39560-34-4Relevant articles and documents
Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors
Zhang, Yong,Jung, Seo Yoon,Jin, Changbae,Kim, Nam Doo,Gong, Ping,Lee, Yong Sup
scheme or table, p. 502 - 507 (2011/02/28)
The involvement of μ-calpain in neurological disorders, such as stroke and Alzheimer's disease has attracted considerable interest in the use of calpain inhibitors as therapeutic agents. 4-Aryl-4-oxobutanoic acid amide derivatives 4 were designed as acyclic variants of μ-calpain inhibitory chromone and quinolinone derivatives. Of the compounds synthesized, 4c-2, which possesses a 2-methoxymethoxy group at the phenyl ring and a primary amide at the warhead region most potently inhibited μ-calpain (IC50 = 0.34 μM). Our findings suggest that the 4-aryl-4-oxobutanoic acid amide derivatives should be considered as a new family of μ-calpain inhibitors.
Photochemical Versus Aluminium Chloride-Catalyzed Fries Rearrangement of Aryl Hydrogen Succinates. Synthesis of 2(3H)-Furanones
Fillol, Luis,Martinez-Utrilla, Roberto,Miranda, Miguel A.,Morera, Isabel M.
, p. 863 - 870 (2007/10/02)
The photochemical and aluminium chloride-catalyzed Fries rearrangement of a series of aryl hydrogen succinates 3 a-f to the corresponding 4-oxoacids 1 a-f are compared.Both approaches are complementary: the photochemical process is more general and becomes the method of choice for the succinoylation of phenols supporting alkoxy or hydroxy substituents, while the classical rearrangement is superior in the presence of alkyl or halogen substituents.These results are applied to the preparation of the 2(3H)-furanones 2 a-f. - Keywords: Fries rearrangement; Photo-Fries rearrangement; Aryl hydrogen succinates; 4-Oxoacids; 2(3H)-Furanones.