No abstract

Our research provided enough evidence of the efficacy of isoxazoles as AChE inhibitors. The isoxazoles were synthesized and evaluated as inhibitors of AChE. The docking study based on a novel series of complexes isoxazole with AChE from Electroporus electricus has demonstrated that the ligand bind is similar to the compounds used as reference. To find new candidates with the isoxazole core that act as inhibitors of AChE, part of the structure of the compound 9 was used for de-novo design. Molecular docking models of the ligand-AChE complexes suggest that the compound 10 is located on the periphery of the AChE active site.

No abstract

The HOMO energies and the charges on the aromatic carbons of two sets of MAO-A-inhibiting phenylisopropylamines, one containing 4-amino substituents, were calculated by the AM1 method, in order to evaluate the importance of charge-transfer interactions between drug and enzyme. Multiple-linear regressions of the pIC50 values on the calculated descriptors were performed with 33 compounds from the two sets, and separately with each set. A poor correlation was obtained when the two sets were merged, as a result of opposing trends shown by the two separate sets. These opposing trends were reconciled by invoking a partial protonation of the basic 4-amino substituents by a hydrogen-bond-donor fragment of the enzyme. The resulting analysis indicated that electron-rich rings and higher HOMO levels tended to increase activity. This model received support from the evaluation of the IMAO activity of four new phenylisopropylamines.

RESUMENAntecedentes: La incontinencia urinaria (IU) corresponde a la pérdida involuntaria de orina. En la medida en que la población envejece, aumenta su prevalencia y severidad. Objetivo: Describir el impacto de la incontinencia de orina en la población adulto mayor, así como conocer su fisiopatología e implicancias en la calidad de vida. Método: Revisión de la literatura disponible en PubMed, Embase y Medline utilizando los términos "urinary incontinence" y "elderly" entre los años 1990 y 2018. Resultados: La IU en el adulto mayor impacta negativamente en la calidad de vida de esta población, teniendo una multiplicidad de causas subyacentes que implican un tratamiento integral y multidisciplinario de esta patología. Conclusión: Dado el incremento de la edad en la población, conocer y manejar esta patología es importante para el clínico y el especialista para que de esta forma mejore la calidad de vida en este grupo etario.