Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India.
Bioorg Med Chem Lett. 2012 Oct 15;22(20):6385-90. doi: 10.1016/j.bmcl.2012.08.071. Epub 2012 Aug 24.
A series of novel 6-methoxy-2-(piperazin-1-yl)-4H-chromen-4-one and 5,7-dimethoxy-2-(piperazin-1-ylmethyl)-4H-chromen-4-one derivatives of biological interest were prepared and screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Among all the compound screened (5a-j and 10k-t), the compounds 5c, 5g, 5h, 10l, 10m, 10n and 10r found to have promising anti-inflammatory activity (up to 65-87% TNF-α and 70-93% IL-6 inhibitory activity) at concentration of 10 μM with reference to standard dexamethasone (71% TNF-a and 84% IL-6 inhibitory activities at 1 μM) while the compounds 5b, 5i, 5j, 10s and 10t found to be potent antimicrobial agent showing even 2 to 2.5-fold more potency than that of standard ciprofloxacin and miconazole at the same MIC value of 10 μg/mL.
一系列具有生物活性的新型 6-甲氧基-2-(哌嗪-1-基)-4H-色烯-4-酮和 5,7-二甲氧基-2-(哌嗪-1-基甲基)-4H-色烯-4-酮衍生物被制备出来，并对其进行了促炎细胞因子（TNF-α 和 IL-6）和抗菌活性（抗细菌和抗真菌）的筛选。在所筛选的所有化合物（5a-j 和 10k-t）中，化合物 5c、5g、5h、10l、10m、10n 和 10r 被发现具有有前途的抗炎活性（在 10 μM 浓度下，TNF-α 抑制率高达 65-87%，IL-6 抑制率高达 70-93%），参考标准地塞米松（在 1 μM 时 TNF-a 抑制率为 71%，IL-6 抑制率为 84%），而化合物 5b、5i、5j、10s 和 10t 则表现出很强的抗菌活性，在相同的 10 μg/mL MIC 值下，其活性比标准环丙沙星和咪康唑强 2 至 2.5 倍。
