SAR directed design and synthesis of novel β (1-4)-Glucosyltransferase inhibitors and Their In vitro inhibition studies

AK Bhattacharya, F Stolz, J Kurzeck, W Rüger…

Index: Bhattacharya, Asish K; Stolz, Florian; Kurzeck, Juergen; Rueger, Wolfgang; Schmidt, Richard R Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 4 p. 1129 - 1136

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Citation Number: 8

Abstract

This paper describes SAR directed design and synthesis of novel β (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 ...