Abstract

A series of novel N-4-piperazinyl ciprofloxacin-ester hybrids has been synthesized and the structures confirmed by¹H and ¹³C NMR, FT-IR spectral data, and elemental analysis. The products have been tested in vitro for their antibacterial activity against six bacterial strains (MRSA, Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli,Salmonella enterica, and Klebsiella pneumoniae) and have demonstrated good antibacterial activity with MIC values range 6.25–200 µg/mL. Antifungal and cytotoxic activities of the products have been tested against Candida kefyr and human leukemia K562 cell line, respectively. All compounds inhibit growth of K562 cells more efficiently than the parent ciprofoxacin in a dose- and duration-dependent way. Molecular docking studies performed for the compound 3i indicates that similarly to ciprofloxacin it can act as an inhibitor of S. aureus DNA gyrase.

中文翻译：

---

新型N -4-哌嗪基环丙沙星-酯杂化物：合成，生物学评估和分子对接研究

摘要

合成了一系列新颖的N -4-哌嗪基环丙沙星酯杂化物，并通过¹ H和¹³ C NMR，FT-IR光谱数据和元素分析确认了结构。该产品已通过体外测试，对六种细菌菌株（MRSA，表皮葡萄球菌，枯草芽孢杆菌，大肠杆菌，沙门氏菌和小肠肺炎克雷伯菌）具有抗菌活性，并具有良好的抗菌活性，MIC值为6.25–200 µg /毫升 该产品的抗真菌和细胞毒性活性已通过针对假丝酵母Kefyr的测试和人类白血病K562细胞系。与母体环丙沙星相比，所有化合物均以剂量和持续时间依赖性方式更有效地抑制K562细胞的生长。对化合物3i进行的分子对接研究表明，与环丙沙星类似，它可以作为金黄色葡萄球菌DNA促旋酶的抑制剂。