TY - JOUR
T1 - Inhibition of neuraminidase activity by derivatives of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid
AU - Meindl, P.
AU - Bodo, G.
AU - Palese, P.
AU - Schulman, J.
AU - Tuppy, H.
N1 - Funding Information:
Part of this investigation was conducted under the auspices of the Commission on Influenza of the Armed Forces Epidemiological Board, and was supported (in part) by the U.S. Army Medical Research Development Command under research No. DADA17-69-C-9137, by Public research Grant No. A109304 from Institute of Allergy and Infectious and by contract U-2076 from the Research Council City New York.
PY - 1974/4
Y1 - 1974/4
N2 - Eighteen derivatives of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid were assayed for inhibitory activity against neuraminidases from viral and bacterial sources. Twelve of these compounds were active against neuraminidases of Vibrio cholerae, influenza A Mel, B Lee, and Newcastle disease virus, causing 50% enzyme inhibition in concentrations ranging from 10-3 M to 10-6 M. The most active of them and the most potent neuraminidase inhibitor described so far is 2-deoxy-2,3-dehydro-N-trifluoroacetylneuraminic acid. This compound has an inhibitor constant (Ki) of 7,9 × 10-7, M for influenza A Mel virus neuraminidase whereas the Km of the virus enzyme for the substrate is 1000 times weaker (Km = 6, 9 × 10-4 M). The mechanism of inhibition is competitive, and enzyme inhibition is independent of enzyme concentration. 2-Deoxy-2,3-dehydro-N-trifluoroacetylneuraminic acid inhibits hemagglutination by NDV and SV5 but does not inhibit agglutination of red cells by Sendai virus or influenza A and B viruses.
AB - Eighteen derivatives of 2-deoxy-2,3-dehydro-N-acetylneuraminic acid were assayed for inhibitory activity against neuraminidases from viral and bacterial sources. Twelve of these compounds were active against neuraminidases of Vibrio cholerae, influenza A Mel, B Lee, and Newcastle disease virus, causing 50% enzyme inhibition in concentrations ranging from 10-3 M to 10-6 M. The most active of them and the most potent neuraminidase inhibitor described so far is 2-deoxy-2,3-dehydro-N-trifluoroacetylneuraminic acid. This compound has an inhibitor constant (Ki) of 7,9 × 10-7, M for influenza A Mel virus neuraminidase whereas the Km of the virus enzyme for the substrate is 1000 times weaker (Km = 6, 9 × 10-4 M). The mechanism of inhibition is competitive, and enzyme inhibition is independent of enzyme concentration. 2-Deoxy-2,3-dehydro-N-trifluoroacetylneuraminic acid inhibits hemagglutination by NDV and SV5 but does not inhibit agglutination of red cells by Sendai virus or influenza A and B viruses.
UR - https://www.scopus.com/pages/publications/0015959249
U2 - 10.1016/0042-6822(74)90080-4
DO - 10.1016/0042-6822(74)90080-4
M3 - Article
C2 - 4362431
AN - SCOPUS:0015959249
SN - 0042-6822
VL - 58
SP - 457
EP - 463
JO - Virology
JF - Virology
IS - 2
ER -