9 research outputs found
Synthesis and biological evaluation of new fluconazole β-lactam conjugates linked via 1,2,3-triazole
No full textNovel 1,2,3-triazole-linked β-lactam–fluconazole conjugates 12(a–l) were designed and synthesized. The compounds showed potent antifungal activity against two pathogenic Candida strains; Candida albicans ATCC 24433 and Candida albicans ATCC 10231 with MIC values in the range of 0.0625–2 μg mL−1. Compounds 12h, 12j and 12k showed promising antifungal activity against all the tested fungal pathogens except C. neoformans ATCC 34554 compared to fluconazole. Compound 12j in which the β-lactam ring was formed using para-anisidine and benzaldehyde was found to be more potent than fluconazole against all the fungal strains with an IC50 value of <0.015 μg mL−1 for Candida albicans (ATCC 24433). Mechanistic studies for active compounds revealed that the antifungal action was due to ergosterol inhibition. Compounds 12h and 12j at a concentration of 0.125 μg mL−1 caused 91.5 and 96.8% ergosterol depletion, respectively, compared to fluconazole which at the same concentration caused 49% ergosterol depletion. The molecular docking study revealed that all the fluconazole β-lactam conjugates 12(a–l) could snugly fit into the active site of lanosterol 14α-demethylase (CYP51) with varying degrees of affinities. As anticipated, the binding energy for compound 12j (−58.961 kcal mol−1) was much smaller than that for fluconazole (−52.92 kcal mol−1). The synthesized compounds have therapeutic potential for the control of candidemia.</p
Silica-Based Solid Acid Catalyst with Different Concentration of H2SO4 and Calcination Temperature: Preparation and Characterization
No full textMagneto-structural and photocatalytic behavior of mixed Ni–Zn nano-spinel ferrites: visible light-enabled active photodegradation of rhodamine B
No full textEffect of different synthetic routes on the performance of propylene hydroformylation over 3V-PPh3 polymer supported Rh catalysts
No full textIonic liquid attached to colloidal silica nanoparticles: as high performance catalyst for the preparation of dihydrofurans under microwave irradiation
No full textBis (1(3-trimethoxysilylpropyl)-3-methyl-imidazolium) copper tetrachloride attached to colloidal silica nanoparticles as an efficient catalyst for the preparation of propargylamines
No full text
