423730-82-9Relevant academic research and scientific papers
Microwave assisted synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from substituted amidoximes and benzoyl cyanides
Kandre, Shivaji,Bhagat, Pundlik Rambhau,Sharma, Rajiv,Gupte, Amol
supporting information, p. 3526 - 3529 (2013/07/05)
We report herein the synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from amidoximes and substituted or unsubstituted benzoyl cyanides under microwave irradiation. Substituted or unsubstituted O-carboxyphenyl amidoxime is a key intermediate of this alternative method developed for the synthesis of these heterocycles. These reactions employ simple synthetic protocols devoid of lengthy purification procedures and proceed with good yield.
Design, synthesis and biological activity evaluation of 2,5-diphenyl-1,3,4-oxadiazole derivatives as novel inhibitors of fructose-1,6-bisphosphatase
He, Hai-Bing,Gao, Li-Xin,Zhou, Yue-Yang,Liu, Ting,Tang, Jie,Gong, Xue-Ping,Qiu, Wen-Wei,Li, Jing-Ya,Li, Jia,Yang, Fan
, p. 2693 - 2712 (2013/01/15)
Fructose-1,6-bisphosphatase (FBPase), an important gluconeogenic enzyme, catalyzes the hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate. The effort to discover new FBPase inhibitors was carried out by high-throughput screening (HTS) of a library of 56,000 lead-like compounds, and a 2,5-diphenyl-1,3,4-oxadiazole (3a, IC50 = 15.45 μM) which bearing no phosphate group was identified as a potential FBPase inhibitor for the first time. Structure-activity-relationship (SAR) research of a series of analogues obtained by modifying the substituent groups and replacing the 1,3,4-oxadiazole with several other heterocycles disclosed the key structure and substituent groups related to the binding with FBPase.
