677341-21-8Relevant academic research and scientific papers
Synthesis of Cα methylated carboxylic acids: Isosteres of arginine and lysine for use as N-terminal capping residues in polypeptides
Orwig, Kevin S.,Dix, Thomas A.
, p. 7007 - 7009 (2007/10/03)
Replacement of the N-terminal α-amine with the isosteric methyl functionality in bioactive peptides can influence various pharmacokinetic parameters, including hydrophobicity and stability. Cα methylated amino acid analogues are thus of great interest to expand the repertoire of nonnatural synthons available as N-terminal 'capping' residues for peptide-based drug design. Several novel arginine and lysine analogues stereoselectively modified in the Cα position with a methyl group in place of the α-amine were prepared.
Design, synthesis, and evaluation of 4-(4′-aminobenzyl)-2-oxazolidinones as novel inhibitors of the cytochrome P-450 enzyme aromatase
Ahmed, Sabbir,Adat, Shaheen,Murrells, Annabel,Owen, Caroline P.,Amanuel, Yonas
, p. 315 - 331 (2007/10/03)
The synthesis of a series of N-alkylated 4-(4′aminobenzyl)-2-oxazolidinones is described using a synthetically useful scheme which avoids the use of phosgene - since the derivatization is undertaken with the oxazolidin-2-one ring intact. The compounds were tested for human placental aromatase (AR) inhibition in vitro, using [1β, 2β-3H]androstenedione as substrate for the AR enzyme. The compounds were found, in general, to be more potent than the standard compound, amino-glutethimide (AG), and as such proved to be good lead compounds in the search for more specific AR inhibitors.
