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Naphthylthiazoles: Targeting Multidrug-Resistant and Intracellular Staphylococcus aureus with Biofilm Disruption Activity
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2018-09-24 00:00:00 , DOI: 10.1021/acsinfecdis.8b00172
Mohamed Hagras 1 , Nader S. Abutaleb 2, 3 , Alsagher O. Ali 2, 4 , Jelan A. Abdel-Aleem 2, 5 , Mohamed M. Elsebaei 1 , Mohamed N. Seleem 2, 6 , Abdelrahman S. Mayhoub 1, 7
Affiliation  

Thirty-two new naphthylthiazole derivatives were synthesized with the aim of exploring their antimicrobial effect on multidrug-resistant Gram-positive bacteria. Compounds 25 and 32, with ethylenediamine and methylguanidine side chains, represent the most promising derivatives, as their antibacterial spectrum includes activity against multidrug-resistant staphylococcal and enterococcal strains. Moreover, the new derivatives are highly advantageous over the existing frontline therapeutics for the treatment of multidrug-resistant Gram-positive bacteria. In this vein, compound 25 possesses three attributes: no bacterial resistance was developed against it even after 15 passages, it was very efficient in targeting intracellular pathogens, and it exhibited a concentration-dependent ability to disrupt the preformed bacterial biofilm.

中文翻译:

萘噻唑:靶向耐多药和细胞内金黄色葡萄球菌具有生物膜破坏活性。

合成了32种新的萘噻唑衍生物,目的是探索它们对耐多药革兰氏阳性细菌的抗菌作用。具有乙二胺和甲基胍侧链的化合物2532代表最有前途的衍生物,因为它们的抗菌谱包括对耐多药葡萄球菌和肠球菌菌株的活性。而且,新的衍生物在治疗多药耐药的革兰氏阳性细菌方面比现有的一线治疗剂更具优势。就此而言,化合物25 具有三个属性:即使经过15次传代也没有针对它的细菌抗药性;它对细胞内病原体的靶向非常有效;并且它具有浓度依赖性的能力来破坏预先形成的细菌生物膜。
更新日期:2018-09-24
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