Department of Chemistry, Faculty of Science, University of Kragujevac, Radoja Domanovića 12, Kragujevac 34000, Serbia.
Department of Sciences, Institute for Information Technologies Kragujevac, University of Kragujevac, Jovana Cvijića bb, Kragujevac 34000, Serbia.
Med Chem. 2022;18(7):784-790. doi: 10.2174/1573406418666220304230342.
It is known that pyrrolidinone derivates belong to a class of biologically active compounds with a broad spectrum of biological actions. Nowadays, many scientists are making an effort in the discovery of more effective ways to eliminate reactive oxygen species (ROS) that cause oxidative stress or to eliminate the harmful microorganisms from the organism in humans. Therefore, pyrrolidinones seem to be great candidates for the research of this field.
The antimicrobial activity of tested compounds was estimated by the determination of the minimal inhibitory concentration by the broth micro-dilution method against four species of bacteria and five species of fungi. The antioxidant activity was evaluated by free radical scavenging and reducing power.
Among the tested compounds, P22 showed marked antibacterial activity on Staphylococcus aureus with a MIC value of 0.312 mg/mL. Maximum antifungal activity with MIC value 0.625 mg/mL was shown by P23 and P25 compounds against Trichophyton mentagrophytes. Tested samples showed a relatively strong scavenging activity on DPPH radical (IC ranged from 166.75- 727.17 μg/mL). The strongest DPPH radical scavenging activity was shown by P3 compound with an IC value of 166.75 μg/mL. Moreover, the tested compounds had effective reducing power. Compounds P3, P10, and P13 showed the highest reducing power than those from the other samples. Results of the interactions between DNA and P3 indicated that P3 had the affinity to displace EB from the EB-DNA complex through intercalation [K = (1.4 ± 0.1) × 10 M], while K values obtained via titration of BSA with P23 or P25 [K = (6.2 ± 0.2) and (5.0 ± 0.2) × 10 M] indicate that the notable quantity of the drug can be transmitted to the cells.
Achieved results indicate that our compounds are potential candidates for use as medicaments.
众所周知，吡咯烷酮衍生物属于具有广泛生物活性的生物活性化合物类。如今，许多科学家正在努力寻找更有效的方法来消除活性氧（ROS），以消除氧化应激，或从人体中消除有害微生物。因此，吡咯烷酮类化合物似乎是该领域研究的理想选择。
采用肉汤微量稀释法测定四种细菌和五种真菌的最小抑菌浓度（MIC）来评估测试化合物的抗菌活性。通过自由基清除和还原能力来评估抗氧化活性。
在所测试的化合物中，P22 对金黄色葡萄球菌表现出显著的抗菌活性，MIC 值为 0.312mg/mL。P23 和 P25 化合物对须癣毛癣菌的抗真菌活性最强，MIC 值为 0.625mg/mL。测试样品对 DPPH 自由基具有较强的清除活性（IC 值范围为 166.75-727.17μg/mL）。P3 化合物表现出最强的 DPPH 自由基清除活性，IC 值为 166.75μg/mL。此外，这些测试化合物具有有效的还原能力。化合物 P3、P10 和 P13 显示出比其他样品更高的还原能力。P3 与 EB-DNA 复合物的相互作用结果表明，P3 通过嵌入作用具有取代 EB 的亲和力[K=（1.4±0.1）×10 M]，而通过 P23 或 P25 滴定 BSA 获得的 K 值[K=（6.2±0.2）和（5.0±0.2）×10 M]表明，大量药物可以传递到细胞中。
研究结果表明，我们的化合物可能是作为药物使用的潜在候选物。
