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ACE Inhibitors: Structure-Activity Relationship

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ACE Inhibitors: Structure-Activity Relationship

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@FavoriteBodhran8492

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Questions and Answers

What is the function of the COOH group in the N-ring of ACE inhibitors?

To improve oral bioavailability via esterification

To act as a zinc-binding site

To enhance the hydrophobicity of the molecule

To mimic the C-terminal COOH of Angiotensin I (correct)

Which of the following statements regarding zinc binding in ACE inhibitors is true?

SH groups can lead to adverse effects while being favorable for binding. (correct)

COOH groups hinder the binding to zinc.

Zinc binding requires only hydrophobic groups.

The zinc-binding group is unrelated to the chemical structure.

How does esterification affect ACE inhibitors?

It decreases water solubility and increases toxicity.

It alters the stereochemistry of the compound.

It improves oral bioavailability. (correct)

It converts them into inactive forms.

Which structural feature is essential for mimicking the amino acid Phenylalanine in ACE inhibitors?

<p>Hydrophobic heterocyclic rings</p> Signup and view all the answers

What is the common substitution found in the structure of ACE inhibitors?

<p>Methyl groups</p> Signup and view all the answers

Study Notes

Structure-Activity Relationship of ACE Inhibitors

ACE inhibitors (ACEi) mimic the structure of Angiotensin I, specifically the C-terminal COOH group.
Large hydrophobic heterocyclic rings in the N-ring of ACEi contribute to their potency and permeability.
Specific functional groups, like SH, COOH, or POOH, are crucial for binding zinc in ACEi.
SH groups are effective for zinc binding but can cause skin rash and taste disturbances.
ACEi mimic the amino acid Phenylalanine (Phe) and the peptide hydrolysis transition state, compensating for the absence of an SH group in some ACEis.
Esterification of COOH or POOH groups in ACEi creates prodrugs, enhancing oral bioavailability.
Methyl groups are frequently used as substitutions in the ACEi structure.
The stereochemistry of ACEi conforms to L-amino acids, reflecting their natural occurrences.

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Description

This quiz explores the structure-activity relationship (SAR) of ACE inhibitors, focusing on key structural features that enhance their potency and bioavailability. It covers specific functional groups important for zinc binding and the significance of stereochemistry in mimicking natural compounds. Test your knowledge on the intricate chemistry behind these vital medications.