硝基磺酰氟是用于开发抗生素的一种新的药效基团。
Nitro Sulfonyl Fluorides are a new pharmacophore for the development of antibiotics.
作者信息
Sadlowski Corinne, Park Bora, Araújo Clarissa, Das Subhamoy, Kerr D Lucas, He Maomao, Han Hesong, Riley Lee, Murthy Niren
机构信息
Department of Bioengineering, University of California, Berkeley, California, 94720, USA.
These authors contributed equally to this work.
出版信息
Mol Syst Des Eng. 2018 Aug 1;3(4):599-603. doi: 10.1039/C8ME00011E. Epub 2018 Jun 7.
Abstract
The development of antibiotics against Gram-negative bacteria is a central problem in drug discovery. In this report, we demonstrate that aromatic sulfonyl fluorides with a nitro group in their ortho position have remarkable antibacterial activity and are active against drug-resistant pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug resistant Acinetobacter baumannii, and Pseudomonas aeruginosa.
摘要
开发针对革兰氏阴性菌的抗生素是药物研发中的一个核心问题。在本报告中，我们证明了在其邻位带有硝基的芳基磺酰氟具有显著的抗菌活性，并且对耐药病原体如耐甲氧西林金黄色葡萄球菌（MRSA）、多重耐药鲍曼不动杆菌和铜绿假单胞菌具有活性。
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