Synthesis and biological evaluation of α-triazolyl chalcones as a new type of potential antimicrobial agents and their interaction with calf thymus DNA and human serum albumin

• Synthesis and valuable antimicrobial potency of α-triazolyl chalcones.
• Some prepared compounds were highly sensitive to MRSA.
• Intercalation of 9a into DNA revealed to be responsible for antimicrobial activity.
• α-Triazolyl chalcone 9a could be effectively stored and carried by HSA.
• Some metal ions were found to increase the concentration of free compound 9a.

A series of α-triazolyl chalcones were efficiently synthesized. Most of the prepared compounds showed effective antibacterial and antifungal activities. Noticeably, α-triazolyl derivative 9a exhibited low MIC value of 4 μg/mL against MRSA and Micrococcus luteus, which was comparable or even superior to reference drugs. The further research revealed that compound 9a could effectively intercalate into Calf Thymus DNA to form 9a–DNA complex which might block DNA replication to exert their powerful antimicrobial activities. Competitive interactions between 9a and metal ions to Human Serum Albumin (HSA) suggested the participation of Fe3+, K+ and Mg2+ ions in 9a–HSA system could increase the concentration of free 9a, shorten its storage time and half-life in the blood, thus improving its antimicrobial efficacy.

A series of α-triazolyl chalcones were synthesized and screened for their antimicrobial activities, further binding behavior with calf thymus DNA and human serum albumin was investigated.Figure optionsDownload as PowerPoint slide