Stereoselective Synthesis and Antiallodynic Activity of 3-Hydroxylated Paroxetines.

Stereoselective Synthesis and Antiallodynic Activity of 3-Hydroxylated Paroxetines.
ChemMedChem. 2020 Oct 19;:
Authors: Sartillo-Piscil F, Chamorro-Arenas D, Salgado-Moreno G, Martinez-Mendieta L, Godínez-Chaparro B, Quintero L
Abstract
The design, stereoselective synthesis and in vivo antiallodynic activity of four novel paroxetine analogs, named 3-hydroxy paroxetines (3HPXs), is reported.  Among the novel synthesized compounds, three of them showed antiallodynic effect, while the ( R , R )-3HPX resulted to be 2.5 times more bioactive than (-)-paroxetine itself in neuropathic rats. Consequently, the current investigation not only discloses a novel promising analgesic drug , but also reveals that functionalization at the C-3 position of paroxetine could be as effective as the common functionalization at either C-4 or within the sesamol group.
PMID: 33078572 [PubMed - as supplied by publisher]

Source: ChemMedChem - October 19, 2020 Category: Chemistry Authors: Sartillo-Piscil F, Chamorro-Arenas D, Salgado-Moreno G, Martinez-Mendieta L, Godínez-Chaparro B, Quintero L Tags: ChemMedChem Source Type: research