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Explain in detail where drug is converted to prodrug to mask toxicity and side effects considering...

Explain in detail where drug is converted to prodrug to mask toxicity and side effects considering L-lysyl diazepam (LDZ) as an example (Scheme should be drawn).

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Answer #1

LDZ is a prodrug of Diazepam to avoid drowsy side effects of the active drug.

LDZ with the help of aminopeptidase enzyme and further cyclization is converted into Diazepam.

after entering into the bloodstream with the help of enzyme the lysine side chain is removed and free amine group is attacked on ketone group present on the aromatic ring and makes a transition state intermediate and further water is released from the intermediate. after that rearrangement of molecule takes place and proton is released and Diazepam is formed.

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