A Simple Efficient Synthesis of 5,8-Isoquinolinedione

Anderson, Wayne K.; Connarty, Bernard P.; El‐Hajj, T.

doi:10.1080/00397918608056409

Cited by 6 publications

(3 citation statements)

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“…Isoquinoline-5,8-dione was synthesized by following the literature procedure. 37,38 The synthetic procedure for YQ-025 was adapted from the literature procedure. 39,40 To a stirred mixture of 6,7-dichloroisoquinoline-5,8-dione (20 mg, 0.088 mmol, 1 equiv) and CeCl 3 •7H 2 O (1.63 mg, 0.05 equiv) in EtOH (1.2 mL) was added aniline (12 μL, 1.5 equiv) at rt.…”

Section: ■ Methodsmentioning

confidence: 99%

“…The following compounds ( YQ-003 , YQ-004 , YQ-005 , YQ-006 , YQ-007 , YQ-008 , YQ-009 , YQ-010 , YQ-011 , YQ-012 , YQ-013 , YQ-014 , YQ-015 , YQ-016 , YQ-017 , YQ-018 , YQ-019 , YQ-020 , YQ-021 , YQ-022, YQ-023 , YQ-024 , YQ-032 , YQ-033 , YQ-034 , and YQ-035 ) were prepared by the same procedure used for the synthesis of YQ-001 and 002 . Isoquinoline-5,8-dione was synthesized by following the literature procedure. , …”

Section: Methodsmentioning

confidence: 99%

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Fluorescent 1,4-Naphthoquinones To Visualize Diffuse and Dense-Core Amyloid Plaques in APP/PS1 Transgenic Mouse Brains

Shin

Jeon

Jung

et al. 2019

ACS Chem. Neurosci.

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Recent clinical approvals of brain imaging radiotracers targeting amyloid-β provided clinicians the tools to detect and confirm Alzheimer's disease pathology without autopsy or biopsy. While current imaging agents are effective in postsymptomatic Alzheimer's patients, there is much room for improvement in earlier diagnosis, hence prompting a need for new and improved amyloid imaging agents. Here we synthesized 41 novel 1,4naphthoquinone derivatives and initially discovered 14 antiamyloidogenic compounds via in vitro amyloid-β aggregation assay; however, qualitative analyses of these compounds produced conflicting results and required further investigation. Follow-up docking and biophysical studies revealed that four of these compounds penetrate the blood-brain barrier, directly bind to amyloid-β aggregates, and enhance fluorescence properties upon interaction. These compounds specifically stain both diffuse and dense-core amyloid-β plaques in brain sections of APP/PS1 double transgenic Alzheimer's mouse models. Our findings suggest 1,4-naphthoquinones as a new scaffold for amyloid-β imaging agents for early stage Alzheimer's.

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Section: ■ Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

Fluorescent 1,4-Naphthoquinones To Visualize Diffuse and Dense-Core Amyloid Plaques in APP/PS1 Transgenic Mouse Brains

Shin

Jeon

Jung

et al. 2019

ACS Chem. Neurosci.

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“…(35) herstellten. [14] Dabei nitrosierten sie zunächst in para-Position mit Natriumnitrit in konzentrierter Salzsäure, reduzierten dann die Nitrofunktion mit Natriumdithionit zum Amin und oxidierten anschließend durch Eisen(III)chlorid zum Zielprodukt mit einer Gesamtausbeute von 13% über 3 Stufen (Schema 5). ).…”

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Totalsynthese der Mansouramycine A-E aus Streptomyces sp. und Rhodium-katalysierte 1,2-Additionen an cyclische Enone

Johannes¹

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IC 50 -Werte in μg/mL gegen IC-2 WT -Zellinie von Mäusen. Antiproliverative in vitro Tests an der aus Mäusen stammenden Zellinie IC-2 WT ergaben IC 50 -Werte zwischen 0.03 und 1.67 μg/mL. Kürzlich von Brison et al. veröffentlichte mechanistische Studien hierzu konnten zeigen, dass sowohl eine selektive Inhibition, als auch der Abbau von Cdc25-Proteinphosphatasen stattfinden, welche mitverantwortlich für den

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