A new class of peptidomimetic is reported in which one of the amide C=O bonds of the peptide backbone is replaced by an oxetane ring. They are synthesised by conjugate addition of various α-amino esters to a 3-(nitromethylene)oxetane, reduction of the nitro group and further coupling with N-Z protected amino acids to grow the peptide chain. Structural insights are provided by X-ray diffraction ...

N-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leish...

After the first synthesis reported in 1994, azabicycloalkane amino acids have raised increasing interest, becoming one of most important classes constrained dipeptide mimics. Their incorporation into peptidomimetic structures allowed obtainment a wide range biologically active compounds. Over years, different research groups worked at development synthetic strategies to gain these rigid surroga...

A peptidomimetic compound containing leucine, tyrosine and malonic acid self-assembles through various noncovalent interactions to form spider silk-like fibers at ambient temperature. From the high-density liquid, a liquid-solid phase transition is initiated at 20 °C and solidification occurs upon contact with air. The fiber has comprehensive mechanical strength and optical properties similar t...