Tricyclic Triazoles as σ Receptor Antagonists for Treating Pain.

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ID: 275496
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.
Reference Key
daz2021tricyclicjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
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
URL
Keywords
Antimicrobial endophytes cytotoxic fusarium oxysporum vicia faba

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