Synthesis of ruthenium complexes functionalized with benzothiophene and their antibacterial activity against Staphylococcus aureus. Issue 16 (9th April 2021)

• Record Type: Journal Article
• Authors: Liao, Xiangwen; Liu, Lianghong; Tan, Yanhui; Jiang, Guijuan; Fang, Haihong; Xiong, Yanshi; Duan, Xuemin; Jiang, Guangbin; Wang, Jintao
• Is Part Of: Dalton transactions. Volume 50:Issue 16(2021)
• Page Start: 5607
• Page End: 5616
• Publication Date: 2021-04-09
• Subjects: Chemistry, Inorganic -- Periodicals; Chemistry, Physical and theoretical -- Periodicals; Chemistry, Inorganic -- Periodicals; 546.05
• DOI: 10.1039/d0dt04258g
• Languages: English
• ISSNs: 1477-9226

Abstract

Abstract : Ruthenium complex Ru(II)-3 functionalized with benzothiophene showed good antimicrobial activity against Staphylococcus aureu s in vivo . Abstract : New effective antimicrobial agents with novel modes of action are urgently needed due to the continued emergence of drug-resistant bacteria. Here, three ruthenium complexes functionalized with benzothiophene: [Ru(phen)2 (BTPIP)](ClO4 )2 (Ru(II)-1 ), [Ru(dmp)2 (BTPIP)](ClO4 )2 (Ru(II)-2 ) and [Ru(dmb)2 (BTPIP)](ClO4 )2 (Ru(II)-3 ) (dmb = 4, 4′-dimethyl-2, 2′-bipyridine, phen = 1, 10-phenanthroline, dmp = 2, 9-dimethyl-1, 10-phenanthroline) have been synthesized and their antimicrobial activities in vitro were assessed. Minimum inhibitory concentration (MIC) assays indicated that the three Ru(II)-1, Ru(II)-2 and Ru(II)-3 complexes all showed antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa. The most active Ru(II)-3 complex was further tested against biofilms. Furthermore, it was also tested whether complex Ru(II)-3 could serve as an antibacterial adjuvant. Interestingly, the checkerboard data showed that Ru(II)-3 selectively exhibited synergism with aminoglycoside antibiotics. More importantly, the observed synergetic effect might be attributed to the inhibition of the regulatory function of Sa CcpA. Finally, in vivo bacterial infection treatment studies through a murine skin infection model and skin irritation test were also conducted. All in all, these results confirmed that ruthenium complexes functionalized with benzothiophene have good antimicrobial activity against Staphylococcus aureus .