AIM The aim of the present study was to design, synthesize, and evaluate novel antibacterial agents, derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide. METHODS A total of 44 derivatives of aryl-4-guanidin-omethylbenzoate (series A) and N-aryl-4-guanidinomethylbenzamide (series B) were synthesized and their antibacterial activities were assessed in vitro against a variety of Gram-positive and Gram-negative bacteria by an agar dilution method. RESULTS Twelve compounds showed potent bactericidal effects against a panel of Gram-positive germs, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), vancomycin-intermediate Staphylococcus aureus (VISA), and methicillin-resistant coagulase-negative staphylococci (MRCNS), with minimum inhibitory concentrations (MIC) ranging between 0.5 and 8 microg/mL, which were comparable to the MIC values of several marketed antibiotics. They exhibited weak or no activity on the Gram-negative bacteria tested. In addition, these compounds displayed high inhibitory activities towards oligopeptidase B of bacterial origin. CONCLUSION In comparison with the previously reported MIC values of several known antibiotics, the derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide showed comparable in vitro bactericidal activities against VRE and VISA as linezolid. Their growth inhibitory effects on MRSA were similar to vancomycin, but were less potent than linezolid and vancomycin against MRCNS. This class of compounds may have the potential to be developed into narrow spectrum antibacterial agents against certain drug-resistant strains of bacteria.

中文翻译：

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芳基-4-胍基甲基苯甲酸酯和N-芳基-4-胍基甲基苯甲酰胺作为新型抗菌剂的衍生物：合成和生物活性。

目的本研究的目的是设计，合成和评估新型抗菌剂，芳基-4-胍基甲基苯甲酸酯和N-芳基-4-胍基甲基苯甲酰胺的衍生物。方法合成了44种芳基-4-胍基-邻甲基苯甲酸酯衍生物（A系列）和N-芳基-4-胍基甲基苯甲酰胺（B系列）衍生物，并在体外评估了它们对多种革兰氏阳性和革兰氏阳性菌的抗菌活性。通过琼脂稀释法检测阴性细菌。结果十二种化合物对一组革兰氏阳性细菌显示出有效的杀菌作用，这些细菌包括耐甲氧西林的金黄色葡萄球菌（MRSA），耐万古霉素的肠球菌（VRE），耐万古霉素的金黄色葡萄球菌（VISA）和耐甲氧西林的凝固酶葡萄球菌（MRCNS）最低抑菌浓度（MIC）在0.5至8微克/毫升之间，与几种市售抗生素的MIC值相当。它们对所测试的革兰氏阴性细菌表现出微弱或没有活性。另外，这些化合物对细菌来源的寡肽酶B显示出高抑制活性。结论与先前报道的几种已知抗生素的MIC值相比，芳基-4-胍基甲基苯甲酸酯和N-芳基-4-胍基甲基苯甲酰胺的衍生物在体外对VRE和VISA的杀菌活性与利奈唑胺相当。它们对MRSA的生长抑制作用与万古霉素相似，但效力不及利奈唑胺和万古霉素对MRCNS的抑制作用。