1384516-10-2Relevant articles and documents
Compound with high affinity with orphan nuclear hormone receptor [alpha], and preparation method and application thereof
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Paragraph 0037-0045; 0081-0086, (2021/05/01)
The invention provides a compound with high affinity with an orphan nuclear hormone receptor [alpha], and a preparation method and application thereof, and belongs to the field of organic synthesis. The structural formula of the compound with high affinity with the orphan nuclear hormone receptor [alpha] is shown as a formula I, wherein A is an ester group. The compound with high affinity with the orphan nuclear hormone receptor [alpha] not only has high affinity with the orphan nuclear hormone receptor [alpha], but also can reduce cell viability, change cell metabolism, change gene transcription in hepatocytes and embryonic stem cells lacking REV-ERB[alpha]. The preparation method of the compound with high affinity with the orphan nuclear hormone receptor [alpha] is simple, raw materials are easy to obtain, and the compound can be used for treating various diseases related to the orphan nuclear hormone receptor [alpha] and has a wide application prospect.
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα
Shin, Youseung,Noel, Romain,Banerjee, Subhashis,Kojetin, Douglas,Song, Xinyi,He, Yuanjun,Lin, Li,Cameron, Michael D.,Burris, Thomas P.,Kamenecka, Theodore M.
scheme or table, p. 4413 - 4417 (2012/07/17)
The structure-activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease.