Stereoselective Synthesis and Antiallodynic Activity of 3‐Hydroxylated Paroxetines
| Autor: | Giovanna Salgado-Moreno, Fernando Sartillo-Piscil, Beatriz Godínez-Chaparro, Delfino Chamorro-Arenas, Leticia Quintero, Liliana Martinez-Mendieta |
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| Rok vydání: | 2020 |
| Předmět: |
Stereochemistry
Analgesic Pain Hydroxylation Biochemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery medicine Animals Rats Wistar General Pharmacology Toxicology and Pharmaceutics Sesamol Pharmacology Analgesics Dose-Response Relationship Drug Molecular Structure Organic Chemistry Stereoisomerism Paroxetine Rats Disease Models Animal chemistry Molecular Medicine Female Stereoselectivity medicine.drug |
| Zdroj: | ChemMedChem. 16:472-476 |
| ISSN: | 1860-7187 1860-7179 |
| DOI: | 10.1002/cmdc.202000674 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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