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Literature summary for 3.5.1.5 extracted from

  • Rauf, A.; Liaqat, S.; Qureshi, A.; Yaqub, M.; Rehman, A.; Hassan, M.; Chohan, Z.; Nasim, F.; Hadda, T.
    Synthesis, characterization, and urease inhibition of 5-substituted-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-diones (2012), Med. Chem. Res., 21, 60-74.
No PubMed abstract available

Inhibitors

Inhibitors Comment Organism Structure
3-[(2-acetylanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]-pyrimidine-2,4-dione 54% inhibition at 0.01 mM Canavalia ensiformis
3-[(2-fluoroanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]-pyrimidine-2,4-dione 44% inhibition at 0.01 mM Canavalia ensiformis
3-[(3-acetylanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]-pyrimidine-2,4-dione 28% inhibition at 0.01 mM Canavalia ensiformis
3-[(3-fluoroanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]-pyrimidine-2,4-dione 3% inhibition at 0.01 mM Canavalia ensiformis
3-[(4-acetylanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4-dione 5% inhibition at 0.01 mM Canavalia ensiformis
3-[(4-fluoroanilino)methylidene]-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4-dione 21% inhibition at 0.01 mM Canavalia ensiformis
3-[(mesitylamino)methylidene]-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4-dione
-
Canavalia ensiformis
4-bromo-N'-[[8-methyl-2,4-dioxo-2H-pyrido[1,2-a]pyrimidin-3(4H)-ylidene]methyl]benzohydrazide 23% inhibition at 0.01 mM Canavalia ensiformis
4-chloro-N'-[[8-methyl-2,4-dioxo-2H-pyrido[1,2-a]pyrimidin-3(4H)-ylidene]methyl]benzohydrazide 14% inhibition at 0.01 mM Canavalia ensiformis
4-hydroxy-N'-[[8-methyl-2,4-dioxo-2H-pyrido[1,2-a]pyrimidin-3(4H)-ylidene]methyl]benzohydrazide 22% inhibition at 0.01 mM Canavalia ensiformis
4-nitro-N'-[[8-methyl-2,4-dioxo-2H-pyrido[1,2-a]pyrimidin-3(4H)-ylidene]methyl] benzohydrazide 60% inhibition at 0.01 mM Canavalia ensiformis
8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione 26% inhibition at 0.01 mM Canavalia ensiformis
8-methyl-3-[(2-sulfanylanilino)methylidene]-2H-pyrido[1,2-a]pyrimidine-2,4-dione 73% inhibition at 0.01 mM Canavalia ensiformis
8-methyl-3-[[(4-methyl-2-pyridinyl)amino]methylidene]-2Hpyrido[1,2-]pyrimidine-2,4-dione 20% inhibition at 0.01 mM Canavalia ensiformis
8-methyl-3-[[(5-methyl-2-pyridinyl)amino] methylidene]-2H-pyrido[1,2-]pyrimidine-2,4-dione 48% inhibition at 0.01 mM Canavalia ensiformis
8-methyl-3-[[(5-nitro-2-pyridinyl)amino] methylidene]-2H-pyrido[1,2-a]pyrimidine-2,4-dione 36% inhibition at 0.01 mM Canavalia ensiformis
additional information synthesis, characterization, and urease inhibition of 5-substituted-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-diones, anilines, amino pyridines and hydrazides derivatives, detailed overview. No inhibition by 5 Canavalia ensiformis
N'-[[8-methyl-2,4-dioxo-2H-pyrido[1,2-a]pyrimidin-3(4H)-ylidene]methyl]-benzo-hydrazide 13% inhibition at 0.01 mM Canavalia ensiformis
Thiourea 21% inhibition at 0.01 mM Canavalia ensiformis

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
urea + H2O Canavalia ensiformis
-
CO2 + 2 NH3
-
?

Organism

Organism UniProt Comment Textmining
Canavalia ensiformis P07374
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
urea + H2O
-
Canavalia ensiformis CO2 + 2 NH3
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Canavalia ensiformis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.021
-
pH not specified in the publication, 25°C Canavalia ensiformis 8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-dione