Drug intelligence / Profile preview

CHIR-090

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Experimental Only; Not Established For Clinical Use
01

Overview

CHIR-090 is a synthetic small molecule inhibitor of the enzyme UDP-3-O-acyl-N-acetylglucosamine deacetylase (LpxC), which is essential for lipopolysaccharide (LPS) biosynthesis in Gram-negative bacteria. By inhibiting LpxC, CHIR-090 disrupts the production of LPS—a critical component of the outer membrane—leading to bacterial cell death. This mechanism makes it a potent experimental antibacterial agent targeting Gram-negative pathogens. The compound is an acetylenic benzamide derivative with morpholine and hydroxamic acid functional groups and has been studied primarily in preclinical research as a tool compound for validating LpxC as an antibiotic target[3][8].

Other names
N-{(1S,2R)-2-hydroxy-1-[(hydroxyamino)carbonyl]propyl}-4-{[4-(morpholin-4-ylmethyl)phenyl]ethynyl}benzamide(2S,3R)-N,3-dihydroxy-2-{[4-(2-{4-[(morpholin-4-yl)methyl]phenyl}ethynyl)phenyl]formamido}butanamide
02

Targets

LpxC (UDP-3-O-[3-hydroxymyristoyl] N-acetylglucosamine Deacetylase)

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