23781-00-2Relevant academic research and scientific papers
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists
Lotesta, Stephen D.,Marcus, Andrew P.,Zheng, Yajun,Leftheris, Katerina,Noto, Paul B.,Meng, Shi,Kandpal, Geeta,Chen, Guozhou,Zhou, Jing,McKeever, Brian,Bukhtiyarov, Yuri,Zhao, Yi,Lala, Deepak S.,Singh, Suresh B.,McGeehan, Gerard M.
supporting information, p. 1384 - 1391 (2016/03/01)
Mineralocorticoid receptor (MR) antagonists continue to be a prevalent area of research in the pharmaceutical industry. Herein we report the discovery of various spirooxindole and dibenzoxazepine constructs as potent MR antagonists. SAR analysis of our spirooxindole hit led to highly potent compounds containing polar solubilizing groups, which interact with the helix-11 region of the MR ligand binding domain (LBD). Various dibenzoxazepine moieties were also prepared in an effort to replace a known dibenzoxepane system which interacts with the hydrophobic region of the MR LBD. In addition, an X-ray crystal structure was obtained from a highly potent compound which was shown to exhibit both partial agonist and antagonist modes of action against MR.
Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1
Sutin, Lori,Andersson, Soeren,Bergquist, Lars,Castro, Victor M.,Danielsson, Eva,James, Stephen,Henriksson, Martin,Johansson, Lars,Kaiser, Christina,Flyren, Katarina,Williams, Meredith
, p. 4837 - 4840 (2008/02/11)
2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented.
2-Amino-5-spiro substituted oxazoline-4-one compounds
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, (2008/06/13)
A novel series of 2-amino-5-spiro substituted oxazolin-4-ones and intermediates for making said compounds. These compounds are prepared by first converting the appropriately substituted cycloketone to the corresponding cyclocyanohydrin; converting this co
