24973-22-6Relevant articles and documents
Synthesis of Functionalized Indolines and Dihydrobenzofurans by Iron and Copper Catalyzed Aryl C-N and C-O Bond Formation
Henry, Martyn C.,Senn, Hans Martin,Sutherland, Andrew
, p. 346 - 364 (2019/01/08)
A simple and effective one-pot, two-step intramolecular aryl C-N and C-O bond forming process for the preparation of a wide range of benzo-fused heterocyclic scaffolds using iron and copper catalysis is described. Activated aryl rings were subjected to a highly regioselective, iron(III) triflimide-catalyzed iodination, followed by a copper(I)-catalyzed intramolecular N-or O-arylation step leading to indolines, dihydrobenzofurans, and six-membered analogues. The general applicability and functional group tolerance of this method were exemplified by the total synthesis of the neolignan natural product, (+)-obtusafuran. DFT calculations using Fukui functions were also performed, providing a molecular orbital rationale for the highly regioselective arene iodination process.
A novel anti-Alzheimer agent inhibiting oligomerization and fibriliation of beta-amyloid protects neuronal cell from Aβ-induced cytotoxicity
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Paragraph 0064; 0066, (2017/04/25)
The present invention relates to development of a novel treatment agent for Alzheimerandprime;s disease, having ability of protecting neural cells and inhibiting fibrosis and oligomerization of beta-amyloid. A compound of the present invention is capable of, while maintaining therapeutic effects on Alzheimerandprime;s disease, recovering ability of directly inhibiting oligomerized and fibrous amyloid beta, which is inherent activities of existing curcumin, thereby being useful as a novel inhibitor.COPYRIGHT KIPO 2017
Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: Further structure-activity relationships, in vivo studies, and preliminary toxicity profiling
Gemma, Sandra,Camodeca, Caterina,Sanna Coccone, Salvatore,Joshi, Bhupendra P.,Bernetti, Matteo,Moretti, Vittoria,Brogi, Simone,De Marcos, Maria Cruz Bonache,Savini, Luisa,Taramelli, Donatella,Basilico, Nicoletta,Parapini, Silvia,Rottmann, Matthias,Brun, Reto,Lamponi, Stefania,Caccia, Silvio,Guiso, Giovanna,Summers, Robert L.,Martin, Rowena E.,Saponara, Simona,Gorelli, Beatrice,Novellino, Ettore,Campiani, Giuseppe,Butini, Stefania
, p. 6948 - 6957 (2012/11/07)
Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development of a novel antimalarial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of clotrimazole-based antimalarials. Here we describe the optimization of this class of hybrid drug through in-depth structure-activity relationship studies. Antiplasmodial properties and mode of action were characterized in vitro and in vivo, and interactions with the parasites 'chloroquine resistance transporter' were investigated in a Xenopus laevis oocyte expression system. These tests indicated that piperazine derivatives 4b and 4d may be suitable for coadministration with chloroquine against chloroquine-resistant parasites. The potential for metabolism of the drugs by cytochrome P450 was determined in silico, and the lead compounds were tested for toxicity and mutagenicity. A preliminary pharmacokinetic analysis undertaken in mice indicated that compound 4b has an optimal half-life.
