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Literature summary for 3.6.1.54 extracted from

  • Lee, M.; Zhao, J.; Kwak, S.H.; Cho, J.; Lee, M.; Gillespie, R.A.; Kwon, D.Y.; Lee, H.; Park, H.J.; Wu, Q.; Zhou, P.; Hong, J.
    Structure-activity relationship of sulfonyl piperazine LpxH inhibitors analyzed by an LpxE-coupled malachite green assay (2019), ACS Infect. Dis., 5, 641-651 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.6.1.54

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3)Star cells Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
1-(5-[4-[3-(propan-2-yl)phenyl]piperazine-1-carbonyl]-2,3-dihydro-1H-indol-1-yl)ethan-1-one 29% residual activity at 0.01 mM Escherichia coli
1-(5-[4-[3-(trifluoromethyl)phenyl]-1,4-diazepane-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl)ethan-1-one 94% residual activity at 0.01 mM Escherichia coli
1-(5-[4-[3-(trifluoromethyl)phenyl]piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl)ethan-1-one 6.0% residual activity at 0.01 mM Escherichia coli
1-[5-(4-phenylpiperazine-1-sulfonyl)-2,3-dihydro-1H-indol-1-yl]ethan-1-one 32% residual activity at 0.01 mM Escherichia coli
1-[5-(4-[[3-(trifluoromethyl)phenyl]methyl]piperazine-1-carbonyl)-2,3-dihydro-1H-indol-1-yl]ethan-1-one 87% residual activity at 0.01 mM Escherichia coli
1-[5-[4-(3-bromophenyl)piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl]ethan-1-one 24% residual activity at 0.01 mM Escherichia coli
1-[5-[4-(3-ethylphenyl)piperazine-1-carbonyl]-2,3-dihydro-1H-indol-1-yl]ethan-1-one 21% residual activity at 0.01 mM Escherichia coli
1-[5-[4-(3-hydroxyphenyl)piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl]ethan-1-one 91% residual activity at 0.01 mM Escherichia coli
1-[5-[4-([1,1'-biphenyl]-3-yl)piperazine-1-carbonyl]-2,3-dihydro-1H-indol-1-yl]ethan-1-one 24% residual activity at 0.01 mM Escherichia coli
2-oxo-2-((4-((4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)sulfonyl)phenyl)amino)acetic acid 55% residual activity at 0.01 mM Escherichia coli
3-[4-[3-(trifluoromethyl)phenyl]piperazine-1-sulfonyl]benzoic acid 98% residual activity at 0.01 mM Escherichia coli
4-[5-[4-(3-bromophenyl)piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl]-4-oxobutanoic acid 24% residual activity at 0.01 mM Escherichia coli
methyl 4-[5-[4-(3-bromophenyl)piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl]-4-oxobutanoate 42% residual activity at 0.01 mM Escherichia coli
N-(4-((4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)sulfonyl)phenyl)acetamide 36% residual activity at 0.01 mM Escherichia coli
N-(4-[4-[3-(trifluoromethyl)phenyl]piperazine-1-sulfonyl]phenyl)acetamide 30% residual activity at 0.01 mM Escherichia coli
N1-hydroxy-N2-(4-((4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)sulfonyl)phenyl)oxalamide 41% residual activity at 0.01 mM Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
UDP-2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosamine + H2O Escherichia coli
-
 2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosaminyl 1-phosphate + UMP
-
 ?

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
UDP-2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosamine + H2O
-
 Escherichia coli 2-N,3-O-bis[(3R)-3-hydroxytetradecanoyl]-alpha-D-glucosaminyl 1-phosphate + UMP
-
 ?

Synonyms

Synonyms Comment Organism
LpxH
-
 Escherichia coli
UDP-2,3-diacylglucosamine pyrophosphatase
-
 Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000147
-
 at pH 8.0 and 37°C Escherichia coli 1-(5-[4-[3-(trifluoromethyl)phenyl]piperazine-1-sulfonyl]-2,3-dihydro-1H-indol-1-yl)ethan-1-one