Drug intelligence / Profile preview

1(R)-1-acetamido-2-(3-carboxyphenyl)ethyl boronic acid

Development stage
Preclinical
Modality
Light/Condition-Responsive Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
01

Overview

1(R)-1-acetamido-2-(3-carboxyphenyl)ethyl boronic acid is a synthetic small molecule and organoboron compound. It is structurally characterized by an acetamido group, a carboxy-substituted phenyl ring, and a boronic acid moiety. This compound has been studied primarily as an experimental inhibitor of β-lactamase enzymes, particularly TEM-type β-lactamases in bacteria. By mimicking the transition state of the enzyme's natural substrate, it acts as a competitive inhibitor at the active site of β-lactamase, potentially restoring the efficacy of β-lactam antibiotics against resistant bacterial strains[5][7]. The compound remains experimental with no approved clinical indications.

Other names
3-[(2R)-2-acetamido-2-(dihydroxyboryl)ethyl]benzoic acidBenzoic acid, 3-[(2R)-2-(acetylamino)-2-boronoethyl]-Acide 3-[(2R)-2-acétamido-2-(dihydroxyboryl)éthyl]benzoïque (French)
02

Targets

CD248 (Endosialin)

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