Synthesis of Bioactive Molecules

Another aspect of our research focuses on the synthesis of bioactive compounds. The biological and physicochemical profile of known agents, especially pesticides, should be improved by the synthesis of novel derivatives, so-called mimics or bioisosteres.

One of our mostly used type of mimic is the modulation of amide-bonds, a fundamental motif in many natural products, drugs and other active compounds. Therefore we develop the synthesis of surrogates with amide-mimic in respect of the low stability of amides towards hydrolysis in biological systems. Besides, numerous derivatives containing heteroatoms like nitrogen, oxygen or sulfur, cyclic or fluorinated bioisosteres may facilitate the optimization of the lead compound. In particular α-trifluoromethylated amines may be an appropriate replacement for peptide bonds due to their modified metabolism in vivo.