20950-96-3Relevant articles and documents
Discovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I
Chen, Caiping,Cheng, Keguang,Cheng, Yalong,Dai, Liang,Li, Haobin,Qian, Ming,Sun, Geng,Wang, Pengfei,Wen, Xiaoan,Xu, Qing-Long,You, Yanping,Yuan, Haoliang,Zhou, Xinyu
supporting information, (2020/06/08)
Activation of AMPK emerges as a potential therapeutic approach to metabolic diseases. AdipoRon is claimed to be an adiponectin receptor agonist that activates AMPK through adiponectin receptor 1 (AdipoR1). However, AdipoRon also exhibits moderate inhibition of mitochondrial complex I, leading to increased risk of lactic acidosis. In order to find novel AdipoRon analogues that activate AMPK without inhibition of complex I, 27 analogues of AdipoRon were designed, synthesized and biologically evaluated. As results, benzyloxy arylamide B10 was identified as a potent AMPK activator without inhibition of complex I. B10 dose-dependently improved glucose tolerance in normal mice, and significantly lowered fasting blood glucose level and ameliorated insulin resistance in db/db diabetic mice. More importantly, unlike the pan-AMPK activator MK-8722, B10 did not cause cardiac hypertrophy, probably owing to its selective activation of AMPK in the muscle tissue but not in the heart tissue. Together, B10 represents a novel class of AMPK activators with promising therapeutic potential against metabolic disease.
Synthesis, cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones
Du, Guohua,Jia, Xinxin,Li, Yan,Liu, Qi,Wang, Shiyi,Zeng, Binglin,Zhang, Chen
, (2020/05/29)
Parthenolide is an important sesquiterpene lactone with potent anticancer activities. In order to further improve its biological activity, a series of parthenolide semicarbazone or thiosemicarbazone derivatives was synthesized and evaluated for their anti
2 - Amino pyrimidine compounds and their use (by machine translation)
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Paragraph 0099; 0110; 0111, (2019/10/22)
The invention belongs to the technical field of pharmaceutical chemical synthesis, relates to the general formula (I) indicated by the 2 - amino pyrimidine compounds and their pharmaceutically acceptable salt, solvate or prodrug, their method of preparation and containing pharmaceutical composition of said compound, wherein substituent R1 , R2 , R6 With the meanings given in the specification. The invention also relates to the compounds of the formula I or its pharmaceutical composition for treating and/or preventing malignant blood diseases or other proliferative diseases in the use of the medicament. (by machine translation)