Maliszewski Dawid, Demirel Rasime, Wróbel Agnieszka, Baradyn Maciej, Ratkiewicz Artur, Drozdowska Danuta
Department of Organic Chemistry, Medical University of Bialystok, 15-089 Bialystok, Poland.
Department of Biology, Eskisehir Technical University, Eskişehir 26555, Turkey.
Pharmaceuticals (Basel). 2023 Sep 4;16(9):1248. doi: 10.3390/ph16091248.
The spectrum of biological properties of s-triazine derivatives is broad and includes anti-microbial, anti-cancer, and anti-neurodegenerative activities, among others. The s-triazine molecule, due to the possibility of substituting three substituents, offers many opportunities to obtain hybrid compounds with a wide variety of activities. A group of 1,3,5 triazine derivatives containing a dipeptide, 2-ethylpiperazine, and a methoxy group as substituents was screened for their antimicrobial activity. An in vitro study was conducted on pathogenic bacteria (, , and ), yeasts (), and filamentous fungi (, , , and ) via microdilution in broth, and the results were compared with antibacterial (Streptomycin) and antifungal (Ketoconazole and Nystatin) antibiotics. Several s-triazine analogues have minimal inhibitory concentrations lower than the standard. To confirm the inhibitory potential of the most active compounds against gyrases and , a bacterial gyrases inhibition assay, and molecular docking studies were performed. The most active s-triazine derivatives contained the -NH-Trp(Boc)-AlaOMe, -NH-Asp(OtBu)-AlaOMe, and -NH-PheOMe moieties in their structures.
均三嗪衍生物的生物学特性范围广泛，包括抗菌、抗癌和抗神经退行性活性等。由于均三嗪分子有可能取代三个取代基，因此为获得具有多种活性的杂化化合物提供了许多机会。对一组含有二肽、2-乙基哌嗪和甲氧基作为取代基的1,3,5-三嗪衍生物进行了抗菌活性筛选。通过肉汤微量稀释法对病原菌（、、和）、酵母（）和丝状真菌（、、和）进行了体外研究，并将结果与抗菌（链霉素）和抗真菌（酮康唑和制霉菌素）抗生素进行了比较。几种均三嗪类似物的最低抑菌浓度低于标准值。为了证实最具活性的化合物对促旋酶和的抑制潜力，进行了细菌促旋酶抑制试验和分子对接研究。最具活性的均三嗪衍生物在其结构中含有-NH-Trp(Boc)-AlaOMe、-NH-Asp(OtBu)-AlaOMe和-NH-PheOMe部分。
