Producción CyT
Congreso
Autoría
GUTIÉRREZ, EDUARDO LUCIANO
;
Russo, Marcos G.
;
Brusau, Elena V.
;
Ellena, Javier
;
Di Salvo, Florencia
Fecha
2024
Editorial y Lugar de Edición
Instituto de Física de São Carlos (IFSC)
Resumen
Información suministrada por el agente en
SIGEVA
Benzimidazole (B) is a N-containing heterocycle molecule which act as an important pharmacophore exhibiting several biological activities. B derivatives (Bs) present several therapeutic applications, mainly for their pharmacological activities against various pathogens [1]. For example, a series 2-aminobenzimidazole (2-AB) 5-derivatives approved drugs, such as mebendazole (MBZ) and albendazole (ABZ) show broad-spectrum anthelmintic activities and have been extensively used in medicine in the la...
Benzimidazole (B) is a N-containing heterocycle molecule which act as an important pharmacophore exhibiting several biological activities. B derivatives (Bs) present several therapeutic applications, mainly for their pharmacological activities against various pathogens [1]. For example, a series 2-aminobenzimidazole (2-AB) 5-derivatives approved drugs, such as mebendazole (MBZ) and albendazole (ABZ) show broad-spectrum anthelmintic activities and have been extensively used in medicine in the last decades [2].It is of importance the design of Bs multicomponent systems aiming to obtain a new material incorporating the APIs and showing good solubility and dissolution profiles and preventing some problems such us polymorph interconversion. 2-AB and its 5-derivates have a very interesting structure in terms of supramolecular chemistry, with several hydrogen bond acceptor and/or donor sites [3].Here, we present the rational design based on crystal engineering techniques, synthesis and structural determination by single-crystal X-ray diffraction (SCXRD) of a series of new materials as a means to modulate the physicochemical and pharmaceutical properties of 2-AB and the APIs MBZ and ABZ. The rational design of these new materials was performed on the basis of the high statistical probability of formation of a R22(8) supramolecular synthon between the APIs and several oxyanions of trigonal o tetrahedral geometry (Figure 1). Some of these materials have already been fully characterized by SCXRD and a set of complementary solid-state techniques by our group. Preliminary results suggest that these materials present good thermal stability and solubility behaviour, making them suitable for pharmaceutical formulations.
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Palabras Clave
RATIONAL DESIGNCRYSTAL ENGENEERINGSUPRAMOLECULAR SYNTHONBENZIMIDAZOLESX-RAY DIFFRACTION