Synthesis and In Vitro Antimicrobial SAR of Benzyl and Phenyl Guanidine and Aminoguanidine Hydrazone Derivatives
作者:Wolfgang Dohle、Xiangdong Su、Yamni Nigam、Edward Dudley、Barry V. L. Potter
DOI:10.3390/molecules28010005
日期:——
A series of benzyl, phenyl guanidine, and aminoguandine hydrazone derivatives was designed and in vitro antibacterial activities against two different bacterial strains (Staphylococcus aureus and Escherichia coli) were determined. Several compounds showed potent inhibitory activity against the bacterial strains evaluated, with minimal inhibitory concentration (MIC) values in the low µg/mL range. Of
设计了一系列苄基、苯基胍和氨基胍腙衍生物,并测定了对两种不同菌株(金黄色葡萄球菌和大肠杆菌)的体外抗菌活性。几种化合物对所评估的细菌菌株表现出有效的抑制活性,最小抑制浓度 (MIC) 值在低 µg/mL 范围内。在所有胍衍生物中,3-[2-氯-3-(三氟甲基)]-苄氧基衍生物 9m 显示出最佳效力,MIC 分别为 0.5 µg/mL(金黄色葡萄球菌)和 1 µg/mL(大肠杆菌) 。几种氨基胍腙衍生物也表现出良好的总体活性。化合物 10a、10j 和 10r-s 对金黄色葡萄球菌和大肠杆菌的 MIC 均为 4 µg/mL。在氨基胍腙系列中,3-(4-三氟甲基)-苄氧基衍生物 10d 对金黄色葡萄球菌 (MIC 1 µg/mL) 表现出最佳效力,但对大肠杆菌 (MIC 16 µg/mL) 的活性要差得多。化合物 9m 和对位取代衍生物 9v 对两种耐甲氧西林金黄色葡萄球菌 (MRSA) 菌株