Open AccessSynthetic Approaches toward Monocyclic 3‐Amino‐β‐lactams
Author(s) -
Deketelaere Sari,
Van Nguyen Tuyen,
Stevens Christian V.,
D'hooghe Matthias
Publication year - 2017
Publication title -
chemistryopen
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.644
H-Index - 29
ISSN - 2191-1363
DOI - 10.1002/open.201700051
Subject(s) - lactam , ring (chemistry) , antibiotics , substituent , combinatorial chemistry , chemistry , penicillin , stereochemistry , penicillin binding proteins , organic chemistry , biochemistry
Due to the emerging resistance against classical β‐lactam‐based antibiotics, a growing number of bacterial infections has become harder to treat. This alarming tendency necessitates continued research on novel antibacterial agents. Many classes of β‐lactam antibiotics are characterized by the presence of the 3‐aminoazetidin‐2‐one core, which resembles the natural substrate of the target penicillin‐binding proteins. In that respect, this Review summarizes the different synthetic pathways toward this key structure for the development of new antibacterial agents. The most extensively applied methods for 3‐amino‐β‐lactam ring formation are discussed, in addition to a few less common strategies. Moreover, approaches to introduce the 3‐amino substituent after ring formation are also covered.