89465-97-4Relevant articles and documents
Discovery of 5-HT6 receptor ligands based on virtual HTS
Tasler, Stefan,Kraus, Jürgen,Wuzik, Andreas,Müller, Oliver,Aschenbrenner, Andrea,Cubero, Elena,Pascual, Rosalia,Quintana-Ruiz, Jordi-Ramon,Dordal, Alberto,Mercè, Ramon,Codony, Xavier
, p. 6224 - 6229 (2008/03/18)
Based on a pharmacophore alignment on a 5-HT6 ligand applying 4SCan technology, a new lead series was identified and further structurally investigated. Kis down to 8 nM were achieved.
Applicability aspects of transition metal-catalyzed aromatic amination protocols in medicinal chemistry
Tasler, Stefan,Mies, Jan,Lang, Martin
, p. 2286 - 2300 (2008/09/19)
The application of palladium- and coppercatalyzed reactions for the aromatic amination of pharmacologically relevant scaffolds is investigated. The focus is set on the scope of several protocols for the introduction of amines of broad structural diversity, allowing for the synthesis of numerous derivatives of one biological hit structure for screening in biological assay systems. Thus, attaining optimized yields and TONs had not a major priority, most important were practical aspects, that is no further purification and drying of reagents and solvents had to be envisaged, ideally only a few transition metalbased protocols had to be applied for synthesizing structurally diverse compounds in sufficient amounts (several milligrams) for screening without any finetuning of conditions and catalytic systems.
Novel cinnamic amides
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Page/Page column 9, (2008/06/13)
E-cinnamic amides of piperazine derivatives according to formula (I) wherein X is chloro or fluoro and R1 is an aromatic or heteroaromatic group, their pharmaceutically acceptable salts or solvates. The invention also relates to pharmaceutical
Novel bisamidate phosphonate prodrugs
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, (2008/06/13)
Novel bisamidate phosphonate prodrugs of FBPase inhibitors of the Formula IA: and their use in the treatment of diabetes and other conditions associated with elevated blood glucose.