Trichomonas vaginalis is the etiologic agent of trichomoniasis, a worldwide distributed sexually transmitted infection (STI) that affects the genitourinary tract. Even though this disease already has a treatment in the prescription of drugs of the 5-nitroimidazole class, described low treatments adhesion, adverse side effects and cases of resistant isolates demonstrate the need for new formulations. With this in mind, chalcones emerge as a potential alternative to be tested, being compounds widely distributed in nature, easy to chemically synthesize and presenting several biological activities already reported.
View Article and Find Full Text PDFTrichomoniasis is a great public health burden worldwide and the increase in treatment failures has led to a need for finding alternative molecules to treat this disease. In this study, we present in vitro and in silico analyses of two 2,8-bis(trifluoromethyl) quinolines (QDA-1 and QDA-2) against Trichomonas vaginalis. For in vitro trichomonacidal activity, up to seven different concentrations of these drugs were tested.
View Article and Find Full Text PDFThe 3-[(4-methoxyphenyl)selanyl]-2-phenylimidazo[1,2-a] pyridine (MPI), a novel organic selenium compound, has been receiving increased attention due to its antioxidant effects and its ability to protect against depression-like behaviours. However, it remains elusive whether MPI is able to reverse depressive-like symptoms and biochemical alterations in mice. In the present work, we explored the ability of MPI (10 mg/kg, i.
View Article and Find Full Text PDFCompr Psychoneuroendocrinol
May 2021
Despite the severity and the high prevalence of depression and anxiety and the efforts that have been done to improve their treatment, the available pharmacotherapy still has several limitations. Therefore, the investigation of novel agents and the characterization of the molecular signaling pathways underlying their effects are needed. The organoselenium compound 3-[(4-chlorophenyl)selanyl]-1-methyl-1-indole (CMI) has emerged as a promising antidepressant and anxiolytic molecule in several animal models of depression through the modulation of neuroinflammation and oxidative stress.
View Article and Find Full Text PDFPyrazoles represent a significant class of heterocyclic compounds that exhibit pharmacological properties. The present study aimed to investigate the antioxidant potential of pyrazol derivative compounds in brain of mice in vitro and the effect of pyrazol derivative compounds in the oxidative damage and toxicity parameters in mouse brain and plasma of mice. The compounds tested were 3,5-dimethyl-1-phenyl-4-(phenylselanyl)-1-pyrazol (), 3,5-dimethyl-4-(phenylselanyl)-1-pyrazole (), 4-((4-methoxyphenyl)selanyl)-3,5-dimethyl-1-phenyl-1-pyrazole (), 4-((4-chlorophenyl)selanyl)-3,5-dimethyl-1-phenyl-1-pyrazole (), 3,5-dimethyl-1-phenyl-4-(phenylthio)-1-pyrazole (), 3,5-dimethyl-4-(phenylthio)-1-pyrazole (), 4-((4-methoxyphenyl)thio)-3,5-dimethyl-1-phenyl-1-pyrazole (), 4-((4-chlorophenyl)thio)-3,5-dimethyl-1-phenyl-1-pyrazole (), and 3,5-dimethyl-1-phenyl-1-pyrazole ().
View Article and Find Full Text PDFJ Psychiatr Res
August 2019
Major depression and anxiety are highly incapacitating psychiatric disorders often present simultaneously, and the causal relationship between these disorders and inflammation are under extensive investigation. The treatment for this comorbidity still relies on drugs acting on the serotonergic neurotransmission, but the modulation of immune-inflammatory pathways has attained an increasing interest in the drug discovery. We have previously demonstrated that the selenoorganic compound 3-[(4-chlorophenyl)selanyl]-1-methyl-1H-indole (CMI) possess antioxidant, anti-inflammatory, antinociceptive and antidepressant-like effect in mice.
View Article and Find Full Text PDFIn the last decades, selenium-containing compounds have received increasing attention due to their various biological and pharmacological properties. In the present study, we investigated the effects of 3-[(4-methoxyphenyl) selanyl]-2-phenylimidazo[1,2-a] pyridine (MPI; 1, 10 or 50 mg/kg, i.g.
View Article and Find Full Text PDFNeuropharmacology
March 2019
The lipopolysaccharide (LPS) is an endotoxin derived from gram-negative bacteria, which induces inflammation. The aims of this study were to evaluate the possible α-(phenylselanyl) acetophenone (PSAP) activity in reducing comorbid hyperalgesia, depressive-like and anxiogenic-like symptoms induced by LPS in mice. In additional, investigated physical chemical properties of PSAP through in silico analysis by ADMET predictor software.
View Article and Find Full Text PDFα-(phenylselanyl) acetophenone (PSAP) is an organoselenium compound that presents antidepressive-like and antinociceptive effect in animal models. In this study, we evaluate the potential pharmacological effects of PSAP on acute stress restriction (ARS)-induced depressive and anxiogenic-like behavior associated with hyperalgesia and mechanical allodynia in male adult Swiss mice (25-35 g). The ARS is an unavoidable stress situation that was applied for a period of 4 h using an individual rodent restraint.
View Article and Find Full Text PDFChronic pain and depressive disorders have been estimated to co-occur in up to 80% of patients and traditional antidepressants and analgesics have shown limited clinical efficacy. α- (phenylselanyl) acetophenone (PSAP) is an organic selenium compound which has already demonstrated antioxidant, antidepressant and antinociceptive activities in animal models, without showing acute toxicity. In view of develop more effective treatments to comorbid pain and depression, the purpose of this study was to evaluate the behavioral and biochemical effects of PSAP on reserpine induced pain-depression dyad model in mice as well to analyze the interaction of PSAP with specific targets by molecular docking analysis.
View Article and Find Full Text PDFBackground: Pain is one of the most prevalent, costly and disabling conditions that reduces quality of life. Although there are many analgesics available, there is some concern regarding their efficacy, safety and side effects. Organic selenium compounds are attractive targets of various research groups due to their pharmacological properties.
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