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Literature summary extracted from

  • Suganuma, K.; Sarwono, A.E.; Mitsuhashi, S.; J?kalski, M.; Okada, T.; Nthatisi, M.; Yamagishi, J.; Ubukata, M.; Inoue, N.
    Mycophenolic acid and its derivatives as potential chemotherapeutic agents targeting inosine monophosphate dehydrogenase in Trypanosoma congolense (2016), Antimicrob. Agents Chemother., 60, 4391-4393.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide 14.50% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide 4.59% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1,3,4-thiadiazol-2-yl)hex-4-enamide 29.44% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide 46.13% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide 98.87% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-1,2,4-triazol-5-yl)hex-4-enamide 42.79% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide 22.99% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide 3.59% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(1H-tetrazol-5-yl)hex-4-enamide 19.94% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide 14.29% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide 4.65% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(4H-1,2,4-triazol-4-yl)hex-4-enamide 32.43% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide 7.83% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide 2.36% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(pyridin-2-yl)hex-4-enamide 16.66% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide 22.27% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide 1.45% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methyl-N-(thiazol-2-yl)hex-4-enamide 17.11% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid 11.56% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid 3.03% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioic S-acid 13.61% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide 5.24% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide 94.46% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (E)-N-hydroxy-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enamide 14.21% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 9.03% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 3.15% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (R,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 9.49% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 (S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 9.28% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 (S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 0.06% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 (S,E)-7-hydroxy-5-methoxy-4-methyl-6-(3-methyl-6-(oxiran-2-yl)-6-oxohex-2-en-1-yl)isobenzofuran-1(3H)-one 11.99% inhibition at 0.001 mg Trypanosoma evansi
1.1.1.205 Mycophenolic acid 82.99% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity Trypanosoma brucei brucei
1.1.1.205 Mycophenolic acid 99.60% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity Trypanosoma congolense
1.1.1.205 Mycophenolic acid 90.53% inhibition at 0.001 mg, inhibits the enzyme activity and leads to complete inhibition of proliferation of Trypanosoma at below 0.001 mM. Mycophenolic acid derivatives can act as trypanocidal drugs with trypanocidal activity Trypanosoma evansi
1.1.1.205 Pentamidine complete inhibition at 500 ng/ml Trypanosoma brucei brucei
1.1.1.205 Pentamidine complete inhibition at 500 ng/ml Trypanosoma congolense
1.1.1.205 Pentamidine complete inhibition at 500 ng/ml Trypanosoma evansi
1.1.1.205 S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate 16.47% inhibition at 0.001 mg Trypanosoma brucei brucei
1.1.1.205 S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate 6.51% inhibition at 0.001 mg Trypanosoma congolense
1.1.1.205 S-(prop-1-en-2-yl) (E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enethioate 12.79% inhibition at 0.001 mg Trypanosoma evansi

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.205 Trypanosoma brucei brucei P50098
-
-
1.1.1.205 Trypanosoma brucei brucei GUTat3.1 P50098
-
-
1.1.1.205 Trypanosoma congolense A0A0S3MSA1
-
-
1.1.1.205 Trypanosoma congolense IL3000 A0A0S3MSA1
-
-
1.1.1.205 Trypanosoma evansi
-
-
-
1.1.1.205 Trypanosoma evansi Tansui
-
-
-

Synonyms

EC Number Synonyms Comment Organism
1.1.1.205 IMP dehydrogenase
-
 Trypanosoma evansi
1.1.1.205 IMP dehydrogenase
-
 Trypanosoma congolense
1.1.1.205 IMP dehydrogenase
-
 Trypanosoma brucei brucei