Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid
N-Aryl derivatives of edaravone were identified as potentially effective small molecule inhibitors of tau and beta-amyloid aggregation in the context of developing disease-modifying therapeutics for Alzheimer's disease (AD). Palladium-catalyzed hydrazine monoarylation protocols were then employed as an expedient means of preparing a focused library of 21 edaravone derivatives featuring varied N-aryl substitution, thereby enabling structure-activity relationship (SAR) studies. On the basis of data obtained from two functional biochemical assays examining the effect of edaravone derivatives on both fibril and oligomer formation, it was determined that derivatives featuring an N-biaryl motif were four-fold more potent than edaravone.
Maclean, Mark A.,Diez-Cecilia, Elena,Lavery, Christopher B.,Reed, Mark A.,Wang, Yanfei,Weaver, Donald F.,Stradiotto, Mark
supporting information
p. 100 - 104
(2015/12/18)
A convenient preparation of 8-ethyl-4,9-dihydro-3H-pyrano[3,4-b]indole-1-one, key intermediate of the antiinflammatory agent Etodolac
A facile synthesis of 8-ethyl-4,9-dihydro-3H-pyrano[3,4-b]indole-1-one 5 is described which features the condensation of hydrazines with 2-oxo-5-hydroxypentanoic acid, followed by Fischer cyclization of these adducts.
Gonzalez
p. 669 - 674
(2007/10/02)
Carbazole acetic acid derivatives
Tetrahydrocyclopent[b]indole-3-acetic acid, tetrahydrocarbazole-1-acetic acid and hexahydrocyclohept[b]-indole-6-acetic acid derivatives in which the carbon bearing alkyl, lower alkenyl or lower cycloalkyl are disclosed. The compounds are useful antiinflammatory agents and methods for their preparation and use are described.
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(2008/06/13)
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