Specific, uncompetitive inhibition of beta-galactosidases by a 5,6-isopropylidenedioxyfuro[2,3-d]isoxazole-3-methanol derivative.

Schaller C; Demange R; Picasso S; Vogel P

doi:10.1016/s0960-894x(98)00722-7

Back

Journal article

Specific, uncompetitive inhibition of beta-galactosidases by a 5,6-isopropylidenedioxyfuro[2,3-d]isoxazole-3-methanol derivative.

Schaller C Institut de chimie organique de l'Université de Lausanne, Lausanne-Dorigny, Switzerland.
Demange R
Picasso S
Vogel P

1999-02-18

Published in:

Bioorganic & medicinal chemistry letters. - 1999

Dose-Response Relationship, Drug

Magnetic Resonance Spectroscopy

English (-)-(3aS,5S,6S.6aR)-3a,5,6,6a-Tetrahydro-5,6-isopropylide nedioxyfuro [2,3-d]isoxazole-3-methanol ((-)-5) has been tested toward 25 glycohydrolases and found to inhibit beta-galactosidase from Aspergillus niger (Ki = 18 microM) and that from Aspergillus orizae (Ki = 72 microM). Hydrolysis of the acetonide or exchange of CH2OH group for a CHO, CH2OMe or a CH2OMOM group suppresses the inhibitory activity.

Language