On March 5, 2022, Fang, Yuying; Tan, Qingyun; Zhou, Huihao; Gu, Qiong; Xu, Jun published an article.Application In Synthesis of 3-Hydroxyphenylacetic acid The title of the article was Discovery of novel diphenylbutene derivative ferroptosis inhibitors as neuroprotective agents. And the article contained the following:
Herein, with phenotypic assays, a new diphenylbutene derivative ferroptosis inhibitor, DPT was discovered. Based on this hit, new diphenylbutene derivatives I [R1 = H, 2-OMe, 3-OH, etc.; R2 = H, 3-OH, 4-OH, etc.] synthesized via condensation of (piperazinyl)pyrimidine and (phenyl)-phenylpentadienoic acids II and evaluated their ferroptosis inhibitory activities in HT22 mouse hippocampal neuronal cells and found that three compounds exhibited improved inhibitory activities compared with DPT. Among these active compounds, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] displayed the most potent anti-ferroptosis activity (EC50 = 1.7μM). Further studies demonstrated that compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] was a specific ferroptosis inhibitor. It was revealed that different than the classic ferroptosis inhibitors, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] blocked ferroptosis by increasing FSP1 protein level. Compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] could penetrate blood-brain barrier (BBB). In a rat model of ischemic stroke, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] effectively mitigated cerebral ischemic injury. Therefore, it was confirmed that compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] as a novel ferroptosis inhibitor with a new scaffold, was promising for further development as an agent against neurol. diseases. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Application In Synthesis of 3-Hydroxyphenylacetic acid
The Article related to phenyl pyrimidinyl piperazinyl pentadienone diastereoselective preparation ferroptosis inhibitor dpt, piperazinyl pentadienone phenyl pyrimidinyl diastereoselective preparation adme human, phenylpentadienoic phenyl acid preparation piperazinyl pyrimidine condensation, cinnamaldehyde phenylacetic acid perkin, diphenylbutene, fsp1 and other aspects.Application In Synthesis of 3-Hydroxyphenylacetic acid
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