660440-94-8Relevant articles and documents
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
Koszel, Dominik,Lacka, Izabela,Kozlowska-Tylingo, Katarzyna,Andruszkiewicz, Ryszard
experimental part, p. 167 - 173 (2012/07/13)
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.
A New Aliphatic Amino Prodrug System for the Delivery of Small Molecules and Proteins Utilizing Novel PEG Derivatives
Greenwald, Richard B.,Zhao, Hong,Yang, Karen,Reddy, Prasanna,Martinez, Anthony
, p. 726 - 734 (2007/10/03)
A new amino PEG prodrug system, based entirely on aliphatic structures, has been designed using ester derivatives easily synthesized from N-modified bis-N-2-hydroxyethylglycinamides. Hydrolysis of the various promoiety bonds, in vivo, regenerated amine in a predictable manner. Thus, a novel new methodology for controlled release of amino-containing drugs, peptides, and proteins has been accomplished. This work demonstrates the usefulness of a PEG prodrug strategy that results in solubilization of insoluble amino-containing drugs and provides prodrugs with relatively long circulating half-lives. It can be appreciated that this novel system should also be applicable for nonpolymer-containing prodrugs as well.
