Synthesis and antibacterial activity evaluation of aminoguanidine or dihydrotriazine derivatives

Bai, Xueqian ; Zhao, Limin ; Liu, Zhe ; Li, Yan ; Zhang, Tianyi ; Liu, Xuekun

Abstract

In the alarming context of rising bacterial antibiotic resistance, there is an urgent need to discover new antibiotics or increase and/or enlarge the activity of those currently in use. In this article, aminoguanidine and dihydrotriazine derivatives were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities. Most of the synthesized compounds showed potent inhibitory activities against different bacteria and one fungus with minimum inhibitory concentrations (MICs) ranging from 1 to 64 μg/mL, which obviously better than the positives control drug. The compound 23a showed the best antibacterial activities, whose MIC value was 1 μg/mL against eight strains. The cytotoxic activity of the compound 4c, 8a and 23a were assessed in Human liver cancer cells. The preliminary docking results imply that compounds 21b and 23a possibly display their antibacterial activity through the interaction with DHFR protein by targeting residues of the active cavities of DHFR.



Keyword(s)

Aminoguanidine; Antibacterial activities; Antifungal activities; Cytotoxicity; Dihydrotriazine

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