RESUMO
Tetrahydropyridine (THP) moiety is a part of many biologically active systems. The discovery of the neurotoxic properties of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) as well as numerous alkaloids, prompted extensive research on the synthesis and pharmacological properties of these compounds. The goal was extending the database for structure-activity relationship (SAR) studies. Consequently, many promising drug candidates were designed and a lot more are under clinical study. The current paper reviews the most popular approaches for the synthesis of THP derivatives. The pharmacological characteristics of some THP derivatives are summarized together with composite of the data from their in vitro, ex vivo and in vivo assays.
Assuntos
Piridinas , Humanos , Isomerismo , Estrutura Molecular , Piridinas/síntese química , Piridinas/química , Piridinas/farmacologia , Relação Estrutura-AtividadeRESUMO
An approach for quantitative spectrophotometric analysis of binary mixtures based on first derivative spectra is developed. The proposed method is used for investigation of the complex formation of some aza-15-crown-5-containing ligands with Sr(2+), where the stability constant is low and the absorption spectrum of the complex cannot be obtained directly. The described general approach can be applied for quantitative analysis of any other two-component mixture where the absorption spectra of the components cannot be obtained experimentally.
RESUMO
Complexation of two cationic styryl dyes containing aza-15-crown-5 moiety and Na(+), K(+), Ca(2+) and Ba(2+) was investigated spectrophotometrically in water-containing acetonitrile medium. The ligand/complex ratio was estimated using a method for resolution of overlapping bands. A model for evaluation of the water action is proposed and stability constants were calculated for all metal ions in question.
