Targeted lysosome disruptive elements for improvement of parenchymal liver cell-specific gene delivery

Bio-organic Synthesi

Reaction of N-trityl amino acids with BOP: Efficient synthesis of t-butyl esters as well as N-trityl serine- and threonine-β-lactones

Upon exposure to methoxymethylamine and BOP, the stable hydroxybenzotriazolyl amide of TrPheOH was isolated instead of the expected Weinreb amide. This amide behaves as an active amide similar to the Weinreb amide and could be used, among others, for the synthesis of t-Bu esters. Reaction of N-trityl serine and threonine led to the corresponding β-lactones in unprecedented high yields

Increased stability of peptidesulfonamide peptidomimetics towards protease catalyzed degradation

Replacement of amide bonds in peptides by sulfonamide moieties resulted in peptidosulfonamides with an increased stability towards protease catalyzed degradation. In addition to protection of the protease cleavage site, it was found that introduction of a sulfonamide also influenced the stability of adjacent amide bonds

Clickable Mesoporous Silica via Functionalization with 1,omega ¿--Alkenes

Tuning the surface properties of mesoporous silica is desirable for many applications, such as catalysis. We present a new modification method of calcined mesoporous silica, based on the thermal grafting of 1,7-octadiene. This easy method generates a high loading of terminal alkenes. We show that the modified surface is directly available for thiol-ene click chemistry, which enables a wide variety of molecules to be attached to this alkene-functionalized mesoporous silica