20920-99-4Relevant academic research and scientific papers
3,4-Dihydro-3-methyl-6-nitro-2H-1,3-benzoxazin-2-one, a Reagent for Labeling p-Nitrophenyl Esterases with a Chromophoric Reporter Group - Synthesis and Reaction with Chymotrypsin
Kitson, Trevor M.,Freeman, Graham H.
, p. 354 - 365 (1993)
We reported the synthesis of 3,4-dihydro-3-methyl-6-nitro-2H-1,3-benzoxazin-2-one (DMNB), a close structural anlogue of p-nitrophenyl dimethylcarbamate.DMNB is unstable in aqueous solution when exposed to light, but is stable in the dark.The compound reac
Novel chromogenic aminopeptidase substrates for the detection and identification of clinically important microorganisms
Cellier, Marie,James, Arthur L.,Orenga, Sylvain,Perry, John D.,Rasul, Ari K.,Robinson, Shaun N.,Stanforth, Stephen P.
, p. 5249 - 5269 (2014/12/11)
A series of amino acid derivatives 8-10, 42 and 43 have been prepared as chromogenic enzyme substrates in order to detect aminopeptidase activity in clinically important Gram-negative and Gram-positive bacteria. Enzymatic hydrolysis liberates the amino ac
Design, synthesis and in vitro pharmacology of GluK1 and GluK3 antagonists. Studies towards the design of subtype-selective antagonists through 2-carboxyethyl-phenylalanines with substituents interacting with non-conserved residues in the GluK binding sites
Sk?ld, Niklas,Nielsen, Birgitte,Olsen, Jacob,Han, Liwei,Olsen, Lars,Madsen, Ulf,Kristensen, Jesper L.,Pickering, Darryl S.,Johansen, Tommy N.
, p. 5368 - 5377 (2014/12/11)
In order to identify compounds selective for the GluK1 and GluK3 subtypes of kainate receptors we have designed and synthesized a series of (S)-2-amino-3-((2-carboxyethyl)phenyl)propanoic acid analogs with hydrogen bond donating and accepting substituents on the aromatic ring. Based on crystal structures of GluK1 in complex with related ligands, the compounds were designed to explore possible interactions with non-conserved residues outside the glutamate ligand binding site and challenge the water binding network. Apart from obtaining GluK1 selective antagonists one analog with a phenyl-substituted urea (compound 31) showed some preference for GluK3 over GluK1-receptors. Docking studies indicate that this preference may be attributed to contacts between the NH of the urea substituent and non-conserved Ser741 and Ser761 residues.
Syntheses of Triazolophthalide and Triazolodihydrocoumarin
Katritzky, Alan R.,Ji, Fu-Bao,Fan, Wei-Qiang,Beretta, Paolo,Bertoldi, M.
, p. 1519 - 1523 (2007/10/02)
Triazolophthalide has been synthesized in a seven step sequence from phthalide in 24percent overall yield, and triazolodihydrocoumarin has been prepared in nine steps from dihydrocoumarin in 20percent overall yield.The 1H and 13C nmr spectra and the tautomeric equilibria of the final compounds and intermediates are discussed.
