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…

文献索引：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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被引用次数: 8

摘要

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 ...