521949-80-4Relevant articles and documents
A way to manage the thermal flexibility of ligand candidates for bioassays
Altamura, Maria,Balacco, Giuseppe,Cuda, Francesco,Guerri, Annalisa,Guidi, Antonio,Meini, Stefania,Menichetti, Stefano,Nativi, Cristina,Pasqui, Franco
, p. 6754 - 6761 (2006)
An original way to manage both stereochemistry and conformational constraints in ligand candidates for bioassays is presented with reference to a group of model N,N′-tetrasubstituted o-phthalamides and thioamides. The study shows that a scale of thermal flexibility in solution can be envisaged, the divisions of which are represented by compounds sharing quite similar geometrical features. NMR spectroscopy and powder X-ray analysis were used for the physical chemical investigation. An attempt to exploit the conformational instability of a model thioamide in the medium of a bioassay was also performed.