6196-83-4Relevant articles and documents
Electrophotochemical Ring-Opening Bromination oftert-Cycloalkanols
Yamamoto, Kosuke,Toguchi, Hiroyuki,Kuriyama, Masami,Watanabe, Shin,Iwasaki, Fumiaki,Onomura, Osamu
, p. 16177 - 16186 (2021/09/13)
An electrophotochemical ring-opening bromination of unstrainedtert-cycloalkanols has been developed. This electrophotochemical method enables the oxidative transformation of cycloalkanols with 5- to 7-membered rings into synthetically useful ω-bromoketones without the use of chemical oxidants or transition-metal catalysts. Alkoxy radical species would be key intermediates in the present transformation, which generate through homolysis of the O-Br bond in hypobromite intermediates under visible light irradiation.
Syntheses and In-Vitro evaluation of novel adamantane based γ-secretase inhibitors
Adeniji,Wells,Adejare
experimental part, p. 2458 - 2471 (2012/08/13)
Abnormal processing of amyloid precursor protein (APP) by β - and γ -secretases to produce excess amyloid-β-peptide is believed to contribute to the pathophysiological cascade that results in Alzheimer's disease. γ -Secretase inhibition or modulation ther
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein
Macdonald, Dwight,Brideau, Christine,Chan, Chi Chung,Falgueyret, Jean-Pierre,Frenette, Richard,Guay, Jocelyne,Hutchinson, John H.,Perrier, Helene,Prasit, Peptiboon,Riendeau, Denis,Tagari, Philip,Therien, Michel,Young, Robert N.,Girard, Yves
, p. 2023 - 2027 (2008/12/23)
The discovery and SAR of a novel series of substituted 2,2-bisaryl-bicycloheptane inhibitors of 5-lipoxygenase activating protein (FLAP) are herein described. SAR studies have shown that 2,5-substitution on the exo-aryl group is optimal for potency. The most potent compounds in this series have an ortho-nitrogen aryl linked with a methyleneoxy as the 5-substituent and a polar group such as a urethane as the 2-substituent. One of the most potent compounds identified is the 5-benzothiazolymethoxy-2-pyridinylcarbamate derivative 2 (FLAP IC50 = 2.8 nM) which blocks 89% of ragweed induced urinary LTE4 production in dogs (at an I.V. dose of 2.5 μg/kg/min). This compound inhibits calcium ionophore stimulated LTB4 production in both human polymorphonuclear (PMN) leukocytes and human whole blood (IC50 = 2.0 and 33 nM, respectively).
