STUDY ON DERIVATIVES OF 5-AMINO-4-ACYLAMINO-1H-PYRAZOLE AS INHIBITORS OF FURIN
1Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Kyiv;
2Palladin Institute of Biochemistry, National Academy of Sciences of Ukraine, Kyiv
A series of 5-amino-1H-pyrazoles was synthesized and studied as inhibitors of furin. The most potent compound, 5-amino-4-acetylamino-3-(4-methylphenylamino)-1H-pyrazole, was found to retard the activity of furin by mixed-type inhibition with Ki = 288 ?М. These findings permit to plan new ways for chemical modifications of the 5-amino-1H-pyrazole structure and design more potent furin inhibitors of non-peptide nature.
Key words: furin, inhibitors of furin, derivatives of 5-amino-1H-pyrazole.
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