Abstract

Diazabicyclooctane (DBO) scaffold is the backbone of non-β-lactam based second generation β-lactamase inhibitors. As part of our efforts we have synthesized a series of DBO derivatives A1-A23 containing amidine substituents at C2 position of the bicyclic ring. These compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their antibacterial activity in vitro. All compounds didn’t show antibacterial activity when alone (MIC, >64 mg/L), however exhibited moderate inhibition activity in the presence of meropenem by lowering its MIC values. Compound A12 proved most potent among the other counterparts against all bacterial species with MIC from <0.125 mg/L – 2 mg/L, and is comparable to avibactam against both E. coli strains with MIC value of <0.125 mg/L.

Keywords: Amidine, β-lactamases inhibitors, diazabicyclooctane, synthesis, antibacterial activity.

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iqbal, Z.; Gao, Y.; Tang, D.; Ma, X.; Ji, J.; Sun, J.; Ji, J.; Liu, Y.; Zhai, L.; Jiang, R.; Mu, Y.; He, L.; Yang, H.; Yang, Z. Beilstein Arch. 2020, 2020143. doi:10.3762/bxiv.2020.143.v1

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