Dendrimers provide an excellent platform to tailor molecular diversity by appending numerous biologically active elements at terminal positions. Recently, we proposed a novel approach, where not only end of branches but also the whole dendrimer tree was used to locate active groups responsible for interactions with microbial membranes (aromatic and positively charged amino acid residues). Recently, dendrimeric peptides based on lysine as a trivalent core and branching element have been developped [1]. They expressed wide spectrum of antimicrobial activity against Gram-positive (S. aureus), Gram-negative (E. coli) and C. albicans strains. This confirmed our postulate that bioactive conformation could be achieved by selection one out of many topologically relevant structures.

Cytotoxicity studies showed that better properties have compounds with higher degree of branching ("dendrimeric effect") [2]. Therefore, several new N-propylamino derivatives of basic amino acids were designed and used as cores in the synthesis of a new generation of dendrimeric peptides.

The present communication will present synthetic approach towards preparation of analogs containing higher number of active elements within the dendrimer tree and therefore, more rigid structure.

This project was supported by grant No. 3T09B 115 28 from the Ministry of Education and Science.

1. Janiszewska J, Swieton J, Lipkowski AW, Urbanczyk-Lipkowska Z., Bioorg. Med. Chem. Lett., 2003,13, 3711-3713.

2., Klajnert B., Janiszewska J, Urbanczyk-Lipkowska Z, Bryszewska M., Shcharbin D, Labieniec M, Intern. J. Pharmaceutics 2006, 309, 208-217.

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