1278585-69-5Relevant articles and documents
Discovery of dronedarone and its analogues as NLRP3 inflammasome inhibitors with potent anti-inflammation activity
Chen, Hao,Chen, Xiuhui,Sun, Ping,Wu, Dan,Yue, Hu,Pan, Jintao,Li, Xinxuan,Zhang, Cheng,Wu, Xinyi,Hua, Lei,Hu, Wenhui,Yang, Zhongjin
, (2021)
Inhibiting NLRP3 inflammasome activation is a prospective therapeutic strategy for uncontrolled inflammatory diseases. It is the first time that dronedarone, a multiply ion channel blocker, was identified as a NLRP3-inflammasome inhibitor with an IC50 value of 6.84 μM against IL-1β release. A series of novel 5-amide benzofuran derivatives were designed and synthesized as NLRP3-inflammasome inhibitors. Compound 8c showed slightly increased activity (IC50 = 3.85 μM) against IL-1β release. Notably, treatment with 8c could significantly inhibit NLRP3-mediated IL-1β release and ameliorate peritoneal inflammation in a mouse model of sepsis. Collectively, 8c is a promising lead compound for further chemical development as a NLRP3 inhibitor with anti-inflammation effects.
2-butyl-3 - (4-substituted propoxy benzoyl) - 5-substituted aminobenzofuran and its application
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, (2017/01/19)
The invention discloses 2-n-butyl-3-(4-subsitituted propylbenzoyl)-5-substituted amino benzofuran and application thereof. The 2-n-butyl-3-(4-subsitituted propylbenzoyl)-5-substituted amino benzofuran can be used for preparing dronedarone and pharmaceutic
PROCESS FOR PREPARING AMINOBENZOFURAN DERIVATIVES
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, (2013/03/26)
This disclosure relates to a process for preparing 5-aminobenzofuran derivatives of general formula (I): in which R1 and R2 are as defined in the description, by treating a 5-N-alkylamidobenzofuran derivative of general formula (II): in which R1, R2, and R3 are as defined in the description, with a strong acid, so as to form an acid addition salt of the compound of formula (I), which salt is itself treated, if necessary, with a basic agent so as to form this compound of formula (I) in free base form.