1,2,4-恶二唑/2-咪唑啉杂合体：用于治疗传染病和癌症的多靶点导向化合物。
1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer.
机构信息
Pharmaceutical Technology Transfer Center, Ushinsky Yaroslavl State Pedagogical University, 108 Respublikanskaya St., Yaroslavl 150000, Russia.
Institute of Chemistry, Saint Petersburg State University, 26 Universitetskii Pr, Peterhof, Saint Petersburg 198504, Russia.
出版信息
Int J Mol Sci. 2019 Apr 5;20(7):1699. doi: 10.3390/ijms20071699.
Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (, ) and Gram-negative (, ) strains. Furthermore, selected compounds markedly inhibited the growth of certain drug-resistant bacteria. Additionally, the study revealed the antiproliferative activity of several antibacterial frontrunners against pancreas ductal adenocarcinoma (PANC-1) cell line, as well as their type-selective monoamine oxidase (MAO) inhibitory profile.
用 1,2,4-噁二唑核取代最近报道的外排泵抑制剂支架中的酰胺部分，得到了一系列新型噁二唑/2-咪唑啉杂合化合物。后者对革兰氏阳性（ ， ）和革兰氏阴性（ ， ）菌株均表现出有希望的抗菌活性。此外，选定的化合物显著抑制了某些耐药菌的生长。此外，该研究还揭示了几种抗菌先导化合物对胰腺导管腺癌（PANC-1）细胞系的增殖活性及其对单胺氧化酶（MAO）的选择性抑制谱。
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