LpxH-IN-AZ1, a sulfonyl piperazine compound, is a potent UDP-2,3-diacylglucosamine pyrophosphate drolase LpxH inhibitor. LpxH-IN-AZ1 is a potent inhibitor of Klebsiella pneumoniae LpxH with IC50 of 0.36 μM [1].
LpxH-IN-AZ1 displays IC50 values of 0.36 μM against K. pneumoniae LpxH and 0.14 μM against E. coli LpxH, respectively[1].
LpxH-IN-AZ1 (1 μM) inhibits 75% of the activity of K. pneumoniae LpxH and 83% of the activity of E. coli LpxH in the presence of 100 μM UDPDAGn[1].
[1]. Cho J, et al. Structural basis of the UDP-diacylglucosamine pyrophosphodrolase LpxH inhibition by sulfonyl piperazine antibiotics. Proc Natl Acad Sci U S A. 2020 Feb 25;117(8):4109-4116.