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Literature summary for 2.5.1.58 extracted from

  • Olepu, S.; Suryadevara, P.K.; Rivas, K.; Yokoyama, K.; Verlinde, C.L.; Chakrabarti, D.; Van Voorhis, W.C.; Gelb, M.H.
    2-Oxo-tetrahydro-1,8-naphthyridines as selective inhibitors of malarial protein farnesyltransferase and as anti-malarials (2008), Bioorg. Med. Chem. Lett., 18, 494-497.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 98% inhibition at 500 nM Plasmodium falciparum
methyl 4-[([6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl][(1-methyl-1H-imidazol-4-yl)sulfonyl]amino)methyl]piperidine-1-carboxylate 85% inhibition at 0.005 mM Rattus norvegicus
N-[6-bromo-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 74% inhibition at 500 nM Plasmodium falciparum
N-[6-bromo-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 51% inhibition at 0.005 mM Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 94% inhibition at 500 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-1H-imidazole-4-sulfonamide 39% inhibition at 0.005 mM Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-imidazole-4-sulfonamide 99% inhibition at 500 nM Plasmodium falciparum
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1-methyl-N-[4-(methylsulfonyl)benzyl]-1H-imidazole-4-sulfonamide 47% inhibition at 0.005 mM Rattus norvegicus
N-[6-cyano-1-[(1-methyl-1H-imidazol-5-yl)methyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-N-[4-(methylsulfonyl)benzyl]pyridine-2-sulfonamide 91% inhibition at 500 nM Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
farnesyl diphosphate + protein-cysteine
-
 Rattus norvegicus diphosphate + S-farnesyl protein
-
 ?
farnesyl diphosphate + protein-cysteine
-
 Plasmodium falciparum diphosphate + S-farnesyl protein
-
 ?

Synonyms

Synonyms Comment Organism
PFT
-
 Rattus norvegicus
PFT
-
 Plasmodium falciparum