Design and enantioselective synthesis of 3-(α-acrylic acid) benzoxaboroles to combat carbapenemase resistance

• DOI: 10.1039/d1cc03026d
• Publication Date: 2021-07-14T12:08:34Z
• Authors: You-Cai Xiao; Xiao-Pan Chen; Ji Deng; Yu-Hang Yan; Kai-Rong Zhu; Gen Li; Jun-Lin Yu; Jürgen Brem; Fener Chen; Christopher J. Sc...; Guo-Bo Li
• Keywords: Chemistry; Benzoxazoles; 0303 health sciences; 03 medical and health sciences; Bacterial Proteins; Drug Design; Drug Resistance, Bacterial; Stereoisomerism; Chemistry Techniques, Synthetic; beta-Lactamases; Anti-Bacterial Agents

An organocatalytic MBH cascade reaction was developed to construct new 3-(α-acrylic acid) benzoxaboroles, designed to mimic ‘anchoring’ pharmacophore features of carbapenems, with the aim of helping overcome carbapenemase resistance.