title: Novel isothiourea derivatives as potent neuroprotectors and cognition enhancers: synthesis, biological and physicochemical properties.
abstract: Various salts of 3-allyl-1,1-dibenzyl-2-ethyl-isothiourea, 1 (hydrochloride), 2 (hydrobromide), and 3 (hydroiodide), were synthesized. Ca-blocking properties of these salts were studied. Comparative analysis of the potentiating effects of 3 and cyclothiazide (CT) on transmembrane currents caused by kainic acid (KA) and glutamate in Purkinje neurons was performed. Analysis of the effects of 1 on N-methyl-D-aspartate (NMDA) receptors was performed on primary culture of heterogeneous neurons of rat cerebral cortex. Single crystals were grown and X-ray diffraction experiments solving the crystal structures of 1-3 were carried out. Analysis of conformations of the molecules in the crystal lattices was performed. The temperature dependencies of the solubility of 1-3 in water and n-octanol were obtained, and the thermodynamic parameters of solubility process were calculated. The effect of halogen atoms on the solubility was analyzed. The partitioning processes in the water-octanol system were studied at 25 degrees C. Chemical stability of tested salts in pH 7.4 phosphate buffer was determined at 25 degrees C.
authors.affiliation: Institute of Solution Chemistry, Russian Academy of Sciences, Ivanovo, Russia. glp@isc-ras.ru
authors.forename: German L
authors.initials: GL
authors.lastname: Perlovich
authors.forename: Alexey N
authors.initials: AN
authors.lastname: Proshin
authors.forename: Tatyana V
authors.initials: TV
authors.lastname: Volkova
authors.forename: Sergey V
authors.initials: SV
authors.lastname: Kurkov
authors.forename: Vlaimir V
authors.initials: VV
authors.lastname: Grigoriev
authors.forename: Ludmila N
authors.initials: LN
authors.lastname: Petrova
authors.forename: Sergey O
authors.initials: SO
authors.lastname: Bachurin