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Enzyme Inhibitory, Antioxidant And Antibacterial Potentials Of Synthetic Symmetrical And Unsymmetrical Thioureas
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Journal Article
Enzyme Inhibitory, Antioxidant And Antibacterial Potentials Of Synthetic Symmetrical And Unsymmetrical Thioureas
2019
Overview
In this study, 2 symmetrical and 3 unsymmetrical thioureas were synthesized to evaluate their antioxidant, antibacterial, antidiabetic, and anticholinesterase potentials.
The symmetrical thioureas were synthesized in aqueous media in the presence of sunlight, using amines and CS
as starting material. The unsymmetrical thioureas were synthesized using amines as a nucleophile to attack the phenyl isothiocyanate (electrophile). The structures of synthesized compounds were confirmed through H
NMR. The antioxidant potential was determined using DPPH and ABTS assays. The inhibition of glucose-6-phosphatase, alpha amylase, and alpha glucosidase by synthesized compounds was used as an indication of antidiabetic potential. Anticholinesterase potential was determined from the inhibition of acetylcholinesterase and butyrylcholinesterase by the synthesized compounds.
The highest inhibition of glucose-6-phosphatase was shown by compound
(03.12 mg of phosphate released). Alpha amylase was most potently inhibited by compound
with IC
value of 62 µg/mL while alpha glucosidase by compound
with IC
value of 75 µg/mL. The enzymes, acetylcholinesterase, and butyrylcholinesterase were potently inhibited by compound
with IC
of 63 µg/mL and 80 µg/mL respectively. Against DPPH free radical, compound
was more potent (IC
= 64 µg/mL) while ABTS was more potently scavenged by compound
with IC
of 66 µg/mL. The antibacterial spectrum of synthesized compounds was determined against Gram-positive bacteria (
) and Gram-negative bacteria (
and
). Compound
and compound
showed maximum activity against
with MIC values of 4.02 and 4.04 µg/mL respectively. Against
, compound
was more active (MIC = 8.94 µg/mL) while against
.
, compound
was more potent with MIC of 4.03 µg/mL.
From the results, it was concluded that these compounds could be used as antibacterial, antioxidant, and antidiabetic agents. However, further in vivo studies are needed to determine the toxicological effect of these compounds in living bodies. The compounds also have potential to treat neurodegenerative diseases.
Publisher
Dove Medical Press Limited,Taylor & Francis Ltd,Dove Press,Dove,Dove Medical Press
Subject
/ Acetylcholinesterase - metabolism
/ Agrobacterium - drug effects
/ Amines
/ Amylases
/ Anti-Bacterial Agents - chemical synthesis
/ Anti-Bacterial Agents - chemistry
/ Anti-Bacterial Agents - pharmacology
/ Antioxidants - chemical synthesis
/ Bacteria
/ Benzothiazoles - antagonists & inhibitors
/ Biphenyl Compounds - antagonists & inhibitors
/ Butyrylcholinesterase - metabolism
/ Cholinesterase Inhibitors - chemical synthesis
/ Cholinesterase Inhibitors - chemistry
/ Cholinesterase Inhibitors - pharmacology
/ Diabetes
/ Enzymes
/ Glucose
/ Humans
/ Minimum inhibitory concentration
/ NMR
/ Pharmacy
/ Picrates - antagonists & inhibitors
/ Proteus vulgaris - drug effects
/ Staphylococcus aureus - drug effects
/ Staphylococcus aureus infections
/ Sulfonic Acids - antagonists & inhibitors
