Thiol-Ene Synthesis of Cationic Carbosilane Dendrons: a New Family of Synthons

A variety of neutral and cationic carbosilane dendrons containing a wide range of active groups, such as −N₃, −OH, −NH₂, and −SH, at the focal points were synthesized from carbosilane vinyl dendrons BrG_<i>n</i>V_<i>m</i> from generations 1–3 by substitution of the bromine atom at the focal point and functionalization of the vinyl groups via thiol-ene click chemistry with HS­(CH₂)₂NMe₂·HCl. These dendritic wedges were characterized by NMR, MS, and elemental analysis

Improved Efficiency of Ibuprofen by Cationic Carbosilane Dendritic Conjugates

In order to improve the efficiency of the anti-inflammatory drug ibuprofen, cationic carbosilane dendrimers and dendrons with ibuprofen at their periphery or at their focal point, respectively, have been synthesized, and the release of the drug was studied using HPLC. Macrophages were used to evaluate the anti-inflammatory effect of the ibuprofen-conjugated dendritic systems and compared with mixtures of non-ibuprofen dendritic systems in the presence of the drug. The cationic ibuprofen-conjugated dendron was the compound that showed higher anti-inflammatory properties. It reduces the LPS-induced <i>COX-2</i> expression and decreases the release of several inflammatory cytokines such as TNFα, IL-1β, IL-6, and CCL3. These results open new perspectives in the use of these compounds as drug carriers