Journal archive > 2011 > N 1 January-February

STUDY ON DERIVATIVES OF 5-AMINO-4-ACYLAMINO-1H-PYRAZOLE AS INHIBITORS OF FURIN

V. K. Kibirev1, T. V. Osadchuk1, O. B. Vadzyuk2, O. V. Shablykin1, O. P. Kozachenko1,
S. A. Chumachenko1, S. V. Popilnichenko1, V. S. Brovarets1

1Institute of Bioorganic Chemistry and Petrochemistry, National Academy of Sciences of Ukraine, Kyiv;
е-mail: This email address is being protected from spambots. You need JavaScript enabled to view it.;
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.

The original article in Russian is available for download in PDF format.

 

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