844648-05-1Relevant academic research and scientific papers
Facile access to chiral 4-substituted chromanes through Rh-catalyzed asymmetric hydrogenation
Tao, Lin,Zhao, Qingyang,Zhang, Xumu,Dong, Xiu-Qin
supporting information, p. 1859 - 1862 (2020/01/21)
Rh/ZhaoPhos-catalyzed asymmetric hydrogenation of a series of (E)-2-(chroman-4-ylidene)acetates was successfully developed to prepare various chiral 4-substituted chromanes with high yields and excellent enantioselectivities (up to 99percent yield, 98percent ee). Moreover, the gram-scale hydrogenation could be performed well in the presence of 0.02 molpercent catalyst loading (TON = 5000), the hydrogenation product was easily converted to access other important compounds, which demonstrated the synthetic utility of this asymmetric catalytic methodology.
Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis
Gobbi, Silvia,Hu, Qingzhong,Zimmer, Christina,Engel, Matthias,Belluti, Federica,Rampa, Angela,Hartmann, Rolf W.,Bisi, Alessandra
, p. 2468 - 2477 (2016/04/10)
The inhibition of corticosteroid biosynthesis could be considered as an emerging strategy to reduce their abnormally high levels, and in this framework CYP11B1 and CYP11B2 represent the most promising targets. In continuing our studies on flavonoid-like scaffolds as privileged structures in medicinal chemistry, in this paper we describe a small library of pyridyl- and imidazolylmethylchromones as potential inhibitors of these enzymes. Testing results proved that position 3 of the chromone scaffold is the most favorable for the introduction of the heme-coordinating heterocycles and, among them, the 4-imidazolyl moiety is the most convenient for the interaction with the heme iron of the selected cytochromes. A low nanomolar inhibitor of CYP11B1 (5c) was obtained, endowed with reasonable selectivity toward CYP11B2 and able to better discriminate with respect to CYP17 and CYP19.
Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor
Battisti, Umberto M.,Corrado, Sandra,Sorbi, Claudia,Cornia, Andrea,Tait, Annalisa,Malfacini, Davide,Cerlesi, Maria Camilla,Calò, Girolamo,Brasili, Livio
supporting information, p. 973 - 983 (2014/07/08)
A series of triazospirodecanone derivatives were synthesized as potential NOP ligands. 8-(Chroman-4-yl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (4) and its 5-fluoro analogue (18) proved to be active as agonists with EC50 values in the submicromolar range. Single enantiomers of compound 4 were separated and tested as NOP agonists; the eutomer R-(+)-4 showed a pEC 50 of 7.34. Finally docking studies were performed on the NOP receptor to identify the most significant stereospecific interactions.
PHARMACEUTICALLY ACTIVE 6-N-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES
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Page/Page column 62, (2009/01/24)
The invention provides compounds of the formula (0), in which the substituents and symbols are as defined in the description. The compounds inhibit the secretion of gastric acid.
Quinoxaline compounds
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Page/Page column 30, (2008/06/13)
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
