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J Pharm Biomed Anal ; 149: 351-357, 2018 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-29145096

RESUMO

Sulfaguanidine (SG), belongs to the class of sulfonamide drug used as an effective antibiotic. In the present work, using crystal engineering approach two novel cocrystals of SG were synthesized (SG-TBA and SG-PT) with thiobarbutaric acid (TBA) and 1,10-phenanthroline (PT), characterized by solid state techniques viz., powder X-ray diffraction (PXRD), fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and the crystal structures were determined by single crystal X-ray diffraction studies. A comparative antibacterial activity and hemolytic potential was done on SG drug, coformers and their cocrystals. The tested cocrystals formulations showed almost two fold higher antibacterial activity against the tested strains of bacteria Gram-positive bacteria (S. mutans and E. faecalis) and Gram-negative bacteria (E. coli, K. pneumonia and E. clocae) over SG alone and their coformers. Cocrystal SG-TBA showed better antibacterial activity and reduced hemolysis, thereby, reduced cytotoxicity than SG-PT.


Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Composição de Medicamentos/métodos , Hemólise/efeitos dos fármacos , Sulfaguanidina/farmacologia , Antibacterianos/química , Varredura Diferencial de Calorimetria , Química Farmacêutica/métodos , Cristalização/métodos , Cristalografia por Raios X/métodos , Voluntários Saudáveis , Humanos , Testes de Sensibilidade Microbiana/métodos , Conformação Molecular , Fenantrolinas/química , Fenantrolinas/farmacologia , Difração de Pó , Espectroscopia de Infravermelho com Transformada de Fourier , Relação Estrutura-Atividade , Sulfaguanidina/química , Tiobarbitúricos/química , Tiobarbitúricos/farmacologia
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