Sep 2026· Chinese Journal of Natural Medicines· Vol 24 9, pp.
1146-1152
· 0 citations· 26 references
Medicine
TL;DR
Mechanistic study showed that 24a effectively inhibits biofilm formation and exerts its antibacterial effect by disrupting the bacterial cell membrane, paving the way for new strategies to combat antimicrobial resistance.
Abstract
The rapid emergence of multidrug-resistant bacterial pathogens, particularly methicillin-resistant Staphylococcus aureus (MRSA), underscores the critical discovery for new antibiotics with novel scaffolds. We identified lead compound LXW933, which exhibits promising anti-MRSA activity and features a unique 1,2,4-oxadiazole scaffold, from our phidianidine-based compound library. Based on this structure, a Function-Oriented Synthesis (FOS) strategy had been conducted to afford a series of phidianidine derivatives for their antibacterial activity evaluation. Compounds 24a exhibited excellent anti-MRSA efficacy with an MIC value of 1.5 μg/mL and low toxicity against HeLa cells. Further mechanistic study showed that 24a effectively inhibits biofilm formation and exerts its antibacterial effect by disrupting the bacterial cell membrane. This research provides valuable insights for the discovery of antibacterial drug leads derived from oxadiazole-containing marine alkaloids, paving the way for new strategies to combat antimicrobial resistance.
A series of new indole-pyrazole-linked isoxazole hybrids (5a-o) were synthesized using Cu(I)-catalyzed 1,3-dipolar cycloaddition and assessed for antibacterial and antibiofilm activities against methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resista...
Venkatesh Reddycherla, K. Chennakesavulu, G. R. Reddy et al.· Asian Journal of Chemistry· 0 citations
A novel series of pyrimidine-based N-heterocyclic hybrids incorporating 1,2,4-triazole (10a–10j) and benzotriazole (11a–11j) moieties was synthesized and evaluated for antibacterial activity against a panel of Gram-positive and Gram-negative bacterial pathogens. The structures of all synthesized compounds were confirme...
Gobind Kumar, Safiyah Ghumran, N. Manhas et al.· RSC Advances· 0 citations
The increasing threat of infections caused by multidrug-resistant Gram-positive pathogens such as MRSA and VRE has driven the structural remodeling and repurposing of traditional antibiotics as a key strategy to combat bacterial resistance. Herein, using bacitracin A as a lead template, we established a site-selective...
Si-Jie Cheng, Jing-Wen Liao, Xin-Ru Xia et al.· Journal of Medicinal Chemist...· 0 citations
Antimicrobial resistance is an urgent global public health threat, killing at least 1.27 million people worldwide and associated with nearly 5 million deaths. Antibiotic resistance has been recently recognized by the WHO as a global health emergency. In this scenario, the research and development of novel derivatives...
Matteo Lusardi, D. Caviglia, Andrea Chiocca et al.· ACS Omega· 0 citations
Background/Objectives: The rapid emergence and spread of antibiotic-resistant bacterial strains represent a major global health threat, requiring the development of novel broad-spectrum antimicrobial agents. This study aims to design, synthesize, and evaluate a novel series of multitarget amphiphilic carvacrol derivati...
D. Zadvornykh, Mei-Ling Wang, A. Bardasheva et al.· Antibiotics· 0 citations
AIMS
Antibiotic-resistant bacteria, particularly methicillin-resistant Staphylococcus aureus (MRSA), have renewed interest in antivirulence strategies. This study aimed to design, synthesize, and evaluate asymmetric di‑heterocyclic benzazole derivatives as antibiofilm agents targeting wall teichoic acid (WTA) biosynthe...
Mine Buga Aktekin, Z. Oksuz, M. Alagoz et al.· Future Medicinal Chemistry· 0 citations
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