Stereoselective Synthesis and Antiallodynic Activity of 3-Hydroxylated Paroxetines |
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| Authors: | Delfino Chamorro-Arenas Giovanna Salgado-Moreno Dr Liliana Martinez-Mendieta Dr Leticia Quintero Dr Beatriz Godínez-Chaparro Prof Fernando Sartillo-Piscil |
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| Affiliation: | 1. Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla, 14 Sur Esq. San Claudio, Col. San Manuel S/N, 72570 Puebla, Mexico;2. Sistemas Biológicos, División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana-Xochimilco, Calzada de Hueso 1100, Col. Villa Quietud, 04960 Ciudad de México, Mexico |
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| Abstract: | The design, stereoselective synthesis and in vivo antiallodynic activity of four novel paroxetine analogs, named 3-hydroxy paroxetines (3HPXs), is reported herein. Among the novel synthesized compounds, three showed an antiallodynic effect, while (R,R)-3HPX was found 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 C3 position of paroxetine could be as effective as the common functionalization at either C4 or within the sesamol group. |
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| Keywords: | allodynia neuropathic pain paroxetine stereoselective synthesis alkaloids |
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