Tuberculosis and fungal infections can pose serious threats to human health. In order to find novel antimicrobial agents, 26 novel quinoxaline-1,4-di-N-oxides containing a thiazolidinone moiety were designed and synthesized, and their antimycobacterial activities were evaluated. Among them, compounds 2t, 2u, 2y, and 2z displayed the most potent antimycobacterial activity against Mycobacterium tuberculosis strain H37Rv (minimal inhibitory concentration [MIC] = 1.56 μg/mL). The antifungal activity of all the compounds was also evaluated against Candida albicans, Candida tropicalis, Aspergillus fumigatus, and Cryptococcus neoformans. Compounds 2t, 2u, 2y, and 2z exhibited potential antifungal activities, with an MIC between 2 and 4 μg/mL. Comparative molecular field analysis (CoMFA: q2 = 0.914, r2 = 0.967) and comparative molecular similarity index analysis (CoMSIA: q2 = 0.918, r2 = 0.968) models were established to investigate the structure and antimycobacterial activity relationship. The results of contour maps revealed that electronegative and sterically bulky substituents play an important role in the antimycobacterial activity. Electronegative and sterically bulky substituents are preferred at the C7 position of the quinoxaline ring and the C4 position of the phenyl group to increase the antimycobacterial activity. Additionally, more hydrogen bond donor substituents should be considered at the C2 side chain of the quinoxaline ring to improve the activity.
Mengmeng Zhang,Wei Zhou,Qingqing Wang,Ning Wang,Xin Wang,Youping Liu,Xin Di
In this work, a novel water compatible core–shell magnetic molecularly imprinted nanocomposite (Fe3O4–COOH@MIPs) was synthesized in an acetonitrile–water reaction system by adopting carboxyl group-functionalized Fe3O4 nanoparticles as the magnetic core, olaquindox as the template molecule and acrylamide as the functional monomer. The resulting Fe3O4–COOH@MIPs was characterized and applied as an adsorbent for magnetic solid-phase extraction (MSPE) of three quinoline-1,4-dioxides (QdNOs). The Fe3O4–COOH@MIPs possessed strong magnetic responsiveness, fast adsorption equilibrium rate (equilibrium within 5 min) and excellent selectivity. By coupling Fe3O4–COOH@MIPs based MSPE with high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS), good linearity (R2 ≥ 0.9985) and low limits of detection (0.83–5.0 ng L−1) for QdNOs were obtained. Finally, the proposed method was applied to determine trace QdNOs in environmental water samples, and the recoveries were in the range of 68.08–99.88% with RSD less than 12.5%.
危险品化学品经营许可证（带存储）