28050-38-6Relevant articles and documents
Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands
Festa, Carmen,Renga, Barbara,D'Amore, Claudio,Sepe, Valentina,Finamore, Claudia,De Marino, Simona,Carino, Adriana,Cipriani, Sabrina,Monti, Maria Chiara,Zampella, Angela,Fiorucci, Stefano
, p. 8477 - 8495 (2015/01/09)
Nuclear and G-protein coupled receptors are considered major targets for drug discovery. FXR and GP-BAR1, two bile acid-activated receptors, have gained increasing consideration as druggable receptors. Because endogenous bile acids often target both receptor families, the development of selective ligands has been proven difficult, exposing patients to side effects linked to an unwanted activation of one of the two receptors. In the present study, we describe a novel library of semisynthetic bile acid derivatives obtained by modifications on the cholane scaffold. The pharmacological characterization of this library led to the discovery of 7α-hydroxy-5β-cholan-24-sulfate (7), 6β-ethyl-3α,7β-dihydroxy-5β-cholan-24-ol (EUDCOH, 26), and 6α-ethyl-3α, 7α-dihydroxy-24-nor-5β-cholan-23-ol (NorECDCOH, 30) as novel ligands for FXR and GP-BAR1 that might hold utility in the treatment of FXR and GP-BAR1 mediated disorders.
Microwave-assisted synthesis and in vitro antibacterial activity of novel steroidal thiosemicarbazone derivatives
Zhao, Zhigang,Shi, Zhichuan,Liu, Min,Liu, Xingli
, p. 7730 - 7734 (2013/02/22)
Herein, we reported the synthesis of 16 novel steroidal thiosemicarbazone derivatives via the condensation of steroidal ketones and substituted thiosemicarbazides under solvent-free conditions using microwave irradiation. The yields obtained are in the ra
POTENTIAL BILE ACID METABOLITES. 5. 12β-HYDROXY ACIDS BY STEREOSELECTIVE REDUCTION
Chang, Frederic C.
, p. 875 - 880 (2007/10/02)
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