Synthesis and Antimicrobial Evaluation of Aminoguanidine and 3-amino- 1,2,4-triazole Derivatives as Potential Antibacterial Agents
作者:Tian-Yi Zhang、Chao Li、Ya-Ru Li、Xiao-Zhen Li、Liang-Peng Sun、Chang-Ji Zheng、Hu-Ri Piao
DOI:10.2174/1570180813666160819151239
日期:2016.10.31
A series of aminoguanidine derivatives bearing a 1,3,4-oxadiazole or piperazine moiety has been synthesized and fully characterized together with a series of 3-amino-1,2,4-triazole derivatives, and the resulting compounds were evaluated for their anti-bacterial activity. Most of these compounds showed broad-spectrum antibacterial activities against both Gram-positive and Gram-negative bacteria with
已合成了一系列带有1,3,4-恶二唑或哌嗪部分的氨基胍衍生物,并与一系列3-氨基-1,2,4-三唑衍生物一起进行了全面表征,并评估了所得化合物的抗-细菌活性。这些化合物大多数对革兰氏阳性和革兰氏阴性细菌均具有广谱抗菌活性,其最低抑菌浓度(MIC)和最低杀菌浓度(MBC)值在1–64μg/ mL范围内,包括耐多药临床分离株和真菌。值得注意的是,化合物19e和19f的抗甲氧西林金黄色葡萄球菌(3167和3506)和喹诺酮抗S的活性高于加替沙星和莫西沙星。金黄色葡萄球菌(3505和3519)的MIC和MBC值在1-2 µg / mL范围内。这两种化合物还显示出显着的抗真菌活性,对白色念珠菌7535的MIC值为1μg/ mL,相当于标准药物氟康唑的MIC值。因此,这些结果表明,不含哌嗪部分的氨基胍衍生物是开发新型抗菌剂的令人感兴趣的支架。