1160004-91-0Relevant academic research and scientific papers
Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain
Díaz, José Luis,Cuevas, Félix,Oliva, Ana I.,Font, Daniel,Sarmentero, M. ángeles,álvarez-Bercedo, Paula,López-Valbuena, José M.,Pericàs, Miquel A.,Enrech, Raquel,Montero, Ana,Yeste, Sandra,Vidal-Torres, Alba,álvarez, Inés,Pérez, Pilar,Cendán, Cruz Miguel,Cobos, Enrique J.,Vela, José Miguel,Almansa, Carmen
, p. 5157 - 5170 (2021/05/07)
The synthesis and pharmacological activity of a new series of 5a,7,8,8a-tetrahydro-4H,6H-pyrrolo[3,4-b][1,2,3]triazolo[1,5-d][1,4]oxazine derivatives as potent sigma-1 receptor (σ1R) ligands are reported. A lead optimization program aimed at improving the aqueous solubility of parent racemic nonpolar derivatives led to the identification of several σ1R antagonists with a good absorption, distribution, metabolism, and excretion in vitro profile, no off-target affinities, and characterized by a low basic pKa (around 5) that correlates with high exposure levels in rodents. Two compounds displaying a differential brain-to-plasma ratio distribution profile, 12lR and 12qS, exhibited a good analgesic profile and were selected as preclinical candidates for the treatment of pain.
Intramolecular azide-Alkyne for the fast assembly of structurally diverse, tricyclic 1,2,3-triazoles
Oliva, Ana I.,Christmann, Ute,Font, Daniel,Cuevas, Flix,Ballester, Pablo,Buschmann, Helmut,Torrens, Antoni,Yenes, Susana,Perics, Miquel A.
supporting information; experimental part, p. 1617 - 1619 (2009/04/07)
The synthesis of novel tricyclic 1,2,3-triazoles starting from cyclic epoxides via the sequential azidolysis, propargylation and 1,3-dipolar cycloaddition is described. Derivatization by N-arylation reaction and the synthesis of enantiomerically pure comp
