Identification of a 2-Aminobenzimidazole Scaffold that Potentiates Gram-Positive Selective Antibiotics Against Gram-Negative Bacteria,ChemBioChem

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Identification of a 2-Aminobenzimidazole Scaffold that Potentiates Gram-Positive Selective Antibiotics Against Gram-Negative Bacteria
ChemBioChem ( IF 2.6 ) Pub Date : 2024-03-07 , DOI: 10.1002/cbic.202400127
Ansley M Nemeth ₁ , Milah M Young ₁ , Roberta J Melander ₁ , Richard D Smith ₂ , Robert K Ernst ₂ , Christian Melander ₁

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Small molecule adjuvants have the potential to expand the spectrum of gram-positive selective antibiotics to encompass gram-negative bacteria. We identifiy a series of 2-aminobenzimidazole (2-ABI) macrolide adjuvants with activity against Acinetobacter baumannii and Klebsiella pneumoniae. Preliminary mechanism of action studies suggests that adjuvants bind to lipopolysaccharide in K. pneumoniae, and modulate lipooligosaccharide biosynthesis, assembly, or transport in A. baumannii.

中文翻译：

鉴定一种 2-氨基苯并咪唑支架，可增强革兰氏阳性选择性抗生素对革兰氏阴性菌的治疗

小分子佐剂有可能扩大革兰氏阳性选择性抗生素的范围以涵盖革兰氏阴性菌。我们鉴定了一系列对鲍曼不动杆菌和肺炎克雷伯菌具有活性的 2-氨基苯并咪唑（2-ABI）大环内酯佐剂。初步作用机制研究表明，佐剂与肺炎克雷伯菌中的脂多糖结合，并调节鲍曼不动杆菌中的脂寡糖生物合成、组装或运输。

更新日期：2024-03-07

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