Fungal biofilm inhibition by piperazine-sulphonamide linked Schiff bases: Design, synthesis, and biological evaluation
Ansari, Siddique Akber . 2018
Abstract
We report the synthesis of some new piperazine-sulphonamide linked Schiff bases as
fungal biofilm inhibitors with antibacterial and antifungal potential. The biofilm
inhibition result of Candida albicans proposed that the compounds 6b (IC50 = 32.1 μM)
and 6j (IC50 = 31.4 μM) showed higher inhibitory activity than the standard fluconazole
(IC50 = 40 μM). Compound 6d (MIC = 26.1 μg/mL) with a chloro group at the para
position was found to be the most active antibacterial agent of the series against
Bacillus subtilis when compared with the standard ciprofloxacin (MIC = 50 μg/mL).
Compound 6j (MIC = 39.6 μg/mL) with an OH─ group at the ortho position showed
more potent antifungal activity as compared to that of the standard fluconazole
(IC50 = 50 μM) against C. albicans. Thus, the synthesized compounds 6a–k were found
to be potent biofilm inhibitors as well as active antibacterial and antifungal agents. The
molecular docking study of the synthesized compounds against the secreted aspartyl
protease (SAP5) enzyme of C. albicans exhibited good binding properties. The in silico
ADME properties of the synthesized compounds were also analyzed and showed their
potential to be developed as potential oral drug candidates.
Phthalazine, a structurally and pharmacologically versatile nitrogen-containing heterocycle, has gained more attention from medicinal chemists in the design and synthesis of novel drugs owing to…
Computational approaches such as pharmacophore modeling, virtual screening and MD simulations were explored to find the potential hits as H. pylori specific panC inhibitors for the management of…
Alzheimer’s disease (AD) is a widespread dynamic neurodegenerative malady. Its etiology is still not clear. One of the foremost pathological features is the extracellular deposits of Amyloid-beta…