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405-05-0

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Inhibition of Acyl-CoA: Cholesterol acyltransferase (ACAT), overexpression of cholesterol transporter gene, and protection of amyloid β (Aβ) oligomers-induced neuronal cell death by tricyclic pyrone molecules
A major effort in Alzheimers disease therapeutic development has targeted Aβ and downstream events. We have synthesized a small library of tricyclic pyrone compounds. Their protective action in MC65 cells and inhibition of ACAT along with the upregulation of cholesterol transporter gene were investigated. Five active compounds exhibited potencies in the nanomolar ranges. The multiple effects of the compounds on Aβ and cellular cholesterol pathways could be potential mechanisms underlying the protective effects in vivo.
Pokhrel, Laxman,Maezawa, Izumi,Nguyen, Thi D. T.,Chang, Kyeong-Ok,Jin, Lee-Way,Hua, Duy H.
p. 8969 - 8973
(2013/01/15)

Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives
Boropinic acid is a natural isopentenyloxycinnamic acid extracted from the aerial parts of Boronia pinnata Sm. (Rutaceae) with soybean 5-lipoxygenase inhibitory activity. In this paper the topical anti-inflammatory activity of boropinic acid and some of its natural and semi-synthetic derivatives was evaluated using the Croton oil ear test in mice as a model of acute inflammation. Some of the tested compounds (15, 17, 19, 20) revealed an effect comparable (ID50 = 0.18 ÷ 0.72 μmol/cm2) to that of the reference drug indomethacin (ID50 = 0.23 μmol/cm 2), a non-steroidal anti-inflammatory drug.
Epifano, Francesco,Sosa, Silvio,Tubaro, Aurelia,Marcotullio, M. Carla,Curini, Massimo,Genovese, Salvatore
supporting information; experimental part
p. 769 - 772
(2011/03/18)

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Chemical Properties

Melting Point: 121-124 °C
Boiling Point: 225.6 °C at 760 mmHg
Flash Point:90.2 °C
Density: 1.35 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
PKA: 6.52±0.18(Predicted)
Sensitive: Air Sensitive
BRN: 3234259
PSA: 37.30000
LogP: 1.34380

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