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Literature summary for 3.1.26.13 extracted from

  • Billamboz, M.; Bailly, F.; Lion, C.; Calmels, C.; Andreola, M.L.; Witvrouw, M.; Christ, F.; Debyser, Z.; De Luca, L.; Chimirri, A.; Cotelle, P.
    2-hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4 (2011), Eur. J. Med. Chem., 46, 535-546.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-hydroxy-4-(2-phenyl)ethylisoquinoline-1,3(2H,4H)-dione enol-form Human Immunodeficiency Virus
2-hydroxy-4-(3-phenyl)propylisoquinoline-1,3(2H,4H)-dione mixture of th mixed ketoenol forms or keto-form Human Immunodeficiency Virus
2-hydroxy-4-(4-methylbenzyl)isoquinoline-1,3(2H,4H)-dione mixture of th mixed ketoenol forms or keto-form Human Immunodeficiency Virus
2-hydroxy-4-(4-trifluoromethylbenzyl)isoquinoline-1,3(2H-4H)-dione keto-form Human Immunodeficiency Virus
2-hydroxy-4-butylisoquinoline-1,3(2H,4H)-dione mixture of th mixed ketoenol forms or keto-form Human Immunodeficiency Virus
2-hydroxy-4-ethylisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
2-hydroxy-4-isopropylisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
2-hydroxy-4-pentylisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
2-hydroxy-4-propylisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
Human Immunodeficiency Virus
4-benzyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione keto-form; mixture of th mixed ketoenol forms Human Immunodeficiency Virus
4-heptyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione enol form Human Immunodeficiency Virus
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione keto-form; mixture of th mixed ketoenol forms Human Immunodeficiency Virus
additional information synthesis of 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives as inhibitors of the RNase H activity of the reverse transcriptase of HIV-1, docking, study, overview. No inhibition by keto-5i and 5l Human Immunodeficiency Virus

Organism

Organism UniProt Comment Textmining
Human Immunodeficiency Virus
-
HIV-1
-

Synonyms

Synonyms Comment Organism
ribonuclease H
-
Human Immunodeficiency Virus
RNase H
-
Human Immunodeficiency Virus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0059
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxyisoquinoline-1,3(2H,4H)-dione
0.0078
-
pH 8.0, 37°C Human Immunodeficiency Virus 4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
0.0132
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-butylisoquinoline-1,3(2H,4H)-dione
0.0149
-
pH 8.0, 37°C Human Immunodeficiency Virus 4-benzyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
0.0185
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-isopropylisoquinoline-1,3(2H,4H)-dione
0.0336
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-pentylisoquinoline-1,3(2H,4H)-dione
0.038
-
pH 8.0, 37°C Human Immunodeficiency Virus 4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
0.0388
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-ethylisoquinoline-1,3(2H,4H)-dione
0.0427
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-(4-trifluoromethylbenzyl)isoquinoline-1,3(2H-4H)-dione
0.045
-
pH 8.0, 37°C Human Immunodeficiency Virus 4-heptyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
0.0468
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-propylisoquinoline-1,3(2H,4H)-dione
0.0668
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-(3-phenyl)propylisoquinoline-1,3(2H,4H)-dione
0.07
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-methylisoquinoline-1,3(2H,4H)-dione
0.08
-
pH 8.0, 37°C Human Immunodeficiency Virus 2-hydroxy-4-(4-methylbenzyl)isoquinoline-1,3(2H,4H)-dione