The emergence of multi-drug resistant bacteria has increased the need for novel antibiotics to help overcome what may be considered the greatest threat to modern medicine. Here we report the synthesis of fifteen novel 3,5-diaryl-1H- pyrazoles obtained via one-pot cyclic oxidation of a chalcone and hydrazine-monohydrate. The synthesised pyrazoles were then screened against Staphylococcus aureus and Escherichia coli to determine their antibacterial potential. The results show that compound 7p is bacteriostatic at MIC 8 µg/mL. The compound is non-toxic against healthy mammalian cells, 3T3-L1 at the highest test concentration 50 µg/mL. Furthermore, compound 7p significantly affected bacterial morphogenesis before cell lysis in Bacillus subtilis when treated above the MIC concentration. From the results, a promising lead compound was identified for future development.

多重耐药细菌的出现增加了对新型抗生素的需求，以帮助克服可能被认为对现代医学的最大威胁。在这里，我们报告了通过查耳酮和肼一水合物的一锅循环氧化获得的十五种新型 3,5-二芳基-1H-吡唑的合成。然后针对金黄色葡萄球菌和大肠杆菌筛选合成的吡唑，以确定它们的抗菌潜力。结果表明，化合物7p在 MIC 8 µg/mL 时具有抑菌作用。该化合物对健康哺乳动物细胞 3T3-L1 无毒，最高测试浓度为 50 µg/mL。此外，化合物7p当处理高于 MIC 浓度时，显着影响枯草芽孢杆菌细胞裂解前的细菌形态发生。根据结果​​，确定了一种有前途的先导化合物，可用于未来的开发。