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  • The synthesis and biological activity of lipophilic derivatives of bicine conjugated with N³-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP)-an inhibitor of glucosamine-6-phosphate synthase.

The synthesis and biological activity of lipophilic derivatives of bicine conjugated with N³-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP)-an inhibitor of glucosamine-6-phosphate synthase.

Journal of enzyme inhibition and medicinal chemistry (2011-06-04)
Dominik Koszel, Izabela Lącka, Katarzyna Kozłowska-Tylingo, Ryszard Andruszkiewicz
ABSTRACT

A series of bis-N,N-(2-hydroxyethyl)glycine (bicine) derivatives, conjugated with an inhibitor of glucosamine-6-phosphate synthase, have been synthesized and their lipophilic and antifungal properties have been tested. The obtained compounds demonstrated higher lipophilicity than free inhibitor (FMDP) and, in consequence, an increased potential to cross the cytoplasmic membrane. All the tested compounds show better antifungal activity than parent compound.

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Sigma-Aldrich
BICINE, ≥99% (titration)
Sigma-Aldrich
BICINE, BioXtra, ≥99% (titration)