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4-(dihydroxyboranyl)-2-({[4-(phenylsulfonyl)thiophen-2-yl]sulfonyl}amino)benzoic acid

Development stage
Preclinical
Modality
Small Molecules
01

Overview

This compound is a synthetic small molecule belonging to the sulfanilide class, characterized by a benzoic acid core substituted with dihydroxyboranyl and sulfonamide groups. It was designed as an experimental inhibitor of AmpC beta-lactamase, an enzyme produced by certain bacteria (notably Escherichia coli), which confers resistance to beta-lactam antibiotics. Structural studies have shown that this boronic acid derivative binds covalently to the active site serine of AmpC beta-lactamase, acting as a potent inhibitor and serving as a lead compound for further development of antibiotic resistance modulators. The molecule has been studied primarily in vitro and in structural biology contexts; it is not approved for clinical use[1][5][8].

Other names
2-[4-(benzenesulfonyl)thiophene-2-sulfonamido]-4-(dihydroxyboranyl)benzoic acid4-(Dihydroxyboryl)-2-({[4-(phenylsulfonyl)-2-thienyl]sulfonyl}amino)benzoic acid
02

Targets

AmpC (AmpC beta-lactamase)

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