1059705-55-3Relevant academic research and scientific papers
Rational design of 5-HT6R ligands using a bioisosteric strategy: Synthesis, biological evaluation and molecular modelling
Staroń, Jakub,Warszycki, Dawid,Kalinowska-T?us?cik, Justyna,Sata?a, Grzegorz,Bojarski, Andrzej J.
, p. 25806 - 25815 (2015/10/20)
A bioisosteric strategy was successfully implemented with a screening protocol for new, potent 5-HT6R ligands. Initially, 2-[5-(4-methylpiperazin-1-yl)-2-nitrophenyl]-1,2,3,4-tetrahydroisoquinoline (9) was found in commercial databases using a
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.
SUBSTITUTED PHENYL-PIPERAZINE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS
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Page/Page column 106-107, (2008/06/13)
The present invention relates to substituted phenyl-piperazine compounds of general formula (I), a process for their preparation, medicaments comprising said substituted phenyl-piperazine compounds as well as the use of said substituted phenyl-piperazine compounds for the preparation of medicaments, which are particularly suitable for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.
