Tiny antimicrobial systems, results from APOGEO in the journal Advanced Synthesis and Catalysis

The new article "Synthesis of Diketopiperazine Scaffolds with Tailored N- and α-Chains by Selective Modification of Customizable Units", published in the journal Advanced Synthesis and Catalysis analyzes recent results developed within the framework of the APOGEO project.

Tiny transport systems that carry phytosanitary products or drugs to fight pathogens, or that are in themselves highly active against the micro-organisms that threaten our crops or our health, are of great interest to the market. To achieve this goal, derivatives of the simplest peptides, the dicetopiperazine, have been designed, consisting of only two amino acids that form a relatively rigid cycle. Dicytopiperazine can have up to four substitutes, as shown in the picture. When there are four chains, they are arranged in space so that two are oriented below the cycle plane, and the other two in the plane or above. This allows for systems in which two chains are used for "anchoring" in the biological targets, and the other two for carrying the products (phytosanitary products, drugs, probes).

However, manufacturing these small cycles with four substitutes is very difficult, especially if some of the substitutes are bulky. In that case, high temperature conditions, treatments with highly reactive molecules, etc. are required. On the other hand, with the method reported in the high-impact journal Advanced Synthesis and Catalysis, with funding from the APOGEO project, it is possible to manufacture these "tailor-made" compounds with four different chains, and with very large substitutes. What's more, it's done under very mild conditions, at low temperature, and it provides good yields of the desired products with high purity. This methodology opens the doors to create collections of phytosanitary products that will be tested in APOGEO. For further information, please visit the link to this article

sistemas antimicrobianos