100202-78-6Relevant articles and documents
In vitro and in vivo evaluation of fluorinated indanone derivatives as potential positron emission tomography agents for the imaging of monoamine oxidase B in the brain
Duki?-Stefanovi?, Sladjana,Hang Lai, Thu,Toussaint, Magali,Clau?, Oliver,Jevti?, Ivana I.,Penji?evi?, Jelena Z.,Andri?, Deana,Ludwig, Friedrich-Alexander,Gündel, Daniel,Deuther-Conrad, Winnie,Kosti?-Raja?i?, Sladjana V.,Brust, Peter,Teodoro, Rodrigo
, (2021)
Monoamine oxidases (MAOs) play a key role in the metabolism of major monoamine neurotransmitters. In particular, the upregulation of MAO-B in Parkinson's disease, Alzheimer's disease and cancer augmented the development of selective MAO-B inhibitors for d
Targeting cyclic nucleotide phosphodiesterase 5 (PDE5) in brain: Toward the development of a PET radioligand labeled with fluorine-18
Wenzel, Barbara,Liu, Jianrong,Dukic-Stefanovic, Sladjana,Deuther-Conrad, Winnie,Teodoro, Rodrigo,Ludwig, Friedrich-Alexander,Chezal, Jean-Michel,Moreau, Emmanuel,Brust, Peter,Maisonial-Besset, Aurelie
, p. 346 - 362 (2019)
With the aim to develop a specific radioligand for imaging the cyclic nucleotide phosphodiesterase 5 (PDE5) in brain by positron emission tomography (PET), seven new fluorinated inhibitors (3–9) were synthesized on the basis of a quinoline core. The inhibitory activity for PDE5 together with a panel of other PDEs was determined in vitro and two derivatives were selected for IC50 value determination. The most promising compound 7 (IC50 = 5.92 nM for PDE5A), containing a 3-fluoroazetidine moiety, was further radiolabeled by aliphatic nucleophilic substitution of two different leaving groups (nosylate and tosylate) using [18F]fluoride. The use of the nosylate precursor and tetra-n-butyl ammonium [18F]fluoride ([18F]TBAF) in 3-methyl-3-pentanol combined with the addition of a small amount of water proved to be the best radiolabeling conditions achieving a RCY of 4.9 ± 1.5% in an automated procedure. Preliminary biological investigations in vitro and in vivo were performed to characterize this new PDE5 radioligand. Metabolism studies of [18F]7 in mice revealed a fast metabolic degradation with the formation of radiometabolites which have been detected in the brain.
Cap-dependent protease inhibitor
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Paragraph 0059-0062, (2021/06/09)
The invention relates to a compound with cap-dependent endonuclease inhibitory activity and application of the compound in the aspect of influenza treatment.