School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, China.
Bioorg Med Chem Lett. 2011 Jul 1;21(13):3909-13. doi: 10.1016/j.bmcl.2011.05.035. Epub 2011 May 15.
A series of substituted pyrazolo[1,5-a]pyrazin-4(5H)-one was synthesized by the reaction of ethyl 1-(2-oxo-2-phenylethyl)-3-phenyl-1H-pyrazole-5-carboxylate derivatives and 2-(2-aminoethoxy)ethanol or 2-morpholinoethanamine in the condition of microwave-assisted one-step and solvent-free in a good yield. The structures of the compounds were determined by IR, (1)H NMR and mass spectroscopy. In addition, a representative single-crystal structure was characterized by using X-ray diffraction analysis. Preliminary biological evaluation showed that the compounds could inhibit the growth of A549 and H322 cells in dosage-dependent manners.
通过 1-(2-氧代-2-苯乙基)-3-苯基-1H-吡唑-5-羧酸乙酯衍生物与 2-(2-氨乙氧基)乙醇或 2-(吗啉代)乙胺在微波辅助无溶剂一步反应条件下，合成了一系列取代的吡唑并[1,5-a]吡嗪-4(5H)-酮。化合物的结构通过 IR、(1)H NMR 和质谱进行了确定。此外，还通过 X 射线衍射分析对代表性的单晶结构进行了表征。初步的生物评价表明，这些化合物能够以剂量依赖的方式抑制 A549 和 H322 细胞的生长。
