N-Benzylgalactonoamidines as potent β-galactosidase inhibitors |
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Authors: | Rami Kanso Elizabeth A Yancey Susanne Striegler |
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Institution: | Auburn University, Department of Chemistry and Biochemistry, 179 Chemistry Building, Auburn, AL 36849, USA |
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Abstract: | A series of N-benzylgalactonoamidines was synthesized to probe their inhibitory ability during the hydrolysis of o-nitrophenyl-β-d-galactopyranoside by β-galactosidase (Aspergillus oryzae). All compounds are characterized as potent competitive inhibitors with inhibition constants (Ki) in the low nanomolar range (12–48 nM). The structure of the inhibitors mimics the bond-lengthening during the hydrolysis and the aromatic aglycon of the substrate. The electronic nature of the substituent in p-position of the aglycon influences the overall inhibitory ability most when compared to the unsubstituted parent compound. |
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