Synthesis, biological evaluation andin silicostudies of 1,2,3-triazolyl-metronidazole derivatives againstLeishmania major

Abstract

The simple and effective approach for the preparation, of 1,2,3-triazolyl-based metronidazole hybrid analogues as promising anti-leishmania agents using of [CuL-SiO-HA] as a catalyst were described. The catalyst was fully characterized...

Metronidazole Interaction with Cu2+ and Zn2+: Speciation Study in Aqueous Solution and Biological Activity Evaluation

“…Metronidazole (2-methyl-5-nitro-1 H -imidazole-1-ethanol, MNZ), shown in Figure , is a 5-nitroimidazole derivative that exhibits great and selective activity against anaerobic bacteria (e.g., Staphylococcus aureus and Escherichia coli ) − and some protozoa (e.g., Entamoeba , Trichomonas , Trypanosoma , and Leishmania spp. ). − It has also been shown to have excellent antifungal properties . Unfortunately, over the years, its overuse has led to the development of MNZ-resistant microorganisms. − Among the various methods reported in the literature to overcome the resistance issue, complexation with transition metals has proven to be one of the strategies with the greatest potential to enhance the bioactivity of MNZ and protect it from degradation by gastric juice .…”

“…Metronidazole (2-methyl-5-nitro-1 H -imidazole-1-ethanol, MNZ), shown in Figure 1 , 1 is a 5-nitroimidazole derivative that exhibits great and selective activity against anaerobic bacteria (e.g., Staphylococcus aureus and Escherichia coli ) 2 − 6 and some protozoa (e.g., Entamoeba , Trichomonas , Trypanosoma , and Leishmania spp.). 7 − 10 It has also been shown to have excellent antifungal properties. 11 Unfortunately, over the years, its overuse has led to the development of MNZ-resistant microorganisms.…”

Computational study of quinoline-based thiadiazole compounds as potential antileishmanial inhibitors

“…9 The 1,3,4thiadiazole molecule is recognized to show unique and prevalent pharmacological inhibitory activities, such as antileishmanial activity. 10,11 Three-dimensional quantitative structure-activity relationships (3D-QSAR) is regarded as one of the most critical procedures in the computational chemistry field. [12][13][14] Its rational purpose is to hunt for places on molecules that could be modified partially or entirely to help boost their activity.…”

“…9 The 1,3,4-thiadiazole molecule is recognized to show unique and prevalent pharmacological inhibitory activities, such as antileishmanial activity. 10,11…”

Fluorinated-Triazole-Modified ZnO and Its Application in Marine Antifouling

“…Dimitrakellis [20] et al pointed out that a low surface energy antifouling coating with new nano−antibacterial filler can achieve the effect of antibiological attachment and the dual development of an "active" antibacterial. In previous studies, the triazole ring structure widely used in biopharmaceutics can destroy the biomass membrane [21][22][23][24][25][26][27], which is usually combined with fluorine to achieve a synergistic antibacterial mechanism. The fluorine's strong electronegativity and hydrogen−like mimic effect [28][29][30][31][32] harm bacterial reproduction and growth.…”