130406-34-7Relevant academic research and scientific papers
pH-Controlled recognition of amino acids by urea derivatives of β-cyclodextrin
Stepniak, Pawel,Lainer, Bruno,Chmurski, Kazimierz,Jurczak, Janusz
, p. 15742 - 15746 (2017)
Water soluble amphiphilic urea-substituted β-cyclodextrins were synthesized and applied as amino acid receptors. A great affinity towards nonpolar amino acids was observed, ranging from 2300 M?1 for alanine to 54?800 M?1 for tryptoph
Bifunctional iminophosphorane organocatalysts for enantioselective synthesis: Application to the ketimine nitro-Mannich reaction
Nunez, Marta G.,Farley, Alistair J. M.,Dixon, Darren J.
, p. 16348 - 16351 (2013/12/04)
The design, synthesis, and development of a new class of modular, strongly basic, and tunable bifunctional Bronsted base/H-bond-donor organocatalysts are reported. These catalysts incorporate a triaryliminophosphorane as the Bronsted basic moiety and are readily synthesized via a last step Staudinger reaction of a chiral organoazide and a triarylphosphine. Their application to the first general enantioselective organocatalytic nitro-Mannich reaction of nitromethane to unactivated ketone-derived imines allows the enantioselective construction of β-nitroamines possessing a fully substituted carbon atom. The reaction is amenable to multigram scale-up, and the products are useful for the synthesis of enantiopure 1,2-diamine and α-amino acid derivatives.
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
Stauffer, Shaun R.,Stanton, Matthew G.,Gregro, Alison R.,Steinbeiser, Melissa A.,Shaffer, Jennifer R.,Nantermet, Philippe G.,Barrow, James C.,Rittle, Kenneth E.,Collusi, Dennis,Espeseth, Amy S.,Lai, Ming-Tain,Pietrak, Beth L.,Holloway, M. Katharine,McGaughey, Georgia B.,Munshi, Sanjeev K.,Hochman, Jerome H.,Simon, Adam J.,Selnick, Harold G.,Graham, Samuel L.,Vacca, Joseph P.
, p. 1788 - 1792 (2008/02/02)
A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1 inhibitors containing an amine transition-state isostere were synthesized and shown to be highly potent in both enzymatic and cell-based assays. These inhibitors contain a trans-S,S-methyl cyclopropane P3 which bind BACE-1 in a 10s-loop down conformation giving rise to highly potent compounds with favorable molecular weight and moderate to high susceptibility to P-glycoprotein (P-gp) efflux.
Tricyclic erythromycin derivatives
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, (2008/06/13)
Compounds, or pharmaceutically acceptable salts and esters thereof, of the formula: wherein A, B, D and E, R1, R2, and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of bacterial infections with such compositions, and processes for the preparation of the compounds.
Preparation and ring-opening reactions of N-diphenylphosphinyl aziridines
Cantrill, Alex A.,Osborn, Helen M. I.,Sweeney, Joseph
, p. 2181 - 2208 (2007/10/03)
Monochiral N-Diphenyphosphinyl aziridines ('N-Dpp azinidines') may efficiently be prepared from monochiral 2-aminoalcohols. Such aziridines undergo ring-opening reaction with a variety of nucleophiles in good yield. Dephosphinylation is accomplished under mild conditions.
Rationally Designed "Dipeptoid" Analogues of CCK. α-Methyltryptophan Derivatives as Highly Selective and Orally Active Gastrin and CCK-B Antagonists with Potent Anxiolytic Properties
Horwell, David C.,Hughes, John,Hunter, John C.,Pritchard, Martyn C.,Richardson, Reginald S.,at al.
, p. 404 - 414 (2007/10/02)
This paper describes the synthesis and structure-activity relationships (SAR) leading to the first rational design of "dipeptoid" analogues of the neuropeptide cholecystokinin (CCK).Compounds *,S*)>-4-2-3-(1H-indol-3-yl)-2-m
