24828-95-3Relevant academic research and scientific papers
Syntheses of Enantiopure 1,2-Ethylenediamines with Tethered Secondary Amines of the Formula H 2NCH 2CH[(CH 2) nNHMe]NH 2(n = 1-4) from α-Amino Acids: New Agents for Asymmetric Catalysis
Kabes, Connor Q.,Gunn, Jack H.,Selbst, Maximilian A.,Lucas, Reagan F.,Gladysz, John A.
, p. 3277 - 3285 (2020/11/02)
Tris(hydrochloride) adducts of the title compounds-are prepared from the inexpensive α-amino acids H 2 N(C=O)CH 2 CH(NH 2)CO 2 H, HO(C=O)(CH 2) n ′ CH(NH 2)CO 2 H (n ′ = 1, 2), and H2 N(CH 2) 4 CH(NH 2)CO 2 H, respectively (steps/overall yield = 5/32, 7/30, 7/33, 5/38). The NH 2 group that is remote from the secondary amine is installed via BH 3 reduction of an amide [-(C=O)NR 2[ derived?-from an α-amino carboxylic acid. The MeNHCH 2 units are introduced by BH 3 reductions of alkyl carbamate [RO(C=O)NHCH 2-; R = Et, t-Bu] or amide [MeHN(C=O)-] moieties.
DIPEPTIDE MIMETICS OF NGF AND BDNF NEUROTROPHINS
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, (2019/04/16)
The invention relates to compounds having either agonist or antagonist activities for the neurotrophins NGF and BDNF and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure. The dimeric structure is produced advantageously by using hexatnethylenediaanine to which dipeptides are attached via their carboxyl groups. The claimed compounds displayed neuroprotective and differentiation-inducing activities in cellular models and enhanced the amount of phosphorylated tyrosine kinase A and the heat shock proteins Hsp32 and Hsp70 in the concentration range of 10 -9 to 10 -5 M. They also displayed neuroprotective, anti-parkinsonian, anti-stroke, anti-ischemic, anti-depressant and anti-amnestic activities in animal models and were active in experimental models of Alzheimer's disease. These in vivo effects of the claimed compounds are displayed in the dose range of 0.01 to 10 mg/kg when administered intraperitoneally.
Replacement of Ala by Aib improves structuration and biological stability in thymine-based α-nucleopeptides
Geotti-Bianchini, Piero,Moretto, Alessandro,Peggion, Cristina,Beyrath, Julien,Bianco, Alberto,Formaggio, Fernando
scheme or table, p. 1315 - 1321 (2010/06/17)
Three thymine-based nucleo-heptapeptides, each containing two nucleo-amino acids and zero, one or four Aib residues, respectively, have been synthesized. A single Aib residue is enough to promote the adoption of a helical structure in our nucleopeptides a
Synthesis and evaluation of lysine derived sulfamides as histone deacetylase inhibitors
Manku, Sukhdev,Allan, Martin,Nguyen, Natalie,Ajamian, Alain,Rodrigue, Jacques,Therrien, Eric,Wang, James,Guo, Tim,Rahil, Jubrail,Petschner, Andrea J.,Nicolescu, Alina,Lefebvre, Sylvain,Li, Zuomei,Fournel, Marielle,Besterman, Jeffrey M.,Deziel, Robert,Wahhab, Amal
scheme or table, p. 1866 - 1870 (2009/11/30)
We have recently reported on a novel class of histone deacetylase (HDAC) inhibitors bearing a sulfamide group as the zinc-binding unit. Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-
SULFAMIDE AND SULFAMATE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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Page/Page column 108, (2010/11/29)
This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I), and racemic and scalemic mixtures, diastereomers and enantiomers thereof: or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein Y, L, Z, W, M, Ra, Rb and Rc are as defined in the specification.
Salen-anthraquinone conjugates. Synthesis, DNA-binding and cleaving properties, effects on topoisomerases and cytotoxicity
Routier, Sylvain,Cotelle, Nicole,Catteau, Jean-Pierre,Bernier, Jean-Luc,Waring, Michael J.,Riou, Jean-Francois,Bailly, Christian
, p. 1185 - 1196 (2007/10/03)
A series of amidoethylamino-anthraquinone derivatives bearing either one or two salen (bis(salicylidene) ethylenediamine) moieties complexed with Cu(II) or Ni(II) have been synthesized, and their DNA-binding and cleaving properties examined. The effects o
