Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties
作者:Zhi-Yu Wei、Ke-Qiang Chi、Zhan-Kui Yu、Hong-Yan Liu、Liang-Peng Sun、Chang-Ji Zheng、Hu-Ri Piao
DOI:10.1016/j.bmcl.2016.11.001
日期:2016.12
Three novel series of chalcone derivatives containing an aminoguanidine or acylhydrazone moiety were designed, synthesized and evaluated in terms of their antibacterial, antifungal and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibitory activity towards various bacteria and one fungus with minimum inhibitory concentrations (MICs) ranging from 1 to 8mug/mL. Compared
根据其抗菌,抗真菌和抗炎活性,设计,合成和评估了三个新颖的包含氨基胍或酰基hydr部分的查耳酮衍生物。大多数合成的化合物显示出对各种细菌和一种真菌的有效抑制活性,最低抑制浓度(MIC)为1至8ug / mL。与我们先前报道的查耳酮衍生物(MICs> 64mug / mL)相比,这些化合物对革兰氏阴性细菌菌株(大肠杆菌1924和1356)显示出更高的抗菌活性(MICs = 2mug / mL)。发现化合物4f和4h对革兰氏阴性细菌鼠伤寒沙门氏菌1926和白色念珠菌7535的MIC最有效,MIC值为1mug / mL。化合物4f在本研究中制备的所有化合物中显示出最有效的抗炎活性,腹膜内给药后抑制率为92.45%,使其比参考药物吲哚美辛和布洛芬更有效。在HeLa,Hep3B和L02细胞中评估了化合物4f的细胞毒活性。