N-(4-Nitrophenyl)oxamic Acid and Related N-Acylanilines Are Non-competitive Inhibitors of vibrio cholerae sialidase but do not inhibit trypanosoma cruzi or trypanosoma brucei trans-sialidases

N‐(4‐Nitrophenyl)oxamic acid 1, N‐(2‐fluoro‐4‐nitrophenyl)oxamic acid 7, N‐(4‐nitrophenyl)‐trifluoroacetamide 3, and N‐(2‐methoxy‐4‐nitrophenyl)trifluoroacetamide 9 are non‐competitive inhibitors of Vibrio cholerae sialidase with Ki‐values ranging from 2.66 to 5.18 · 10−4 M. These compounds, and the...

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Veröffentlicht in:Helvetica chimica acta 1994-06, Vol.77 (4), p.1166-1174
Hauptverfasser: Engstler, Markus, Schauer, Roland, Ferrero-García, Miguel A., Parodi, Armando J., Storz-Eckerlin, Thomas, Vasella, Andrea, Witzig, Christian, Zhu, Xiaoying
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Sprache:eng
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Zusammenfassung:N‐(4‐Nitrophenyl)oxamic acid 1, N‐(2‐fluoro‐4‐nitrophenyl)oxamic acid 7, N‐(4‐nitrophenyl)‐trifluoroacetamide 3, and N‐(2‐methoxy‐4‐nitrophenyl)trifluoroacetamide 9 are non‐competitive inhibitors of Vibrio cholerae sialidase with Ki‐values ranging from 2.66 to 5.18 · 10−4 M. These compounds, and the N‐acetylneuraminic‐acid analogues 11–13 do not inhibit the sialidase and trans‐sialidase activities from Trypanosoma cruzi; nor does N‐(4‐nitrophenyl)oxamic acid (1) inhibit the corresponding enzyme activities from T. brucei.
ISSN:0018-019X
1522-2675
DOI:10.1002/hlca.19940770425