Department of Organic Chemistry, Kaunas University of Technology, Radvilėnų Rd. 19, LT-50254 Kaunas, Lithuania.
Department of Veterinary Pathobiology, Veterinary Academy, Lithuanian University of Health Sciences, Tilžės Str. 18, LT-47181 Kaunas, Lithuania.
Molecules. 2020 May 22;25(10):2433. doi: 10.3390/molecules25102433.
Thiazole derivatives attract the attention of scientists both in the field of organic synthesis and bioactivity research due to their high biological activity. In the present study, thiazole ring was obtained by the interaction of 1-(4-(bromoacetyl)phenyl)-5-oxopyrrolidine-3-carboxylic acid with thiocarbamide or benzenecarbothioamide, as well as tioureido acid. A series of substituted 1-(3-(1,3-thiazol-2-yl)phenyl)-5-oxopyrrolidines with pyrrolidinone, thiazole, pyrrole, 1,2,4-triazole, oxadiazole and benzimidazole heterocyclic fragments were synthesized and their antibacterial properties were evaluated against Gram-positive strains of , , and Gram-negative , and . The vast majority of compounds exhibited between twofold and 16-fold increased antibacterial effect against the test-cultures when compared with .
噻唑衍生物由于其高生物活性，引起了有机合成和生物活性研究领域科学家的关注。在本研究中，噻唑环是通过 1-(4-(溴乙酰基)苯基)-5-氧代吡咯烷-3-羧酸与硫代脲或苯甲硫酰胺以及硫脲酸的相互作用得到的。一系列取代的 1-(3-(1,3-噻唑-2-基)苯基)-5-氧代吡咯烷与吡咯烷酮、噻唑、吡咯、1,2,4-三唑、恶二唑和苯并咪唑杂环片段被合成，并评估了它们对革兰氏阳性菌株 、 、 和革兰氏阴性菌株 、 、 的抗菌性能。与 相比，绝大多数化合物对测试培养物的抗菌效果提高了两到 16 倍。
