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Study of hydrophobic properties of biologically active open analogues of flavonoids.
Opletalová, Veronika; Kastner, Petr; Kucerová-Chlupácová, Marta; Palát, Karel.
Afiliación
  • Opletalová V; Department of Pharmaceutical Chemistry and Drug Control, Charles University in Prague, Faculty of Pharmacy in Hradec Kralove, Hradec Kralove, Czech Republic.
J Mol Graph Model ; 39: 61-4, 2013 Feb.
Article en En | MEDLINE | ID: mdl-23220282
Hydrophobicity can either be determined experimentally or predicted by means of commercially available programs. In the studies concerning biological activities of pyrazine analogues of chalcones, 3-(2-hydroxyphenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones were more potent than the corresponding 3-(4-hydroxyphenyl)-1-(pyrazin-2-yl)prop-2-en-1-ones. As the difference in lipophilicity may be a factor responsible for the difference in the potency, R(M) values of the compounds were determined by RP-TLC and compared with logP values calculated by various commercially available programs. Important discrepancies were found between experimental and computational lipophilicity data. Therefore, we have tried to find a reliable method for calculating R(M) values from in silico derived molecular parameters. The R(M) values obtained with the chromatographic system consisting of Silufol UV 254 plates impregnated with silicon oil as the stationary phase and acetone-citrate buffer (pH=3) 50:50 (v/v) as the mobile phase correlated well with van der Waals volumes (V(W)) and hydration energies [Formula: see text] derived of molecular models calculated on RHF/AM1 level.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Flavonoides / Interacciones Hidrofóbicas e Hidrofílicas Tipo de estudio: Prognostic_studies Idioma: En Revista: J Mol Graph Model Asunto de la revista: BIOLOGIA MOLECULAR Año: 2013 Tipo del documento: Article País de afiliación: República Checa Pais de publicación: Estados Unidos

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Flavonoides / Interacciones Hidrofóbicas e Hidrofílicas Tipo de estudio: Prognostic_studies Idioma: En Revista: J Mol Graph Model Asunto de la revista: BIOLOGIA MOLECULAR Año: 2013 Tipo del documento: Article País de afiliación: República Checa Pais de publicación: Estados Unidos