1155573-56-0Relevant articles and documents
Metal-free ring opening of 5-amino-1,4-diaryl-1H-pyrazoles: A facile access to 2-aryl-3-arylazoacrylonitriles
Bandyopadhyay, Debashruti,Chatterjee, Arpita,Kanchithalaivan, Selvaraj,Peruncheralathan, Saravanan,Radhakrishnan, Divya
supporting information, (2022/01/20)
Various 2-aryl-3-arylazoacrylonitriles are synthesized while attempting the intramolecular N-arylation of 5-aminopyrazoles, using the hypervalent iodine reagent. The synthesis involves phenyl iodine diacetate-assisted ring opening of 5-aminopyrazoles at r
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists
Marinozzi, Maura,Carotti, Andrea,Sansone, Emanuele,MacChiarulo, Antonio,Rosatelli, Emiliano,Sardella, Roccaldo,Natalini, Benedetto,Rizzo, Giovanni,Adorini, Luciano,Passeri, Daniela,De Franco, Francesca,Pruzanski, Mark,Pellicciari, Roberto
supporting information; experimental part, p. 3429 - 3445 (2012/07/30)
A virtual screening procedure was applied to the discovery of structurally diverse non-steroidal Farnesoid X Receptor (FXR) agonists. From 117 compounds selected by virtual screening, a total of 47 compounds were found to be FXR agonists, with 34 of them showing activity below a concentration of 20 μM. 1H-Pyrazole[3,4-e][1,4]thiazepin-7-one-based hit compound 7 was chosen for hit-to-lead optimization. A large number of 1H-pyrazole[3,4-e][1,4]thiazepin-7- one derivatives was designed, synthesized, and evaluated by a cell-based luciferase transactivation assay for their agonistic activity against FXR. Most of them exhibited low micromolar range of potency and very high efficacy.