SCHEDULED MAINTENANCE
Azirine-containing dipeptides and depsipeptides: synthesis, transformations and antibacterial activity†
Nikolai V.
Rostovskii, 
*a
Alexander N.
Koronatov,
a
Pavel A.
Sakharov,
a
Anastasiya V.
Agafonova,
a
Alexander F.
Khlebnikov,
a
*a
Alexander N.
Koronatov,
a
Pavel A.
Sakharov,
a
Anastasiya V.
Agafonova,
a
Alexander F.
Khlebnikov,
a
Abstract
Azirine-containing dipeptides and depsipeptides with a wide range of substituents have been synthesized in high yields via the Passerini and Ugi multicomponent reactions (MCRs) using 2H-azirine-2-carboxylic acids as the acid component. The obtained MCR adducts have been transformed to lactam-fused aziridines, as well as pyrrole, imidazole, aziridine, and other derivatives, containing the dipeptide or depsipeptide moiety. The azirine-containing depsipeptides exhibit antibacterial activity against the ESKAPE pathogens, especially Gram-positive bacterial strains (E. faecium – MIC 16 μg mL−1, S. aureus – MIC 9 μg mL−1).
- This article is part of the themed collection: Synthetic methodology in OBC
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