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Literature summary for 1.8.1.B1 extracted from

  • Tripathi, T.; Chetri, P.B.
    Potent inhibitors of thioredoxin glutathione reductase grail of anti-Schistosome drug within reach? (2020), ACS Infect. Dis., 6, 893-895 .
    View publication on PubMed
Search for more literature for 1.8.1.B1

Inhibitors

Inhibitors Comment Organism Structure
1,3,4-oxadiazole-2-sulfone shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma haematobium
1,3,4-oxadiazole-2-sulfone shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma japonicum
1,3,4-oxadiazole-2-sulfone shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma mansoni
2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration Schistosoma haematobium
2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration Schistosoma japonicum
2-((4-chlorophenyl)sulfonal)-6-methoxy-3-nitropyridine shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. Kills schistosomes within 1 h of administration Schistosoma mansoni
6-nitrobenzo[b]thiophene-1,1-dioxide shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma haematobium
6-nitrobenzo[b]thiophene-1,1-dioxide shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma japonicum
6-nitrobenzo[b]thiophene-1,1-dioxide shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma mansoni
pyrazine-3-one shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma haematobium
pyrazine-3-one shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma japonicum
pyrazine-3-one shows potent schistomicidal activity (LD50 above 0.01 mM) against Schistosoma mansoni, Schistosoma japonicum and Schistosoma hematobium, particularly against immature flukes. The compounds exceeds the standard set by WHO for antischistosome lead compounds. Kills schistosomes within 1 h of administration Schistosoma mansoni

Metals/Ions

Metals/Ions Comment Organism Structure
selenium selenoenzyme Schistosoma mansoni
selenium selenoenzyme Schistosoma japonicum
selenium selenoenzyme Schistosoma haematobium

Organism

Organism UniProt Comment Textmining
Schistosoma haematobium
-
-
-
Schistosoma japonicum
-
-
-
Schistosoma mansoni
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione disulfide + NADPH + H+
-
 Schistosoma mansoni 2 glutathione + NADP+
-
 ?
glutathione disulfide + NADPH + H+
-
 Schistosoma japonicum 2 glutathione + NADP+
-
 ?
glutathione disulfide + NADPH + H+
-
 Schistosoma haematobium 2 glutathione + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+
-
 Schistosoma mansoni thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+
-
 Schistosoma japonicum thioredoxin + NADP+
-
 ?
thioredoxin disulfide + NADPH + H+
-
 Schistosoma haematobium thioredoxin + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
TGR
-
 Schistosoma mansoni
TGR
-
 Schistosoma japonicum
TGR
-
 Schistosoma haematobium
thioredoxin glutathione reductase
-
 Schistosoma mansoni
thioredoxin glutathione reductase
-
 Schistosoma japonicum
thioredoxin glutathione reductase
-
 Schistosoma haematobium

General Information

General Information Comment Organism
drug target the enzyme is a promising drug target, as this enzyme is parasite-specific and absent in their host. A study identifies compounds with extremely potent antischistosome activity. Certain compounds are active against all major schistosomes across different life cycle stages Schistosoma mansoni
drug target the enzyme is a promising drug target, as this enzyme is parasite-specific and absent in their host. A study identifies compounds with extremely potent antischistosome activity. Certain compounds are active against all major schistosomes across different life cycle stages Schistosoma japonicum
drug target the enzyme is a promising drug target, as this enzyme is parasite-specific and absent in their host. A study identifies compounds with extremely potent antischistosome activity. Certain compounds are active against all major schistosomes across different life cycle stages Schistosoma haematobium
physiological function under redox pressure, schistosomes survive in mammalian hosts with the help of thioredoxin glutathione reductase Schistosoma mansoni
physiological function under redox pressure, schistosomes survive in mammalian hosts with the help of thioredoxin glutathione reductase Schistosoma japonicum
physiological function under redox pressure, schistosomes survive in mammalian hosts with the help of thioredoxin glutathione reductase Schistosoma haematobium