A Fast and Convenient Synthesis of New Water-Soluble, Polyanionic Dendrimers.

Grzegorz M Salamończyk

doi:10.3390/molecules26164754

Abstract

Reasonably simple, efficient, and possessing aspects of generality, the methodology for the synthesis of new, water-soluble, dendrimeric polyesters with great potential applications as antiviral drugs in their own right is described. The essential aspect of the presented approach is a quite unique, immediate access to the polyanionic material at each generation during divergent synthesis. Six target polyanionic dendrimers (generations 1, 2, and 3) have been synthesized. The key monomers applied in this project were 1,3,5-benzenetricarboxylic acid derivatives, which also worked as direct precursors of the charged dendrimer surface.

Highlights

Dendrimers are three-dimensional, highly branched, synthetic polymers that possess a well-defined structure
The common feature of all such microbicide compounds is the presence of polyanions, which have the capability to bind to the (e.g., the so-called gp120 protein or spike protein) outer protein located on the viral surface, inhibiting the entire viral infection process [10]
We developed a method for the synthesis of dendrimeric polyphosphates and their analogs [21,22,23,24,25]

Summary

Introduction

Dendrimers are three-dimensional, highly branched, synthetic polymers that possess a well-defined structure. Different types and generations of dendrimers substituted with different charged groups have been explored in the prevention and treatment of HIV. These macromolecular drug candidates can be administered as topical microbicides [7,8,9]. There are numerous examples of this type of compounds that can be found in the literature [11,12,13,14] Thanks to their mode of action, polyanionic dendrimers can be expected to be effective against a broad spectrum of pathogenic viruses. There is an enormous global need for a vaginal microbicide offering protection of this nature It has been licensed as an antiviral condom coating. VIRALEZETM can be complementary to vaccines and other preventive measures

Methods

Results

Conclusion