80894-21-9Relevant academic research and scientific papers
PEG-modified aziridines for stereoselective synthesis of water-soluble fulleropyrrolidines
Kazakova, Angelina V.,Konev, Alexander S.,Zorin, Ivan M.,Poshekhonov, Igor S.,Korzhikov-Vlakh, Viktor A.,Khlebnikov, Alexander F.
, p. 9864 - 9873 (2019/12/06)
Diastereoselective synthesis of water-soluble fullerene compounds bearing a pharmacophore pyrrolofullerene-2′,5′-dicarboxylate unit is reported. The stereocontrol of the product configuration is achieved through stereospecificity of two consecutive concer
Synthesis of 1,2,3-triazole linked galactopyranosides and evaluation of cholera toxin inhibition
Leaver, David J.,Dawson, Raymond M.,White, Jonathan M.,Polyzos, Anastasios,Hughes, Andrew B.
supporting information; experimental part, p. 8465 - 8474 (2012/04/23)
We report the synthesis of a series of bivalent 1,2,3-triazole linked galactopyranosides as potential inhibitors of cholera toxin (CT). The inhibitory activity of the bivalent series was examined (ELISA) and the series showed low inhibitory activity (millimolar IC50s). Conversely, the monomeric galactotriazole analogues were strong inhibitors of cholera toxin (IC 50 = 71-75 μM). The Royal Society of Chemistry 2011.
Lack of effect of the length of oligoglycine- and oligo(ethylene glycol)-derived para-substituents on the affinity of benzenesulfonamides for carbonic anhydrase II in solution
Jain, Ahamindra,Huang, Shaw G.,Whitesides, George M.
, p. 5057 - 5062 (2007/10/02)
Using 1H NMR spectroscopy, values of T2 have been determined for the methylene protons of the oligoglycine moieties of para-substituted benzenesulfonamides having structures H2NO2SC6H4CO(Gly)(n)OH (n = 1-6) bound at the active site of bovine carbonic anhydrase II (CA, EC 4.2.1.1). These values have been correlated with measurements of dissociation constants of these complexes, in order to infer motion of these ligands when bound to the enzyme. Motion of glycines 1-3 (those closest to the aryl ring) is hindered by their proximity to the protein; motion of glycines 4-6 is relatively unhindered. Despite the restriction to motion inferred for glycines 1-3, the values of K(d) for the six compounds (n = 1-6, 1-6) are indistinguishable within experimental uncertainty (± 20%): K(d) in μM (n) 0.30 (1); 0.26 (2); 0.33 (3); 0.37 (4); 0.37 (5); 0.34 (6). There is, therefore, an unexpected compensation of the loss in conformational entropy on binding by another contributor to the free energy.
ETUDE DE LA CHIMIOSELECTIVITE DE LA REACTION DES DICHLOROBORANES AVEC LES AZIDES FONCTIONNELS: UNE SYNTHESE EFFICACE D'AMINES SECONDAIRES FONCTIONNALISEES.
Carboni, B.,Vaultier, M.,Carrie, R.
, p. 1799 - 1810 (2007/10/02)
The reaction of cyclohexyldichloroborane, used as a model, with a wide variety of functionalized azides has been studied.It has been shown to be an efficient synthesis of secondary amines in terms of chemioselectivity, yields and wide applicability.
