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Vol. 25 No. 3 (2013): Vol 25 Issue 3

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Theoretical Analyses of Glibenclamide-Estradiol Derivative and Its Relationship with Some Physico-chemical Descriptors

L. Figueroa-Valverde
Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar sn, Col Buenavista C.P. 24039 Campeche Cam., México
F. Díaz-Cedillo
Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas, C.P. 11340, México D.F.
M. López-Ramos
Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar sn, Col Buenavista C.P. 24039 Campeche Cam., México
E. García-Cervera
Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar sn, Col Buenavista C.P. 24039 Campeche Cam., México
E. Pool Gómez
Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar sn, Col Buenavista C.P. 24039 Campeche Cam., México

Corresponding Author(s) : L. Figueroa-Valverde

lauro_1999@yahoo.com

Asian Journal of Chemistry, Vol. 25 No. 3 (2013): Vol 25 Issue 3

Abstract

A new glibenclamide-estradiol conjugate was synthesized by the reaction of glibenclamidesuccinate and estradiol-ethylenediamine derivative using N,N'-diciclohexylcarbodiimide/p-toluensulfonic acid as catalysts. In order to evaluate the degree of lipophilicity and its relationship with some physicochemical descriptors involved in its chemical structure, the ACD log P and KOWWIN methods were used. The results showed an increase in the values of these physicochemical parameters for the glibenclamide-estradiol conjugate in comparison with glibenclamide and glibenclamide-succinate. These data suggest a relationship between the evaluated physicochemical parameters and the degree of lipophilicity of the glibenclamide-estradiol conjugate.

Keywords

Glibenclamide Estradiol Lipophilicity
Figueroa-Valverde, L., Díaz-Cedillo, F., López-Ramos, M., García-Cervera, E., & Pool Gómez, E. (2012). Theoretical Analyses of Glibenclamide-Estradiol Derivative and Its Relationship with Some Physico-chemical Descriptors. Asian Journal of Chemistry, 25(3), 1405–1409. Retrieved from https://asianpubs.org/index.php/ajchem/article/view/25_3_52
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