245676-75-9Relevant academic research and scientific papers
Synthesis of novel polyethers in a geometrically precise conformation
Rodriguez, Rosa M.,Morales, Ezequiel Q.,Delgado, Mercedes,Espinola, Carmen G.,Alvarez, Eleuterio,Perez, Ricardo,Martin, Julio D.
, p. 725 - 728 (1999)
Formula presented A convergent design for the preparation of a polyoxyethylene-based channel molecule is presented, and the synthesis of the key unit 2 required for the projected construction is described. The essential elements of the design included fac
Synthesis and biological studies of flexible brevetoxin/ciguatoxin models with marked conformational preference
Candenas,Pinto, Francisco M,Cintado, Cristina G,Morales, Ezequiel Q,Brouard, Ignacio,Díaz, M.Teresa,Rico, Milagros,Rodríguez, Elsa,Rodríguez, Rosa M,Pérez, Ricardo,Pérez, Ruby L,Martín, Julio D
, p. 1921 - 1942 (2007/10/03)
A comparison of the more active polyether toxins which are selective activators of voltage-sensitive sodium channels (VSSC), indicate that these molecules are mostly flat, with a hinge part around the middle of the molecules and a large curvature at one of the ends. Assuming that the receptor is topographically complementary to the active molecules, from the result reported here we could conclude, that the specific requirements of the receptor region can be achieved by synthetic polyether models based on exclusive participation of oxane/oxepane moieties. A new convergent approach to give oxepene rings via double reduction of methyl diacetals is explored. In searching for biological models to further characterize Na+ channels, our studies show that different voltage-dependent Na+ channels are expressed in the rat uterus and activated by brevetoxin-B. However, selected compound models synthesized in this work, failed to inhibit or activate Na+ channel function.
