Szulczyk Daniel, Tomaszewski Piotr, Jóźwiak Michał, Kozioł Anna E, Lis Tadeusz, Collu David, Iuliano Filippo, Struga Marta
Department of Biochemistry and Pharmacogenomics, Faculty of Pharmacy, Medical University of Warsaw, 02-097 Warsaw, Poland.
Laboratory of Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B, 02-097 Warsaw, Poland.
Molecules. 2017 Mar 6;22(3):409. doi: 10.3390/molecules22030409.
Thirty six novel heterocyclic derivatives of ethyl 2-(2-pyridylacetate) were efficiently synthesized. The new compounds involve the linkage of a 2-pyridyl ring with thiosemicarbazide (compounds -), 1,2,4-triazole (compounds -), 1,3,4-thiadiazole (compounds -), and 1,3,4-oxadiazole (compounds -) moieties. The last group of compounds - involves the connection of a 2-pyridyl ring with 1,2,4-triazole and thiourea. ¹H-NMR, C-NMR and MS methods were used to confirm the structures of the obtained derivatives. The molecular structures of , , and were further confirmed by X-ray crystallography. All obtained compounds were tested in vitro against a number of microorganisms, including Gram-positive cocci, Gram-negative rods and . In addition, the obtained compounds were tested for cytotoxicity and antiviral activity against HIV-1.
高效合成了36种新型的2-(2-吡啶基乙酸酯)乙酯杂环衍生物。这些新化合物包括2-吡啶环与硫代氨基脲(化合物-)、1,2,4-三唑(化合物-)、1,3,4-噻二唑(化合物-)和1,3,4-恶二唑(化合物-)部分的连接。最后一组化合物-涉及2-吡啶环与1,2,4-三唑和硫脲的连接。采用¹H-NMR、C-NMR和MS方法确认了所得衍生物的结构。通过X射线晶体学进一步确认了化合物、、和的分子结构。所有所得化合物均针对多种微生物进行了体外测试,包括革兰氏阳性球菌、革兰氏阴性杆菌和。此外,还对所得化合物进行了细胞毒性和抗HIV-1病毒活性测试。