Biggadike, Keith; Boudjelal, Mohamed; Clackers, Margaret; Coe, Diane M.; Demaine, Derek A.; Hardy, George W.; Humphreys, Davina; Inglis, Graham G. A.; Johnston, Michael J.; Jones, Haydn T.; House, David; Loiseau, Richard; Needham, Deborah; Skone, Philip A.; Uings, Iain; Veitch, Gemma; Weingarten, Gordon G.; McLay, Iain M.; Macdonald, Simon J. F. published their research in Journal of Medicinal Chemistry on December 27 ,2007. The article was titled 《Nonsteroidal Glucocorticoid Agonists: Tetrahydronaphthalenes with Alternative Steroidal A-Ring Mimetics Possessing Dissociated (Transrepression/Transactivation) Efficacy Selectivity》.Reference of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide The article contains the following contents:
The synthesis and biol. activity of tetrahydronaphthalene derivatives coupled to various heterocycles, e.g. I, are described. These compounds are potent glucocorticoid receptor agonists with efficacy selectivity in an NFκB glucocorticoid receptor (GR) agonist assay (representing transrepression effects) over an MMTV GR agonist assay (representing transactivation effects). Quinolones, indoles, and C- and N-linked quinolines are some of the heterocycles that provide efficacy selectivity. For example, one enantiomer of the isoquinoline II has NFκB agonism with pIC50 of 8.66 (89%) and reduced efficacy in MMTV agonism (6%), and one enantiomer of the quinoline III has NFκB agonism with pIC50 of 9.30 (101%) and reduced efficacy in MMTV agonism with pEC50 of 8.02 (47%). A description of how a compound from each class is modeled in the active site of the receptor is given. In the experimental materials used by the author, we found 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Reference of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide)
2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Reference of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics