2‑Aminoimidazole-benzimidazole Conjugates Potentiate the Gram-Positive Selective Antibiotic Clarithromycin against Acinetobacter baumannii

2-氨基咪唑-苯并咪唑缀合物可增强革兰氏阳性选择性抗生素克拉霉素对鲍曼不动杆菌的抗菌活性

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Abstract

An increase in antibiotic resistance and the paucity of new treatment options have led to the present-day antibiotic resistance crisis. Acinetobacter baumannii is categorized by the World Health Organization as a critical priority. Previously, we reported halogenated aryl 2-aminoimidazole (2-AI) adjuvants that potentiate macrolide antibiotics against A. baumannii; however, this class of adjuvants exhibits cytotoxicity toward HepG2 cells. In this study we generate a library of 2-AI-benzimidazole adjuvants that potentiate clarithromycin (CLR), and exhibit reduced cytotoxicity. Lead compounds lower the CLR minimum inhibitory concentration (MIC) across a panel of A. baumannii clinical isolates, and have therapeutic indices (TI) up to 6-fold higher than the parent 2-AIs.

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