Design and synthesis of N-(trifluoromethyl)phenyl substituted pyrazole derivatives and their potency as antimicrobial agents are described. Several of these novel compounds are effective growth inhibitors of antibiotic-resistant Gram-positive bacteria and prevent the development of biofilms by methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus faecalis. These compounds eradicated the preformed biofilms effectively and were found to be more effective than the control antibiotic vancomycin. Potent compounds showed low toxicity to cultured human embryonic kidney cells with a selectivity factor of >20. The most promising compound is very potent against meropenem, oxacillin, and vancomycin-resistant clinical isolates of Enterococcus faecium. Investigations into the mode of action by performing macromolecular synthesis inhibition studies showed a broad range of inhibitory effects, suggesting targets that have a global effect on bacterial cell function.

中文翻译：

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N-(三氟甲基)苯基取代吡唑衍生物的设计、合成和抗菌活性

描述了N- (三氟甲基) 苯基取代的吡唑衍生物的设计和合成及其作为抗菌剂的效力。其中一些新化合物是耐抗生素革兰氏阳性菌的有效生长抑制剂，可防止耐甲氧西林金黄色葡萄球菌(MRSA) 和粪肠球菌形成生物膜。这些化合物有效地消除了预先形成的生物膜，并且被发现比对照抗生素万古霉素更有效。强效化合物对培养的人胚胎肾细胞具有低毒性，选择性因子>20。最有希望的化合物对美罗培南、苯唑西林和万古霉素耐药的临床分离株非常有效。粪肠球菌。通过进行大分子合成抑制研究对作用方式的调查显示了广泛的抑制作用，表明对细菌细胞功能具有全局影响的靶标。