Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų Rd. 19, LT-50254 Kaunas, Lithuania.
Thermo Fisher Scientific, V. A. Graičiūno st. 8, LT-02241 Vilnius, Lithuania.
Molecules. 2021 Apr 29;26(9):2597. doi: 10.3390/molecules26092597.
The aminobenzoic acid was applied for the synthesis of substituted 1-phenyl-5-oxopyrrolidine derivatives containing benzimidazole, azole, oxadiazole, triazole, dihydrazone, and dithiosemicarbazide moieties in the structure. All the obtained compounds were evaluated for their in vitro antimicrobial activity against , , , , and by using MIC and MBC assays. This study showed a good bactericidal activity of -amino acid and benzimidazoles derivatives. The antimicrobial activity of the most promising compounds was higher than ampicillin. Furthermore, two benzimidazoles demonstrated good antimicrobial activity against (MIC 15.62 µg/mL) that was four times more potent than ampicillin (MIC 65 µg/mL). Further studies are needed to better understand the mechanism of the antimicrobial activity as well as to generate antimicrobial compounds based on the 1-phenyl-5-oxopyrrolidine scaffold.
将氨基苯甲酸用于合成取代的 1-苯基-5-氧代吡咯烷衍生物，这些衍生物结构中含有苯并咪唑、唑、噁二唑、三唑、双腙和二硫代缩氨基脲部分。所有获得的化合物都通过 MIC 和 MBC 测定法评估了它们对 、 、 、 和 的体外抗菌活性。这项研究表明 - 氨基酸和苯并咪唑衍生物具有良好的杀菌活性。最有前途的化合物的抗菌活性高于氨苄西林。此外，两种苯并咪唑对 （MIC 15.62 µg/mL）具有良好的抗菌活性，是氨苄西林（MIC 65 µg/mL）的四倍。需要进一步研究以更好地了解抗菌活性的机制，并基于 1-苯基-5-氧代吡咯烷支架生成抗菌化合物。
