104777-73-3Relevant articles and documents
Bioactive prenylated phenyl derivatives derived from marine natural products: Novel scaffolds for the design of BACE inhibitors
López-Ogalla, Javier,García-Palomero, Esther,Sánchez-Quesada, Jorge,Rubio, Laura,Delgado, Elena,García, Pablo,Medina, Miguel,Castro, Ana,Mu?oz, Pilar
, p. 474 - 488 (2014/04/17)
Abnormal accumulation of neurotoxic beta-amyloid peptides (Aβ) is a key factor in the development of Alzheimer's disease (AD) and strategies to reduce Aβ production constitute an active field of research for the development of novel therapeutic agents for the treatment of AD. In particular, β-secretase-1 (BACE-1) has been a prime target for modulating Aβ production although obtaining drug-like BACE-1 inhibitors has proven to be highly challenging. Here we report the isolation and biochemical characterization of a marine natural product, the prenylated hydroxybenzoic acid 1, with BACE-1 inhibitory activity and ability to decrease Aβ production in cell-based assays. Synthesis and biological activity of a number of new synthetic analogues are also reported, as well as initial structure-activity relationship (SAR) analysis on this chemical family. Hence, these compounds constitute novel scaffolds from which more potent and selective BACE-1 inhibitors could be designed as potential therapeutic agents for the treatment of Alzheimer's disease.
PHENYL-PRENYL DERIVATIVES, OF MARINE AND SYNTHETIC ORIGIN, FOR THE TREATMENT OF COGNITIVE, NEURODEGENERATIVE OR NEURONAL DISEASES OR DISORDERS
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Page/Page column 37, (2009/10/09)
The present invention is related to a family of phenyl-prenyl derivatives of formula (I), and to their use in the treatment of cognitive, neurodegenerative or neuronal diseases or disorders, such as Alzheimer's disease or Parkinson's Disease. The present
The biosynthesis of ubiquinone: Synthesis and enzymatic modification of biosynthetic precursors
Shepherd, Jennifer A.,Poon, Wayne W.,Myles, David C.,Clarke, Catherine F.
, p. 2395 - 2398 (2007/10/03)
The synthesis of key intermediates in the eukaryotic biosynthetic pathway of ubiquinone (Q) and the biotransformation of these materials with yeast (S.cerevisiae) mitochondria are described. The synthesis of Q aromatic precursors 2, 3, and 4 (n = 3 in all cases) relies on the palladium (0) catalyzed coupling of farnesyl tributylstannane with suitably functionalized aryl halides. Preliminary experiments show that incubation of synthetic substrate 3 with mitochondria from yeast containing the 3,4-dihydroxy-5-hexaprenylbenzoate methyltransferase gene (COQ3) and S-[methyl-3H]adenosyl-L-methionine yields radiolabeled 4.