Design, Synthesis, Photophysical Properties, Biological Estimation and Molecular Docking Studies of Novel Schiff Base Derivatives as Potential Urease Inhibitors

Journal of Fluorescence
Balasaheb D VanjareKi Hwan Lee

Abstract

A quinoline functionalized two novel fluorescent Schiff bases, N-(quinolin-2-ylmethylene) anthracen-1-amine (SB1) and 2-(quinolin-2-ylmethyleneamino) benzene thiol (SB2) were synthesized and confirmed by using 1H NMR, IR and GC-MS techniques. The spectroscopic properties were examined by absorption spectroscopy and fluorescence spectroscopy. The absorption and fluorescence spectra of the probes (SB1 and SB2) were measured in a variety of solvents. Both the compounds were tested for urease inhibitory activity. The synthesized compound SB2 proved to be the most effective screening for enzyme inhibitory activity with IC50 = 0.111 μM than SB1 (IC50 = 0.287 μM). Molecular docking studies were performed to delineate the binding affinity and conformational positions of chemical compounds within the active region of the target protein. In-vitro analysis depicts the potency of SB1 in free radical scavenging as compared to the reference drug vitamin C.

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Methods Mentioned

BETA
Nuclear magnetic resonance
Fluorescence
column chromatography
Assay

Software Mentioned

GraphPad Prism
VADAR
ACD
UCSF Chimera
Protparam
Molprobity
ChemSketch
Studio
Autodock VINA
PyRx

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