Novel Hemocompatible Imine Compounds as Alternatives for Antimicrobial Therapy in Pharmaceutical Application

被引:11
作者
Altamimi, Mohammad A. [1 ]
Hussain, Afzal [1 ]
Alshehri, Sultan [1 ,2 ]
Imam, Syed Sarim [1 ]
Alnami, Abdulmalik [1 ]
Bari, Ahmed [3 ,4 ]
机构
[1] King Saud Univ, Dept Pharmaceut, Coll Pharm, Riyadh 11451, Saudi Arabia
[2] Almaarefa Univ, Coll Pharm, Riyadh 11451, Saudi Arabia
[3] King Saud Univ, Coll Pharm, Cent Lab, Riyadh 11451, Saudi Arabia
[4] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia
关键词
novel imine compounds; characterization; in vitro antimicrobial assay; in vitro hemolysis; local and systemic infection control; SCHIFF-BASES; MYCOBACTERIUM-TUBERCULOSIS; SOLID DISPERSIONS; AQUEOUS-MEDIUM; ANTIMYCOBACTERIAL; SPECTROSCOPY; DERIVATIVES; FORMULATION; RIFAMPICIN; EFFICIENT;
D O I
10.3390/pr8111476
中图分类号
TQ [化学工业];
学科分类号
0817 ;
摘要
The aim of this study was to synthesize, characterize, and evaluate neoteric imine compounds for antimicrobial activity and hemocompatibility. Four compounds were synthesized using 3-thiophene carboxaldehyde, ethanol, amine, and acetic acid. The compounds were characterized using nuclear magnetic resonance (NMR) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). A solubility study was conducted with various solvents and surfactants at 40 degrees C. An in vitro antimicrobial assay was performed against bacterial and fungal strains to determine the zone of inhibition and minimum inhibitory concentrations. Finally, an in vitro hemolysis study was conducted using rat erythrocytes. The structure of the compounds was confirmed by NMR, FTIR corroborated their functional group attributes, DSC determined their enthalpies of fusion and fusion temperatures, and PXRD confirmed their crystalline nature. These compounds were water-insoluble but soluble in chloroform, with a maximum solubility of similar to 80 mg/mL. The antimicrobial assay suggested that two of the products exerted potent activities against C. albicans and several bacterial strains. Finally, hemolysis analysis excluded the possibility of hemolysis at the assessed concentrations. In conclusion, two of the novel imine compounds showed promise as antimicrobial agents to control local and systemic microbial infections in a suitable dosage form.
引用
收藏
页码:1 / 19
页数:19
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