SAR directed design and synthesis of novel β(1-4)-glucosyltransferase inhibitors and their in vitro inhibition studies

This paper describes SAR directed design and synthesis of novel beta(1-4)-glucosyltransferase (BGT) inhibitors. The designed inhibitors 1-5 provide conformational mimicry of the transition-state in glucosyltransfer reactions. The compounds were tested for in vitro inhibitory activity against (BGT) and the inhibition kinetics were examined. Three of the designed molecules were found to be potential inhibitors of BGT having IC50 values in micromolar (muM) range. Useful structure-activity relationships were established, which provide guidelines for the design Of future generations of inhibitors of BGT. (C) 2002 Elsevier Science Ltd. All rights reserved.