35304-69-9Relevant academic research and scientific papers
A fluorescent molecular imaging probe with selectivity for soluble tau aggregated protein
Aigbirhio, Franklin I.,Haji-Dheere, Abdul K.,Klenerman, David,Kuan, Wei-Li,Ronchi, Elisabetta,Tóth, Gergely,Thompson, Stephen,Tietz, Ole,Vallin, Benjamin,Zhao, Yanyan
, p. 4773 - 4778 (2020)
Soluble forms of aggregated tau misfolded protein, generally termed oligomers, are considered to be the most toxic species of the different assembly states that are the pathological components of neurodegenerative disorders. Therefore, a critical biomedical need exists for imaging probes that can identify and quantify them. We have designed and synthesized a novel fluorescent probe, pTP-TFE for which binding and selectivity profiles towards aggregated tau and Aβ proteins were assessed. Our results have shown pTP-TFE to be selective for early forms of soluble tau aggregates, with high affinity of dissociation constants (Kd) = 66 nM, and tenfold selectivity over mature tau fibrils. Furthermore, we found that pTP-TFE is selective for tau over Aβ aggregates and had good cell permeability. This selectivity of pTP-TFE towards early forms of aggregated tau protein ex vivo was also supported with studies on human brain tissue containing tau and Aβ pathology. To the best of our knowledge, this is the first fluorescent molecule to be reported to have this form of selectivity profile, which suggests that pTP-TFE is a unique probe candidate for imaging-based detection of early stages of Alzheimer's disease and other tauopathies.
Oxidation of α-trifluoromethyl and non-fluorinated alcohols: Via the merger of oxoammonium cations and photoredox catalysis
Pistritto, Vincent A.,Paolillo, Joshua M.,Bisset, Kathryn A.,Leadbeater, Nicholas E.
supporting information, p. 4715 - 4719 (2018/07/06)
We present an alcohol oxidation strategy to access α-trifluoromethyl ketones (TFMKs) merging catalytic oxoammonium cation oxidation with visible-light photoredox catalysis. This work uses 4-acetamido-(2,2,6,6-tetramethyl-piperidin-1-yl)oxyl as an organic oxidant capable of generating TFMKs in good yields. The methodology serves as an improvement over previous reports of an analogous oxidation strategy requiring superstoichiometric quantities of oxidant. Both primary and secondary non-fluorinated alcohols can also be oxidised in good yields.
COMPOUNDS AND METHODS for the inhibition of HDAC
-
Paragraph 0739-0740, (2015/11/24)
Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
METALLOENZYME INHIBITOR COMPOUNDS
-
Page/Page column 84, (2013/07/05)
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy
Ontoria, Jesus M.,Altamura, Sergio,Di Marco, Annalise,Ferrigno, Federica,Laufer, Ralph,Muraglia, Ester,Palumbi, Maria Cecilia,Rowley, Michael,Scarpelli, Rita,Schultz-Fademrecht, Carsten,Serafini, Sergio,Steinkühler, Christian,Jones, Philip
experimental part, p. 6782 - 6789 (2010/07/02)
5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h, a potent inhibitor of HDAC4 and HDAC6 (HDAC4 WT IC 50 = 310 nM, HDAC6
THIOPHENE AND THIAZOLE SUBSTITUTED TRIFLUOROETHANONE DERIVATIVES AS HISTONE DEACETYLASE (HDAC) INHIBITORS
-
Page/Page column 45, (2008/06/13)
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts and tautomers thereof. Compounds of the present invention are inhibitors of histone deacetylase (HDAC) and are useful for treating cellular proliferative dise
NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME
-
Page/Page column 32, (2008/06/13)
The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
