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Literature summary for 5.1.1.3 extracted from

  • De Jonge, B.; Kutschke, A.; Uria-Nickelsen, M.; Kamp, H.; Mills, S.
    Pyrazolopyrimidinediones are selective agents for Helicobacter pylori that suppress growth through inhibition of glutamate racemase (MurI) (2009), Antimicrob. Agents Chemother., 53, 3331-3336.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development inhibitors of glutamate racemase are potential targets as antibiotic agents against Helicobacter pylori Helicobacter pylori

Cloned(Commentary)

Cloned (Comment) Organism
construction of a glutamate racemase-overexpressing strain by transformation, recombinant strains Hp80.1 and Hp80.2 are constructed in the wild-type background of strain ARHp80 Helicobacter pylori

Inhibitors

Inhibitors Comment Organism Structure
5-methyl-7-(2-methylpropyl)-2-(naphthalen-1-ylmethyl)-3-pyridin-4-yl-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 4 microg/ml Helicobacter pylori
5-[2-[(6-chloro-1,2-dihydroquinolin-4-yl)methyl]-7-(cyclopropylmethyl)-5-methyl-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-3-yl]-1-methyl-1H-pyrrole-3-carbonitrile pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 1 and 0.5 microg/ml Helicobacter pylori
5-[7-(cyclopropylmethyl)-5-methyl-2-[(5-methyl-1H-indol-3-yl)methyl]-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-3-yl]-N-methoxy-1-methyl-1H-pyrrole-3-carboxamide pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 16 microg/ml Helicobacter pylori
6-chloro-4-([7-(cyclopropylmethyl)-5-methyl-3-[1-methyl-4-(methylsulfinyl)-1H-pyrrol-2-yl]-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl]methyl)isoquinoline-3-carbonitrile pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 16 and 8 microg/ml Helicobacter pylori
6-chloro-4-[[3-(4-cyano-1-methyl-1H-pyrrol-2-yl)-7-(cyclopropylmethyl)-4,6-dioxo-5-prop-2-yn-1-yl-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl]methyl]isoquinoline-3-carbonitrile pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 2 and 1 microg/ml Helicobacter pylori
tetracycline inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 0.25 and 0.13 microg/ml Helicobacter pylori
[2-[(6-chloro-1,2-dihydroquinolin-4-yl)methyl]-7-(cyclopropylmethyl)-3-(1-methyl-1H-imidazol-5-yl)-4,6-dioxo-2,4,6,7-tetrahydro-5H-pyrazolo[3,4-d]pyrimidin-5-yl]acetonitrile pyrazolopyrimidinedione inhibits growth of Helicobacter pylori specifically, inhibition of enzyme results in inhibition of peptidoglycan biosynthesis, minimum inhibitory concentration in wild-type strains SS1 and ARHp80 is 2 and 1 microg/ml Helicobacter pylori

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-glutamate Helicobacter pylori
-
D-glutamate
-
?

Organism

Organism UniProt Comment Textmining
Helicobacter pylori
-
J-99 strain, ARHp80 strain and SS1 strain
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-glutamate
-
Helicobacter pylori D-glutamate
-
?

Synonyms

Synonyms Comment Organism
glutamate racemase
-
Helicobacter pylori
MurI
-
Helicobacter pylori

General Information

General Information Comment Organism
physiological function essential enzyme in peptidoglycan biosynthesis Helicobacter pylori