Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 10, Issue 6, Pages 1967-1972Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(02)00005-6
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N-Octyl-beta-valienemine (1), a potent beta-glucocerebrosidase inhibitor, was chemically transformed into two biologically interesting compounds: the 4-epimer 2, beta-galacto-type N-octyl-valienamine, and the 4-O-(beta-D-galactopyranosyl) derivative 3, a carba-lactosylceramide analogue. The former, interestingly, could be demonstrated to act as a very effective inhibitor (IC50=0.3 muM) of human beta-galactosidase. The latter exhibited moderate inhibitory activity (IC50=20 muM) against beta-glucocerebrosidase (mouse liver). (C) 2002 Elsevier Science Ltd. All rights reserved.
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