0000000000319859
AUTHOR
Laura Vila
showing 6 related works from this author
COMPOSICIÓN QUIMICA DE LAS HOJAS y SEMILLAS DE SACHA INCHI (Plukenetia volubilis L.); OLEAMIDA
2021
El estudio se realiza con el objeto de identificar el tipo de alcaloide, protoalcaloide opseudoalcaloide, que puedan ser cuantificables en las hojas y en la torta desemillas tostadas y desengrasadas de la especie Plukenetia volubilis L. y demostrar que su presencia no representa un riesgo para la salud. La metodología utilizada está basada en protometría de acuerdo a la Farmacopea Francesa y Europea, así como la utilización de técnicas de UHPLC-MS/MS y GC-MS que han permitido identificar y cuantificar un compuesto endógeno que revela las características de la cis-9-octadecenamida (oleamida), estructura similar a la anandamida; ligando endógeno de receptores cannabinoides en concentraciones …
Synthesis and biological evaluation of sphingosine kinase 2 inhibitors with anti-inflammatory activity.
2019
The synthesis of inhibitors of SphK2 with novel structural scaffolds is reported. These compounds were designed from a molecular modeling study, in which the molecular interactions stabilizing the different complexes were taken into account. Particularly interesting is that 7‐bromo‐2‐(2‐phenylethyl)‐2,3,4,5‐tetrahydro‐1,4‐epoxynaphtho[1,2‐b]azepine, which is a selective inhibitor of SphK2, does not exert any cytotoxic effects and has a potent anti‐inflammatory effect. It was found to inhibit mononuclear cell adhesion to the dysfunctional endothelium with minimal impact on neutrophil–endothelial cell interactions. The information obtained from our theoretical and experimental study can be us…
1-(2′-Bromobenzyl)-6,7-dihydroxy-N-methyl-tetrahydroisoquinoline and 1,2-Demethyl-nuciferine as Agonists in Human D2 Dopamine Receptors
2020
Certain D2-like dopamine receptor (DR) agonists are useful therapeutically as antiparkinsonian drugs, whereas D2-like DR antagonists or partial agonists are proven effective as antipsychotics. Two ...
Synthesis of benzopyran derivatives as PPARα and/ or PPARγ activators
2019
International audience; We describe the synthesis of 26 compounds, small polycerasoidol analogs, that are Lipinski’s rule-of-five compliant. In order to confirm key structural features to activate PPARα and/or PPARγ, we have adopted structural modifications in the following parts: (i) the benzopyran core (hydrophobic nucleus) by benzopyran-4-one, dihydrobenzopyran or benzopyran-4-ol; (ii) the side chain at 2-position by shortening to C3, C4 and C5-carbons versus C-9-carbons of polycerasoidol; (iii) the carboxylic group (polar head) by oxygenated groups (hydroxyl, acetoxy, epoxide, ester, aldehyde) or non-oxygenated motifs (allyl and alkyl). Benzopyran-4-ones 6, 12, 13 and 17 as well as dihy…
Design, synthesis, biological evaluation and molecular modelling of substituted pyrrolo[2,1-a]isoquinolinone derivatives: discovery of potent inhibit…
2021
We report here the design, synthesis and biological evaluation of a new series of substituted pyrrolo[2,1-a]isoquinolin-3-one derivatives, some of which have strong inhibitory activity against both AChE and BChE enzymes. The design of these new inhibitors was carried out taking rivastigmine as the starting structure. Thus, on the basis of an exhausting molecular modeling study using combined techniques (docking, dynamic molecular simulations and QTAIM calculations), we obtained new ligands possessing stronger inhibitory effects than rivastigmine, the reference compound. QTAIM analysis gave us detailed information about the molecular interactions stabilizing the different ligand–enzyme compl…
Synthesis of 2-Prenylated Alkoxylated Benzopyrans by Horner–Wadsworth–Emmons Olefination with PPARα/γ Agonist Activity
2021
[Image: see text] We have synthesized series of 2-prenylated benzopyrans as analogues of the natural polycerasoidol, a dual PPARα/γ agonist with anti-inflammatory effects. The prenylated side chain consists of five or nine carbons with an α-alkoxy-α,β-unsaturated ester moiety. Prenylation was introduced via the Grignard reaction, followed by Johnson–Claisen rearrangement, and the α-alkoxy-α,β-unsaturated ester moiety was introduced by the Horner–Wadsworth–Emmons reaction. Synthetic derivatives showed high efficacy to activate both hPPARα and hPPARγ as dual PPARα/γ agonists. These prenylated benzopyrans emerge as lead compounds potentially useful for preventing cardiometabolic diseases.