[The use of enzymes for searching for biologically active compounds].
Possible use of extracellular staphylococcal DNAase in screening substances with potential antibacterial activity was studied on quinoxalin as an example. For screening substances with antiviral activity the possible use of the influenza virus neuraminidase was studied on fluoren as an example. Close correlation between the biological activity of quinoxalin derivatives and the ability to inhibit DNAase was revealed. The most active inhibitors of the enzyme were dioxidin and other biologically active analogs of quinoxalin 1,4-di-N-oxide. The use of the extracellular nuclease as a biochemical model permitted to establish the structure/function dependence with respect to the quinoxalin derivatives. The effect of the fluoren derivatives on activity of the influenza virus neuramididase was studied. It was shown that florenal, an antiviral drug inhibited the virus specific enzyme by 80 to 90 per cent and had no effect on catalytic activity of bacterial neuraminidase. Biologically inactive and slightly active derivatives of the compounds did not inhibit the influenza virus enzyme. At the same time some of them lowered the activity of the bacterial enzyme.
Fadeeva
N I
NI
Degtiareva
I N
IN
Gerasina
S F
SF
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology*; D003851:Deoxyribonucleases / Q000037:antagonists & inhibitors / Q000302:isolation & purification; D005449:Fluorenes / Q000494:pharmacology; D009980:Influenza A virus / Q000201:enzymology*; D009439:Neuraminidase / Q000037:antagonists & inhibitors / Q000302:isolation & purification; D011810:Quinoxalines / Q000494:pharmacology; D013210:Staphylococcus / Q000201:enzymology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D000998:Antiviral Agents; D005449:Fluorenes; D011810:Quinoxalines; D003851:Deoxyribonucleases; D009439:Neuraminidase
Ispol'zovanie fermentov dlia poiska biologicheski aktivnykh soedineniĭ.