Department of Chemistry, Sri Jayachamarajendra College of Engineering, JSS Science and Technology University, Mysuru 570 006, Karnataka, India.
PG Department of Chemistry, JSS College of Arts, Commerce and Science, Mysuru 570025, Karnataka, India.
Bioorg Med Chem. 2019 Mar 1;27(5):841-850. doi: 10.1016/j.bmc.2019.01.026. Epub 2019 Jan 28.
Increasing in the alarm against the resistant bacteria due to the failure of antibiotics, thereby the need of more efficiency/potent molecule to treat infections. In the present investigation, series of piperazine derivatives 5(a-l) compounds were synthesized and they were characterised by different spectral techniques such as H NMR, C NMR, IR and LCMS. A novel copper complex (cPAmPiCaTc) was developed for the first time by using potent analog 5e and characterized by IR and LCMS. The cPAmPiCaTc evaluated for antibacterial activity and showed excellent antimicrobial effect (12 ± 0.08 mm, ZOI) at MIC 20 µg/mL against MRSA compared to standard antibiotics streptomycin and bacitracin at MIC 10 µg/mL. The results show promising anti-staphylococcal action against MRSA which confirmed by membrane damage, bioelectrochemistry, gene regulation (SarA and DHFR), and in silico molecular docking studies. Further, the cPAmPiCaTc also showed excellent blood compatibility and this result pave the way for interesting metallodrug therapeutics in future against MRSA infections.
由于抗生素失效，人们对耐药菌的警惕性不断提高，因此需要更有效/强效的分子来治疗感染。在本研究中，合成了一系列哌嗪衍生物 5(a-l)化合物，并通过 H NMR、C NMR、IR 和 LCMS 等不同光谱技术对其进行了表征。首次使用有效模拟物 5e 开发了一种新型铜配合物 (cPAmPiCaTc)，并通过 IR 和 LCMS 对其进行了表征。cPAmPiCaTc 的抗菌活性评估结果表明，与 MIC 为 10 µg/mL 的标准抗生素链霉素和杆菌肽相比，其在 MIC 为 20 µg/mL 时对 MRSA 具有优异的抗菌效果（12 ± 0.08 mm，ZOI）。结果表明，cPAmPiCaTc 对 MRSA 具有有前途的抗葡萄球菌作用，这通过膜损伤、生物电化学、基因调控（SarA 和 DHFR）和计算机分子对接研究得到了证实。此外，cPAmPiCaTc 还表现出优异的血液相容性，这一结果为未来针对 MRSA 感染的有趣金属药物治疗铺平了道路。
