Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists

DOI: 10.1021/jm3002718

Source and publish data:

Journal of Medicinal Chemistry p. 7037 - 7053 (2012)

Update date:2022-08-04

Topics:

Authors:

Huang, Huang

Yu, Ying

Gao, Zhenting

Zhang, Yong

Li, Chenjing

Xu, Xing

Jin, Hui

Yan, Wenzhong

Ma, Ruoqun

Zhu, Jin

Shen, Xu

Jiang, Hualiang

Chen, Lili

Li, Jian

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Article abstract of DOI:10.1021/jm3002718

LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 ± 11.75 μM). On the basis of 11, 26 new derivatives (12a-z) were designed and synthesized accordingly. Five

Full text of DOI:10.1021/jm3002718

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Product name:(Z)-3-(4-(4-isopropoxy-3-methoxybenzylidene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid

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