1373829-81-2Relevant articles and documents
PIPECOLATE-SULFONAMIDES FOR TREATMENT OF PSYCHIATRIC DISORDERS
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Page/Page column 36-37; 39; 60, (2013/07/19)
The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable
Exploration of pipecolate sulfonamides as binders of the FK506-binding proteins 51 and 52
Gopalakrishnan, Ranganath,Kozany, Christian,Wang, Yansong,Schneider, Sabine,Hoogeland, Bastiaan,Bracher, Andreas,Hausch, Felix
experimental part, p. 4123 - 4131 (2012/06/30)
FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders. Rapamycin and FK506 are two macrocyclic natural products, which tightly bind to most FKBP family members, including FKBP51 and FKBP52. A bioisosteric replacement of the α-ketoamide moiety of rapamycin and FK506 with a sulfonamide was envisaged with the retention of the conserved hydrogen bonds. A focused solid support-based synthesis protocol was developed, which led to ligands with submicromolar affinity for FKBP51 and FKBP52. The molecular binding mode for one sulfonamide analogue was confirmed by X-ray crystallography.