75541-62-7Relevant academic research and scientific papers
Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile
Wilson, Kenneth J.,Xiao, Jingbo,Chen, Catherine Z.,Huang, Zaohua,Agoulnik, Irina U.,Ferrer, Marc,Southall, Noel,Hu, Xin,Zheng, Wei,Xu, Xin,Wang, Amy,Myhr, Courtney,Barnaeva, Elena,George, Emmett R.,Agoulnik, Alexander I.,Marugan, Juan J.
, p. 79 - 92 (2018/07/06)
A dose responsive quantitative high throughput screen (qHTS) of >350,000 compounds against a human relaxin/insulin-like family peptide receptor (RXFP1) transfected HEK293 cell line identified 2-acetamido-N-phenylbenzamides 1 and 3 with modest agonist acti
MODULATORS OF THE RELAXIN RECEPTOR 1
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Paragraph 0246-0247, (2015/05/05)
Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardi
Synthesis and structure-activity relationships of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines as a new class of gastric H+/K+-ATPase inhibitors
Yamakawa,Matsukura,Nomura,Yoshioka,Masaki,Igata,Okabe
, p. 1746 - 1752 (2007/10/02)
A series of N-substituted 2-[(2-imidazolylsulfinyl)methyl]anilines was synthesized and evaluated for its biological activity against H+/K+-ATPase prepared from rabbit stomach and gastric acid secretions in Heidenhain pouch dogs. Monoalkyl substituents on the nitrogen atom of the aniline moiety markedly inhibited the enzyme activity to the same degree as omeprazole, a representative H+/K+-ATPase inhibitor. Most of these compounds, administered at 3 mg/kg i.v. inhibited histamine-stimulated gastric acid secretion. The inhibitory activity of these derivatives on the enzymes at pH 6.0 was more potent than that at pH 7.4, and was distinctly correlated to stability in aqueous solution at pH 5.0.
