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Geometrically Constrained Derivatives of Indolylglyoxylamides as Ligands Binding the GABAA/BzR Complex

[ Vol. 12 , Issue. 4 ]


S. Sartini, M. Morelli, F. Simorini, S. Taliani, S. Salerno, A. M. Marini, F. Da Settimo and C. La Motta   Pages 312 - 320 ( 9 )


Indolylglyoxylamides are a class of distinctive benzodiazepine receptor ligands, proposed in the mid-eighties as open analogues of -carbolines. Thorough and long-lasting studies of their structure-activity relationships led to the development of a great deal of derivatives, to satisfy increasingly structural and pharmacophoric requirements of the benzodiazepine binding site in the central nervous system. Efforts to pre-organize their flexible structure in the threedimensional shape adopted when bound to the receptor led to the identification of two novel classes of rigid ligands, characterized by planar tricyclic heteroaromatic cores: the [1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one and the [1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1,5(6H)-dione. The present review focuses on these selected classes of ligands, whose rational development, in terms of chemical structures and structure-activity relationships, will be fully discussed.


[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones, [1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1,5(6H)-diones, BzR ligands, ndolylglyoxylamides, structure-activity relationships, binding site, rigid ligands, heteroaromatic cores, anxiety-related emotional disorders, ligands


Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126, Pisa, Italy.

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