Inhibition studies on Vibrio cholerae neuraminidase. 1977

R Brossmer, and G Keilich, and D Ziegler

A series of viral neuraminidase inhibitors showing no structural analogy to neuraminic acids have been tested to find whether they are effective inhibitors of V. cholerae neuraminidase, too. Here we report the results obtained with the N-phenyloxamic acid derivatives 2 to 6 (R-NH-CO-COOR'; R = -C6H5NO2, -C6H5OH, -C6H5NH2; R' = -H, -C2H5; see Table 1) and with simple aromatic compounds structurally related to R, i.e. 4-nitroaniline (7), N-acetyl-4-nitroaniline (8), 4-nitrophenol (9), 2,4-dinitrophenol (10), and 4-aminophenol (11) (see Table 2). The inhibitory effects of 2 to 11 were studied according to the method of Dixon[19] in 0.1m sodium acetate buffer, pH 5.5, 2mM CaCl2, at 37 degrees C using the benzyl-alpha-ketoside of N-acetyl-D-neuraminic acid (1) as a substrate. The compounds 2 to 11 are shown to be competitive inhibitors of the enzymatic hydrolysis of the alpha-ketoside 1. The competitive inhibition kinetics are supported by the method of Lineweaver and Burk[20]. The inhibition constants (Ki) are found to be in the range of 0.03 to 5.7 mM. The simple aromatic compounds 7 to 11 show higher inhibitory activities than the phenyloxamic acid derivatives 2 to 6. In addition, significant differences in the Ki values were observed within the two series of inhibitors, whereby those containing a nitro group were most effective.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D009439 Neuraminidase An enzyme that catalyzes the hydrolysis of alpha-2,3, alpha-2,6-, and alpha-2,8-glycosidic linkages (at a decreasing rate, respectively) of terminal sialic residues in oligosaccharides, glycoproteins, glycolipids, colominic acid, and synthetic substrate. (From Enzyme Nomenclature, 1992) Sialidase,Exo-alpha-Sialidase,N-Acylneuraminate Glycohydrolases,Oligosaccharide Sialidase,Exo alpha Sialidase,Glycohydrolases, N-Acylneuraminate,N Acylneuraminate Glycohydrolases,Sialidase, Oligosaccharide
D009574 Nitro Compounds Compounds having the nitro group, -NO2, attached to carbon. When attached to nitrogen they are nitramines and attached to oxygen they are NITRATES. Nitrated Compounds
D010072 Oxamic Acid Amino-substituted glyoxylic acid derivative. Oxalamic Acid,Oxamidic Acid,Aminooxoacetic Acid,Acid, Aminooxoacetic,Acid, Oxalamic,Acid, Oxamic,Acid, Oxamidic
D010636 Phenols Benzene derivatives that include one or more hydroxyl groups attached to the ring structure.
D004140 Dinitrophenols Organic compounds that contain two nitro groups attached to a phenol.
D000814 Aniline Compounds Compounds that include the aminobenzene structure. Phenylamine,Phenylamines,Anilines,Compounds, Aniline
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D014734 Vibrio cholerae The etiologic agent of CHOLERA. Bacillus cholerae,Bacillus cholerae-asiaticae,Liquidivibrio cholerae,Microspira comma,Pacinia cholerae-asiaticae,Spirillum cholerae,Spirillum cholerae-asiaticae,Vibrio albensis,Vibrio cholera,Vibrio cholerae-asiaticae,Vibrio comma

Related Publications

R Brossmer, and G Keilich, and D Ziegler
January 1977, Developments in biological standardization,
R Brossmer, and G Keilich, and D Ziegler
June 1959, Nature,
R Brossmer, and G Keilich, and D Ziegler
September 2004, The Journal of biological chemistry,
R Brossmer, and G Keilich, and D Ziegler
October 1956, Journal of general microbiology,
R Brossmer, and G Keilich, and D Ziegler
February 1975, FEBS letters,
R Brossmer, and G Keilich, and D Ziegler
March 1961, Journal of general microbiology,
R Brossmer, and G Keilich, and D Ziegler
January 1950, The Indian journal of medical research,
R Brossmer, and G Keilich, and D Ziegler
January 1961, Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.),
R Brossmer, and G Keilich, and D Ziegler
November 1978, Endokrinologie,
Copied contents to your clipboard!