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,N0-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
A Way to Manage the Thermal Flexibility of Ligand Candidates for Bioassays / M. Altamura; G. Balacco; F. Cuda; A. Guidi; S. Meini; S. Menichetti; C. Nativi; F. Pasqui. - In: TETRAHEDRON. - ISSN 0040-4020. - STAMPA. - 62:(2006), pp. 6754-6761. [10.1016/j.tet.2006.05.011]
A Way to Manage the Thermal Flexibility of Ligand Candidates for Bioassays
MENICHETTI, STEFANO;NATIVI, CRISTINA;
2006
Abstract
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,N0-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 performedFile | Dimensione | Formato | |
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