Work

Synthesis of a Conformationally Fixed Bicyclomarin Derivative

Year: 2025

Type: article

Abstract: Based on an X-ray structure of cyclomarin bound to ClpC1, a new conformationally fixed, bicyclic cyclomarin derivative is synthesized in an effort to enhance antituberculosis activity. The synthesis of the linear heptapeptide and the two macrolactamizations proceed smoothly. Only the very last synthetic step, the cleavage of a benzyl ether, provides a low yield. Despite the successful synthesis, the resulting bicyclic compound shows reduced activity compared to cyclomarin.

Source: ChemMedChem

DOI: 10.1002/cmdc.202500493

Authors: Jennifer Greve, Alexander F. Kiefer, Uli Kazmaier

Institutions: Saarland University, Helmholtz Institute for Pharmaceutical Research Saarland

Language: English

Topic: Chemical Synthesis and Analysis

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,150