id author title date pages extension mime words sentences flesch summary cache txt cord-026010-61j07gq3 Elbein, Alan D. Alkaloid Glycosidase Inhibitors 2010-06-03 .txt text/plain 14892 841 50 or b!mannosidase but instead proved to be an e}ective inhibitor of a!glucosidase\ with a level of activity only slightly less than that of castanospermine[ 21 Numerous additional examples of inhibitory speci_cities due to both naturally occurring alkaloids and synthetic analogues have further undermined this empirical approach and it is obvious that structureƐactivity correlations can only be developed with the aid of sophisticated molecular modeling techniques[ Molecular orbital calculations and molecular modeling have been applied to a series of known mannosidase inhibitors and others which were expected to inhibit but failed to do so[ The results showed that good inhibitors _t closely with a single low!energy conformer of the mannosyl cation and demonstrated that 5!epi!castanospermine did not comply with the structural requirements[ 65\66 The electronegative binding groups present in the inhibitor necessary for speci_city and activity were established\ as were those which were of little signi_cance[ Additional studies of this type should provide valuable information regarding the receptor sites on the various enzymes but the inhibition data available is compromised by the variability in enzymes and the conditions under which measurements have been made[ A comprehensive screening program using standardized conditions would provide much more useful information for structureƐactivity correlations and consequently the design of speci_c and potent inhibitors[ ./cache/cord-026010-61j07gq3.txt ./txt/cord-026010-61j07gq3.txt