Sun, G;
de Resende, PE;
Stapleton, P;
Kuta, M;
Wang, X;
Haider, S;
Yang, M;
(2017)
Regioselective glycosylation of novobiocin alters activity.
Carbohydrate Research
, 452
pp. 116-121.
10.1016/j.carres.2017.10.011.
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Abstract
Glycosylation is a promising approach to overcome antimicrobial drug resistance. In this study, we investigated Koenigs-Knorr and phase transfer glycosylation on novobiocin. While the former only gave a 4'-OH product, the later produced mainly a kinetic controlled 5-OH product, but still achieved the 4'-OH modification and novoise-glycosylated products (with stronger base), as well as a diglycosylated compound. Investigation on the antibacterial activity indicate that the presence of galactose moiety helps to improve activity possibly via enhanced cellular uptake.
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