Journal of pharmaceutical and biomedical analysis · 2017
Sulfaguanidine cocrystals: Synthesis, structural characterization and their antibacterial and hemolytic analysis.
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Abidi Syed Sibte Asghar, Azim Yasser, Khan Shahper Nazeer, Khan Asad U
Аннотация
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.
Предметные рубрики MeSH
Anti-Bacterial AgentsBacteriaCalorimetry, Differential ScanningChemistry, PharmaceuticalCrystallizationCrystallography, X-RayDrug CompoundingHealthy VolunteersHemolysisHumansMicrobial Sensitivity TestsMolecular ConformationPhenanthrolinesPowder DiffractionSpectroscopy, Fourier Transform InfraredStructure-Activity RelationshipSulfaguanidineThiobarbiturates