80860-42-0Relevant academic research and scientific papers
Impact of γ-Amino Acid Residue Preorganization on α/γ-Peptide Foldamer Helicity in Aqueous Solution
Fisher, Brian F.,Gellman, Samuel H.
, p. 10766 - 10769 (2016)
α/γ-Peptide foldamers containing either γ4-amino acid residues or ring-constrained γ-amino acid residues have been reported to adopt 12-helical secondary structure in nonpolar solvents and in the solid state. These observations have engendered
An Imidazolium-Based Lipid Analogue as a Gene Transfer Agent
Bornemann, Steffen,Galla, Hans-Joachim,Gerke, Volker,Glorius, Frank,Herzog, Marius,Kudruk, Sergej,Linard Matos, Anna Livia,Paulisch, Tiffany O.,Roling, Lena,Winter, Roland
, p. 17176 - 17182 (2020)
A dicationic imidazolium salt is described and investigated towards its application for gene transfer. The polar head group and the long alkyl chains in the backbone contribute to a lipid-like behavior, while an alkyl ammonium group provides the ability for crucial electrostatic interaction for the transfection process. Detailed biophysical studies regarding its impact on biological membrane models and the propensity of vesicle fusion are presented. Fluorescence spectroscopy, atomic force microscopy and confocal fluorescence microscopy show that the imidazolium salt leads to negligible changes in lipid packing, while displaying distinct vesicle fusion properties. Cell culture experiments reveal that mixed liposomes containing the novel imidazolium salt can serve as plasmid DNA delivery vehicles. In contrast, a structurally similar imidazolium salt without a second positive charge showed no ability to support DNA transfection into cultured cells. Thus, we introduce a novel and variable structural motif for cationic lipids, expanding the field of lipofection agents.
De-novo designed β-lysine derivatives can both augment and diminish the proliferation rates of E. coli through the action of Elongation Factor P
Connon, Stephen J.,Ghanim, Magda,Kelly, Vincent P.,McDonnell, Ciara M.,Mike Southern, J.
supporting information, (2022/01/24)
An investigation into the effect of modified β-lysines on the growth rates of eubacterial cells is reported. It is shown that the effects observed are due to the post translational modification of Elongation Factor P (EFP) with these compounds catalysed b
PROBENECID COMPOUNDS FOR THE TREATMENT OF INFLAMMASOME-MEDIATED LUNG DISEASE
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Paragraph 0191; 0206, (2022/01/12)
Disclosed herein are methods, compounds, and compositions for treating or preventing inflammasome-mediated diseases or conditions, including inflammasome-mediated lung diseases or conditions.
(S)-2-AMINO-6-((3-AMINOPROPYL)AMINO)HEXANOIC ACID (APL) FOR USE IN THE TREATMENT OF NON-ALCOHOLIC STEATOHEPATITIS (NASH), LIVER INFLAMMATION, HEPATOCELLULAR BALLOONING, LIVER FIBROSIS AND STEATOSIS
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Paragraph 00148, (2021/10/30)
(S)-2-amino-6-((3-aminopropyl)amino)hexanoic acid (APL) for use in the treatment of non-alcoholic steatohepatitis (NASH), liver inflammation, hepatocellular ballooning, liver fibrosis and steatosis.
COMPOUNDS AND USES THEREOF
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Page/Page column 137; 151-152, (2021/10/15)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0138; 0149-0150, (2021/04/02)
Provided herein are novel bifunctional compounds formed by conjugating AR antagonist moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 Ubiquitin ligase for degradation, and methods of preparation and uses thereof.
Regiocontrolled Reductive Vinylation of Aliphatic 1,3-Dienes with Vinyl Triflates by Nickel Catalysis
Pang, Xiaobo,Zhao, Zhen-Zhen,Wei, Xiao-Xue,Qi, Liangliang,Xu, Guang-Li,Duan, Jicheng,Liu, Xue-Yuan,Shu, Xing-Zhong
supporting information, p. 4536 - 4542 (2021/04/07)
The regiocontrolled functionalization of 1,3-dienes has become a powerful tool for divergent synthesis, yet it remains a long-standing challenge for aliphatic substrates. Herein, we report a reductive approach for a branch-selective 1,2-hydrovinylation of aliphatic 1,3-dienes with R-X electrophiles, which represents a new selectivity pattern for diene functionalization. Simple butadiene, aromatic 1,3-dienes, and highly conjugated polyene were also tolerated. The combination of Ni(0) and the phosphine-nitrile ligand generally resulted in >20:1 regioselectivity with the retention of the geometry of the C3-C4 double bonds. This reaction proceeds with a broad substrate scope, and it allows for the conjugation of two biologically active units to form more complex polyene molecules, such as tetraene and pentaene as well as heptaene.
Straightforward Synthesis of Fluorinated Enals via Photocatalytic α-Perfluoroalkenylation of Aldehydes
Wulkesch, Christian,Czekelius, Constantin
, p. 7425 - 7438 (2021/06/21)
(Per)fluorinated substances represent an important compound class with regard to drug design and material chemistry. We found a mild, operationally simple, and inexpensive photocatalytic perfluoroalkenylation reaction giving tetrasubstituted, highly electron-deficient enals straight from aldehydes. This one-step reaction tolerates various functional groups and can be applied to a wide range of substrates giving the products in yields of 52-84%.
A Modular and Diastereoselective 5 + 1 Cyclization Approach to N-(Hetero)Aryl Piperidines
Larsen, Matthew A.,Hennessy, Elisabeth T.,Deem, Madeleine C.,Lam, Yu-Hong,Saurí, Josep,Sather, Aaron C.
supporting information, p. 726 - 732 (2020/01/31)
A new general de novo synthesis of pharmaceutically important N-(hetero)aryl piperidines is reported. This protocol uses a robustly diastereoselective reductive amination/aza-Michael reaction sequence to achieve rapid construction of complex polysubstituted ring systems starting from widely available heterocyclic amine nucleophiles and carbonyl electrophiles. Notably, the diastereoselectivity of this process is enhanced by the presence of water, and DFT calculations support a stereochemical model involving a facially selective protonation of a water-coordinated enol intermediate.
