37034-31-4Relevant academic research and scientific papers
Synthesis and characterization of novel chitosan-dopamine or chitosan-tyrosine conjugates for potential nose-to-brain delivery
Cassano, Roberta,Conese, Massimo,Di Gioia, Maria Luisa,Di Gioia, Sante,Mandracchia, Delia,Pellitteri, Rosalia,Trapani, Adriana,Tripodo, Giuseppe,Trombino, Sonia
, (2020)
This work aims to the synthesis of novel carboxylated chitosan-dopamine (DA) and -tyrosine (Tyr) conjugates as systems for improving the brain delivery of the neurotransmitter DA following nasal administration. For this purpose, ester or amide conjugates were synthesized by N,N-dicyclohexylcarbodiimide (DCC) mediated coupling reactions between the appropriate N-tert-butyloxycarbonyl (Boc) protected starting polymers N,O-carboxymethyl chitosan and 6-carboxy chitosan and DA or O-tert-Butyl-L-tyrosine-tert-butyl ester hydrochloride. The resulting conjugates were characterized by FT-IR and 1H- and 13C NMR spectroscopies and their in vitro mucoadhesive properties in simulated nasal fluid (SNF), toxicity and uptake from Olfactory Ensheathing Cells (OECs) were assessed. Results demonstrated that N,O-carboxymethyl chitosan-DA conjugate was the most mucoadhesive polymer in the series examined and, together with the 6-carboxy chitosan-DA-conjugate were able to release the neurotransmitter in SNF. The MTT assay showed that the starting polymers as well as all the prepared conjugates in OECs resulted not toxic at any concentration tested. Likewise, the three synthesized conjugates were not cytotoxic as well. Cytofluorimetric analysis revealed that the N,O-carboxymethyl chitosan DA conjugate was internalized by OECs in a superior manner at 24 h as compared with the starting polymer. Overall, the N,O-CMCS-DA conjugate seems promising for improving the delivery of DA by nose-to-brain administration.
Lithium Ion Recognition with Nanofluidic Diodes through Host-Guest Complexation in Confined Geometries
Ali, Mubarak,Ahmed, Ishtiaq,Ramirez, Patricio,Nasir, Saima,Mafe, Salvador,Niemeyer, Christof M.,Ensinger, Wolfgang
, p. 6820 - 6826 (2018)
The lithium ion recognition is receiving significant attention because of its application in pharmaceuticals, lubricants and, especially, in energy technology. We present a nanofluidic device for specific lithium ion recognition via host-guest complexatio
Easy access to drug building-blocks through benzylic C-H functionalization of phenolic ethers by photoredox catalysis
Brandhofer, Tobias,Derdau, Volker,García Manche?o, Olga,Méndez, María,P?verlein, Christoph,Stinglhamer, Martin
supporting information, p. 6756 - 6759 (2021/07/13)
A visible light-mediated photocatalyzed C-C-bond forming method for the benzylic C-H functionalization of phenolether containing synthetic building blocks based on a radical-cation/deprotonation strategy is reported. This method allows the mild, selective generation of benzyl radicals in phenolic complex molecules and drug-like compounds, providing new entries in synthetic and medicinal chemistry.
Fluorodesulfurization of Thionobenzodioxoles with Silver(I) Fluoride
Newton, Josiah J.,Brooke, Alan J.,Duhamel, Bastian,Pulfer, Jason M.,Britton, Robert,Friesen, Chadron M.
, p. 13298 - 13305 (2020/11/26)
Difluorobenzodioxole is an important functional group found in both pharmaceuticals and agrochemicals. The late-stage introduction of this functional group is challenged by typical fluorination conditions of HF and strong oxidants. Here, we demonstrate that a range of difluorobenzodioxoles can be prepared from catechols in two steps through conversion into thionobenzodioxoles, followed by desulfurative fluorination with silver(I) fluoride. These mild reaction conditions are compatible with a variety of functional groups and enable access to a range of functionalized difluorobenzodioxoles.
METHODS AND INTERMEDIATES FOR PREPARING DEUTETRABENAZINE
-
Page/Page column 40, (2019/07/17)
Disclosed is a process for the preparation of deutetrabenazine and intermediates useful in the preparation thereof. Disclosed are also process for making amorphous deutetrabenazine.
BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2
-
Paragraph 0216; 0217, (2018/07/05)
The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.
Bioinspired Syntheses of the Pyridoacridine Marine Alkaloids Demethyldeoxyamphimedine, Deoxyamphimedine, and Amphimedine
Khalil, Iman M.,Barker, David,Copp, Brent R.
, p. 282 - 289 (2016/01/15)
Efficient bioinspired syntheses of the biologically active pyridoacridine marine alkaloids demethyldeoxyamphimedine, deoxyamphimedine, and amphimedine are reported. Reaction of styelsamine D, prepared via an optimized route starting from Boc-dopamine, wit
DIMETHOXYPHENYL INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2
-
Paragraph 00175, (2016/09/15)
Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.
Hexagonal magnetite nanoprisms: Preparation, characterization and cellular uptake
Wang,Shrestha,Basel,Pyle,Toledo,Konecny,Thapa,Ikenberry,Hohn,Chikan,Troyer,Bossmann
supporting information, p. 4647 - 4653 (2015/06/16)
The capacity of iron oxide nanocrystals to heat tissue when subjected to an alternating magnetic field (AMF hyperthermia) is shape-selective. Although iron oxide nanostructures with numerous shapes have been synthesized to date, hexagonal Fe3O
BENZOQUINOLINE INHIBITORS OF VESICULAR MONOAMINE TRANSPORTER 2
-
Paragraph 00161, (2015/06/08)
The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof. (I)
