Design, Synthesis, and Biological Evaluation of Pyridazinones Containing the (2-Fluorophenyl) Piperazine Moiety as Selective MAO-B Inhibitors

Twelve pyridazinones (T1-T12) containing the (2-fluorophenyl) piperazine moiety were designed, synthesized, and evaluated for monoamine oxidase (MAO) -A and -B inhibitory activities. T6 was found to be the most potent MAO-B inhibitor with an IC50 value of 0.013 µM, followed by T3 (IC50 = 0.039 µM). Inhibitory potency for MAO-B was more enhanced by meta bromo substitution (T6) than by para bromo substitution (T7). For para substitution, inhibitory potencies for MAO-B were as follows: -Cl (T3) > -N(CH3)2 (T12) > -OCH3 (T9) > Br (T7) > F (T5) > -CH3 (T11) > -H (T1). T6 and T3 efficiently inhibited MAO-A with IC50 values of 1.57 and 4.19 µM and had the highest selectivity indices (SIs) for MAO-B (120.8 and 107.4, respectively). T3 and T6 were found to be reversible and competitive inhibitors of MAO-B with Ki values of 0.014 and 0.0071, respectively. Moreover, T6 was less toxic to healthy fibroblast cells (L929) than T3. Molecular docking simulations with MAO binding sites returned higher docking scores for T6 and T3 with MAO-B than with MAO-A. These results suggest that T3 and T6 are selective, reversible, and competitive inhibitors of MAO-B and should be considered lead candidates for the treatment of neurodegenerative disorders like Alzheimer's disease

Correlates of loneliness among university students

Background The purpose of this study was to investigate level of loneliness, essential needs during university education, and relationships between loneliness, essential needs, and characteristics of university students. A sample comprising 721 students participated in the study. The mean age was 21.58 (SD = 1.73) with a range from 18 to 25. The majority of the students were female (70.6%) and were living in students' dormitory (67.5%) with low (87.8%) income, away from their parents. Methods The UCLA-R loneliness scale and sociodemographic questionnaire which includes an open-ended question on essential needs during university education were administered. Pearson-Product-Moment correlations were used to explore the relationships between participants' loneliness, needs, and characteristics. Results It was found that 60.2% of the participants experienced loneliness. Economical support (81.6%), social interaction (46.9%) and psychosocial support (35%) were the essential needs during university education reported by the participants. The study findings indicate that there were significant relationships between the needs of economical support, social interaction, and loneliness level of university students. Results also show that there were significant relationships among romantic relationship, parents' status and loneliness. Participants' loneliness levels were relatively higher who had not any romantic relationship and were not from married families. Conclusion The findings of this study provided essential information, about Turkish university students, concerning: level of loneliness and relationships that exist among loneliness, needs and sociodemographic characteristics. The findings also suggest implications for psychosocial practice. Because of the mean of loneliness were found to be high (45.49 ± 10.07), for this study, professionals need to pay attention to Turkish university students' psychosocial state, and need to empower them in establishing social relations

Effect of Rare Earth Ions on the Properties of Composites Composed of Ethylene Vinyl Acetate Copolymer and Layered Double Hydroxides

BACKGROUND: The study on the rare earth (RE)-doped layered double hydroxides (LDHs) has received considerable attention due to their potential applications in catalysts. However, the use of RE-doped LDHs as polymer halogen-free flame retardants was seldom investigated. Furthermore, the effect of rare earth elements on the hydrophobicity of LDHs materials and the compatibility of LDHs/polymer composite has seldom been reported. METHODOLOGY/PRINCIPAL FINDINGS: The stearate sodium surface modified Ni-containing LDHs and RE-doped Ni-containing LDHs were rapidly synthesized by a coprecipitation method coupled with the microwave hydrothermal treatment. The influences of trace amounts of rare earth ions La, Ce and Nd on the amount of water molecules, the crystallinity, the morphology, the hydrophobicity of modified Ni-containing LDHs and the adsorption of modifier in the surface of LDHs were investigated by TGA, XRD, TEM, contact angle and IR, respectively. Moreover, the effects of the rare earth ions on the interfacial compatibility, the flame retardancy and the mechanical properties of ethylene vinyl acetate copolymer (EVA)/LDHs composites were also explored in detail. CONCLUSIONS/SIGNIFICANCE: S-Ni₀.₁MgAl-La displayed more uniform dispersion and better interfacial compatibility in EVA matrix compared with other LDHs. Furthermore, the S-Ni₀.₁MgAl-La/EVA composite showed the best fire retardancy and mechanical properties in all composites