73087-97-5Relevant academic research and scientific papers
Non-steroidal dissociated glucocorticoid agonists: Indoles as A-ring mimetics and function-regulating pharmacophores
Betageri, Raj,Gilmore, Thomas,Kuzmich, Daniel,Kirrane, Thomas M.,Bentzien, J?rg,Wiedenmayer, Dieter,Bekkali, Younes,Regan, John,Berry, Angela,Latli, Bachir,Kukulka, Alison J.,Fadra, Tazmeen N.,Nelson, Richard M.,Goldrick, Susan,Zuvela-Jelaska, Ljiljana,Souza, Don,Pelletier, Josephine,Dinallo, Roger,Panzenbeck, Mark,Torcellini, Carol,Lee, Heewon,Pack, Edward,Harcken, Christian,Nabozny, Gerald,Thomson, David S.
, p. 6842 - 6851 (2011/12/22)
We report a SAR of non-steroidal glucocorticoid mimetics that utilize indoles as A-ring mimetics. Detailed SAR is discussed with a focus on improving PR and MR selectivity, GR agonism, and in vitro dissociation profile. SAR analysis led to compound (R)-33 which showed high PR and MR selectivity, potent agonist activity, and reduced transactivation activity in the MMTV and aromatase assays. The compound is equipotent to prednisolone in the LPS-TNF model of inflammation. In mouse CIA, at 30 mg/kg compound (R)-33 inhibited disease progression with an efficacy similar to the 3 mg/kg dose of prednisolone.
Tricyclic indole-2-carboxylic acid derivatives
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, (2008/06/13)
A tricyclic indole-2-carboxylic acid derivative represented by the formula 1: STR1 wherein X represents alkyl, halogen or cyano;R 1 represents hydrogen, or a protecting group of carboxyl group;W represents hydrogen, --CO 2 R 3i, --CONR 3i R 4i, --A--CO 2 R 3i or --A--CONR 3i R 4i, wherein --A-- represents alkylene and R 3i and R 4i independently represent hydrogen, alkyl, aryl or substituted aryl,or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.
