Department of Chemistry & Medical Chemistry, College of Science and Technology, Research & Education Center for Advanced Silicon Materials, Yonsei University, Wonju, Gangwon-Do 220-710, South Korea.
Eur J Med Chem. 2013 Apr;62:84-8. doi: 10.1016/j.ejmech.2012.12.035. Epub 2012 Dec 23.
A new class of sila-substituted 1,3,4-oxadiazoles was synthesized by a convenient synthetic method. Both silathio/silasulfonyl acetic acids were efficiently condensed with benzohydrazides in the presence of phosphorus oxychloride to give sila-substituted 1,3,4-oxadiazoles in high yields. The compounds displayed variable extent of anti-allergic activity on IgE/Ag-stimulated RBL-2H3 cells at 50 and 100 μM concentrations. Compounds having sulfonyl moiety with bis(trimethylsilyl)-1,3,4-oxadiazoles (5a-c), exhibited better anti-allergic activities than those of compounds having sulphur moiety with bis(trimethylsilyl)-1,3,4-oxadiazoles (4a-c).
一类新型的硅取代 1,3,4-噁二唑类化合物通过一种简便的合成方法合成。在三氯氧磷存在下，硅硫/硅砜基乙酸与苯甲酰肼高效缩合，以高产率得到硅取代的 1,3,4-噁二唑类化合物。这些化合物在 50 和 100 μM 浓度下对 IgE/Ag 刺激的 RBL-2H3 细胞显示出不同程度的抗过敏活性。具有双（三甲基硅基）-1,3,4-噁二唑磺酰基的化合物（5a-c）比具有双（三甲基硅基）-1,3,4-噁二唑硫基的化合物（4a-c）具有更好的抗过敏活性。
