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Literature summary for 1.8.1.B1 extracted from

  • Sayed, A.A.; Simeonov, A.; Thomas, C.J.; Inglese, J.; Austin, C.P.; Williams, D.L.
    Identification of oxadiazoles as new drug leads for the control of schistosomiasis (2008), Nat. Med., 14, 407-412.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.8.1.B1

Application

Application Comment Organism
medicine identification of oxadiazole 2-oxides (TGR inhibitors) as new lead compounds for schistosomiasis chemotherapy Schistosoma mansoni

Inhibitors

Inhibitors Comment Organism Structure
(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-furylmethanone)
-
 Schistosoma mansoni
(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-thienylmethanone)
-
 Schistosoma mansoni
(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(1,3-dimethyl-1H-pyrazol-4-yl)methanone]
-
 Schistosoma mansoni
(2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(4-methoxyphenyl)methanone]
-
 Schistosoma mansoni
4-phenyl-1,2,5-oxadiazole-3-carbonitrile 2-oxide
-
 Schistosoma mansoni
P-1,3-benzothiazol-2-yl-N-(2-fluorophenyl)-P-phenylphosphinic amide
-
 Schistosoma mansoni
P-1,3-benzothiazol-2-yl-N-(5-chloropyridin-2-yl)-P-phenylphosphinic amide
-
 Schistosoma mansoni
P-1,3-benzothiazol-2-yl-P-phenyl-N-1,3-thiazol-2-ylphosphinic amide
-
 Schistosoma mansoni

Organism

Organism UniProt Comment Textmining
Schistosoma mansoni
-
-
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000212
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-P-phenyl-N-1,3-thiazol-2-ylphosphinic amide
0.000038
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-furylmethanone)
0.000042
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-thienylmethanone)
0.000082
-
 pH 7, glutathione reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-furylmethanone)
0.000105
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(4-methoxyphenyl)methanone]
0.000121
-
 pH 7, glutathione reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-P-phenyl-N-1,3-thiazol-2-ylphosphinic amide
0.00032
-
 pH 7, glutathione reductase activity Schistosoma mansoni 4-phenyl-1,2,5-oxadiazole-3-carbonitrile 2-oxide
0.00051
-
 pH 7, glutathione reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis(2-thienylmethanone)
0.000789
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-N-(5-chloropyridin-2-yl)-P-phenylphosphinic amide
0.00129
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(1,3-dimethyl-1H-pyrazol-4-yl)methanone]
0.00154
-
 pH 7, glutathione reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-N-(5-chloropyridin-2-yl)-P-phenylphosphinic amide
0.00167
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni 4-phenyl-1,2,5-oxadiazole-3-carbonitrile 2-oxide
0.00244
-
 pH 7, glutathione reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(4-methoxyphenyl)methanone]
0.00408
-
 pH 7, glutathione reductase activity Schistosoma mansoni (2-oxido-1,2,5-oxadiazole-3,4-diyl)bis[(1,3-dimethyl-1H-pyrazol-4-yl)methanone]
0.0151
-
 pH 7, thioredoxin reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-N-(2-fluorophenyl)-P-phenylphosphinic amide
0.0203
-
 pH 7, glutathione reductase activity Schistosoma mansoni P-1,3-benzothiazol-2-yl-N-(2-fluorophenyl)-P-phenylphosphinic amide