β-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes

The 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 - containing amidine substituents at the C2 position of the bicyclic ring. These compounds, alone and in combi...

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Veröffentlicht in:Beilstein journal of organic chemistry 2021-03, Vol.17 (1), p.711-718
Hauptverfasser: Iqbal, Zafar, Zhai, Lijuan, Gao, Yuanyu, Tang, Dong, Ma, Xueqin, Ji, Jinbo, Sun, Jian, Ji, Jingwen, Liu, Yuanbai, Jiang, Rui, Mu, Yangxiu, He, Lili, Yang, Haikang, Yang, Zhixiang
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Sprache:eng
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Zusammenfassung:The 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 - containing amidine substituents at the 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 did not show antibacterial activity when tested alone (MIC >64 mg/L), however, they exhibited a moderate inhibition activity in the presence of meropenem by lowering its MIC values. The compound proved most potent among the other counterparts against all bacterial species with MIC from
ISSN:1860-5397
2195-951X
1860-5397
DOI:10.3762/bjoc.17.60