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Synthesis and Penicillin‐binding Protein Inhibitory Assessment of Dipeptidic 4‐Phenyl‐β‐lactams from α‐Amino Acid‐derived Imines
Author(s) -
Decuyper Lena,
Jukič Marko,
Sosič Izidor,
Amoroso Ana Maria,
Verlaine Olivier,
Joris Bernard,
Gobec Stanislav,
D'hooghe Matthias
Publication year - 2020
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201901470
Subject(s) - penicillin , penicillin binding proteins , inhibitory postsynaptic potential , potency , amino acid , chemistry , minimum inhibitory concentration , antibiotics , bacteria , lactam , microbiology and biotechnology , stereochemistry , amino acid residue , biochemistry , combinatorial chemistry , peptide sequence , biology , in vitro , genetics , neuroscience , gene
Monocyclic β‐lactams revive the research field on antibiotics, which are threatened by the emergence of resistant bacteria. A six‐step synthetic route was developed, providing easy access to new 3‐amino‐1‐carboxymethyl‐4‐phenyl‐β‐lactams, of which the penicillin‐binding protein (PBP) inhibitory potency was demonstrated biochemically.