Design, Synthesis, Antimicrobial and Antioxidant Activities of Novel Threonine-based Sulfonamide Derivatives

Aim:To systematically design, synthesize and evaluate the biological activities of new threonine-based sulfonamide derivatives in order to achieve improved drug potency.Methodology: Sulfamoyl carboxylic acidswere prepared by the reaction of threonine with the appropriate sulfonyl chloride while their acetylated, carboxamide and aniline derivatives were synthesized via Lumiere-Barbier acetylation, Schotten-Baumann ammonolysis and Buchwald-Hartwig cross-coupling methods respectively. The FTIR, 1H-NMR, 13C-NMR and elemental analytical data were employed in the structural characterization. In vitro andin silico antioxidant and antimicrobial studies were carried out.Results:Compounds 1b and 1d displayed thebest in vitro antibacterial activities againstEscherichia coli, Salmonella typhi, Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and antifungal activities against Candida albicansandAspergillus niger. Compound 1f (IC50= 1.150±0.003μg/ml) exhibited the best in vitro antioxidant activity. Compound 1a had a higherin silicoantibacterial (-11.51 kcal/mol) binding energies than antibacterial reference drug, penicillin (-10.89 kcal/mol). Compound 1c had the highest in silicoantifungal binding energy (-10.48kcal/mol)comparable to ketoconazole(-10.85 kcal/mol). Conclusion: All the compounds were found to be potential antioxidant and antimicrobial drug candidates having complied with Lipinski’s rule of five.

Aggressive behaviour in children and adolescents. Part I: A review of the effects of child and family characteristics

Interpersonal violence is a major public health concern throughout the West Indies, particularly in Jamaica. Many factors contribute to a youth's violent or aggressive behaviour, ranging from individual temperament, to family structure, to large sociocultural influences. In Part I, we review the incidence and severity of violence, and discuss the effects of individual characteristics, and of family structure and discipline. In Part II, the reported effects of school structure, peer relationships and interaction, corporal punishment and the media on violent behaviour in children and adolescents are reviewed, and potential policy implications are discussed.