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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
Author(s) -
Engstler Markus,
Schauer Roland,
FerreroGarcía Miguel A.,
Parodi Armando J.,
StorzEckerlin Thomas,
Vasella Andrea,
Witzig Christian,
Zhu Xiaoying
Publication year - 1994
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19940770425
Subject(s) - vibrio cholerae , chemistry , trypanosoma cruzi , sialidase , enzyme , biochemistry , stereochemistry , bacteria , neuraminidase , biology , parasite hosting , genetics , world wide web , computer science
Abstract 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 K i ‐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 .