202402-02-6Relevant articles and documents
NRF2 REGULATORS
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Page/Page column 378; 379, (2015/07/07)
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
Investigations into the mechanism of lactamization of lactones yielding in a novel route to biologically active tryptamine derivatives
Decker, Michael,Nguyen, Thi Thanh Huyen,Lehmann, Jochen
, p. 4567 - 4578 (2007/10/03)
The mechanism of lactamization of corresponding lactones was investigated by means of gas chromatography and synthesis of possible intermediates as references. Lactones react with amines via the amino acid with subsequent elimination of water to the corresponding lactams. In the first step, also hydroxyamides are in equilibrium with the lactones and amines, respectively, which are not able to form the amide though. This mechanism opens a new approach for the synthesis of Nβ-disubstituted tryptamines.
2-Pyrrolidinone moiety is not critical for the cognition-enhancing activity of piracetam-like drugs
Scapecchi, Serena,Martelli, Cecilia,Ghelardini, Carla,Guandalini, Luca,Martini, Elisabetta,Gualtieri, Fulvio
, p. 715 - 722 (2007/10/03)
Following the indications of previous work, 2-pyrrolidinone moiety of piracetam and piracetam-like compounds has been opened to the corresponding amide derivatives. As found previously in the case of 1,4-diazabicyclo[4.3.0]nonan-9-one compounds, the cognition-enhancing activity of 2-pyrrolidinone compounds is maintained in most cases, suggesting that this moiety is not crucial for activity.