advantage would you achieve by adding the group shown in d?

Explanation / Answer

a) Promising properties of a as a lead compound

-low molecular weight

-low clogP

-has potential for diversity using simple chemistry.

b) Addition of amide group provided inhibitory activity against BCR–ABL tyrosine kinase.

c) A flag methyl group abolishes the undesirable protein-kinase-C inhibitory activity.

d) The attachment of an N-methyl piperazine moiety improves the solubility and oral bioavailability.

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