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Potent Rifampicin derivatives can clear MRSA infections at single low doses when concomitantly dosed with Vancomycin
The Journal of Antibiotics ( IF 3.3 ) Pub Date : 2023-10-23 , DOI: 10.1038/s41429-023-00663-6
Thomas Nittoli 1 , Anna Brotcke Zumsteg 1 , Abira Bandyopadhyay 1 , Stephanie Federici 1 , Alida Coppi 1 , Susan Jorgenson 1 , Seung-Yong Choi 2 , Mrinmoy Saha 2 , Benjamin Wertz 2 , Priyanka Trivedi 1 , Chandrashekhar Korgaonkar 1 , Harvey Chin 1 , Onson Luong 1 , Christos Kyratsous 1 , William Olson 1
Affiliation  

For a number of years, antimicrobial resistance (AMR) has been a critical issue for humanity. Drug discovery efforts have been very limited and the spread of bacterial pathogens has over-run our traditional arsenal of antibiotics. Bacteria can involve to evade compounds that can halt their rapid growth. The authors have discovered a potent macrocycle derivative that when dosed concomitantly with the standard of care (SOC) antibiotic vancomycin, can clear methicillin resistant Staphylococcus aureus (MRSA) infections. In addition, we have probed the lead compounds in Salmonella typhimurium bacterial strains. In vitro, in vivo, and ADME data have been included to stress the virtues of this new antibiotic.



中文翻译:

与万古霉素同时服用时,有效的利福平衍生物可以单次低剂量清除 MRSA 感染

多年来,抗菌素耐药性(AMR)一直是人类面临的一个关键问题。药物发现工作非常有限,细菌病原体的传播已经超出了我们传统的抗生素库。细菌可能会逃避能够阻止其快速生长的化合物。作者发现了一种有效的大环衍生物,当与标准护理 (SOC) 抗生素万古霉素同时服用时,可以清除耐甲氧西林金黄色葡萄球菌(MRSA) 感染。此外,我们还探测了鼠伤寒沙门氏菌菌株中的先导化合物。体外、体内和 ADME 数据均包含在内,以强调这种新型抗生素的优点。

更新日期:2023-10-23
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