4.4 Article

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

Journal

JOURNAL OF FLUORESCENCE
Volume 28, Issue 6, Pages 1295-1304

Publisher

SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s10895-018-2289-1

Keywords

Schiff base; Photophysical properties; Urease inhibition; Molecular docking

Funding

  1. Mid-Career Researcher Program through the National Research Foundation of Korea (NRF) - Ministry of Science, ICT & Future Planning (MSIP) [NRF-2016R1A2B4016552]

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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 H-1 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=0.111M than SB1 (IC50=0.287M). 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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