Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative. Issue 19 (5th April 2019)

• Record Type: Journal Article
• Authors: Fang, Zhiyuan; Li, Yanan; Zheng, Yuanyuan; Li, Xiaomei; Lu, Yu-Jing; Yan, Siu-Cheong; Wong, Wing-Leung; Chan, Kin-Fai; Wong, Kwok-yin; Sun, Ning
• Is Part Of: RSC advances. Volume 9:Issue 19(2019)
• Page Start: 10739
• Page End: 10744
• Publication Date: 2019-04-05
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c9ra01001g
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : F20 exhibits strong antibacterial activity through interacting with FtsZ. Abstract : The issue of multidrug resistant bacteria is a worldwide health threat. To develop new antibacterial agents with new mechanisms of action is thus an urgent request to address this antibiotic resistance crisis. In the present study, a new thiophenyl-pyrimidine derivative was prepared and utilized as an effective antibacterial agent against Gram-positive strains. In the tests against MRSA and VREs, the compound showed higher antibacterial potency than that of vancomycin and methicillin. The mode of action is probably attributed to the effective inhibition of FtsZ polymerization, GTPase activity, and bacterial cell division, which cause bactericidal effects. The compound could be a potential candidate for further development as an effective antibiotic to combat drug-resistant bacteria.