5174-90-3Relevant articles and documents
Ferric Chloride-catalyzed Synthesis of 2-Oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate Derivatives and Their Biological Evaluation
Sakram,Madhu,Sonyanaik,Rambabu,Ravi,Kurumanna
, p. 1224 - 1227 (2018)
A new methodology has been developed for the synthesis of novel 2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylates from 2-aminonicotinaldehyde, Meldrum’s acid, and the corresponding alcohols in the presence of anhydrous iron(III) chloride as a cheap and readily available catalyst. The structure of the synthesized compounds was established by IR, 1H NMR, and mass spectral data and elemental analyses. All the synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity, and the activity of some derivatives was comparable with the activity of Ciprofloxacin and Nystatin used as reference drugs.
Development of [18f]lu14 for pet imaging of cannabinoid receptor type 2 in the brain
Teodoro, Rodrigo,Gündel, Daniel,Deuther-Conrad, Winnie,Ueberham, Lea,Toussaint, Magali,Bormans, Guy,Brust, Peter,Moldovan, Rare?-Petru
, (2021/08/04)
Cannabinoid receptors type 2 (CB2R) represent an attractive therapeutic target for neurodegenerative diseases and cancer. Aiming at the development of a positron emission tomography (PET) radiotracer to monitor receptor density and/or occupancy during a CB2R-tailored therapy, we herein describe the radiosynthesis of cis-[18F]1-(4-fluorobutyl-N-((1s,4s)-4-methylcyclohexyl)-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide ([18F]LU14) starting from the corresponding mesylate precursor. The first biological evaluation revealed that [18F]LU14 is a highly affine CB2R radioligand with >80% intact tracer in the brain at 30 min p.i. Its further evaluation by PET in a well-established rat model of CB2R overexpression demonstrated its ability to selectively image the CB2R in the brain and its potential as a tracer to further investigate disease-related changes in CB2R expression.
5-MEMBERED AND BICYCLIC HETEROCYCLIC AMIDES AS INHIBITORS OF ROCK
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Page/Page column 101, (2019/02/02)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.