Tricyclic Triazoles as σ Receptor Antagonists for Treating Pain.
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2021
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Abstract
The synthesis and pharmacological activity of a new series of 5a,7,8,8a-tetrahydro-4,6-pyrrolo[3,4-][1,2,3]triazolo[1,5-][1,4]oxazine derivatives as potent sigma-1 receptor (σR) ligands are reported. A lead optimization program aimed at improving the aqueous solubility of parent racemic nonpolar derivatives led to the identification of several σR antagonists with a good absorption, distribution, metabolism, and excretion in vitro profile, no off-target affinities, and characterized by a low basic p (around 5) that correlates with high exposure levels in rodents. Two compounds displaying a differential brain-to-plasma ratio distribution profile, and , exhibited a good analgesic profile and were selected as preclinical candidates for the treatment of pain.
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daz2021tricyclicjournal
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| Authors | 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; |
| Journal | Journal of medicinal chemistry |
| Year | 2021 |
| DOI |
10.1021/acs.jmedchem.1c00244
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