Asset Details
Do you wish to reserve the book?
Design, synthesis, in vitro, and in silico studies of 4-fluorocinnamaldehyde based thiosemicarbazones as urease inhibitors
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Design, synthesis, in vitro, and in silico studies of 4-fluorocinnamaldehyde based thiosemicarbazones as urease inhibitors
Do you wish to request the book?
Design, synthesis, in vitro, and in silico studies of 4-fluorocinnamaldehyde based thiosemicarbazones as urease inhibitors
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Design, synthesis, in vitro, and in silico studies of 4-fluorocinnamaldehyde based thiosemicarbazones as urease inhibitors
2025
Overview
Clinically significant problems such as kidney stones and stomach ulcers are linked to the activation of the urease enzyme. At low pH, this enzyme gives an ideal environment to Helicobacter pylori in the stomach which is the cause of gastric ulcers and peptic ulcers. In recent work, we have developed a library of 4-fluorocinnamaldehyde base thiosemicarbazones and assessed them for their potential against urease enzyme. The synthesized compounds displayed significant to moderate inhibition potential with IC
50
values ranging from 2.7 ± 0.5 µM to 29.0 ± 0.5 µM. compound
3c
displayed the highest inhibition potential followed by
3a
and
3b
. Two compounds of the series
3f
and
3 g
remained inactive against urease. The kinetic study of compound
3c
exhibited a competitive type of inhibition with a
K
i
value of 3.26 ± 0.0048 µM. SAR analysis was also thoroughly done. Molecular docking was used to analyze the interaction pattern of each derivative, and the outcomes demonstrated that the compounds had excellent binding interactions with the active site.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ ADME
/ Docking
/ Enzyme Inhibitors - chemical synthesis
/ Enzyme Inhibitors - chemistry
/ Enzyme Inhibitors - pharmacology
/ Enzymes
/ FMO
/ Helicobacter pylori - drug effects
/ Helicobacter pylori - enzymology
/ Humanities and Social Sciences
/ Humans
/ Kinetics
/ Molecular Docking Simulation
/ Science
/ Structure-Activity Relationship
/ Thiosemicarbazones - chemical synthesis
/ Thiosemicarbazones - chemistry
/ Thiosemicarbazones - pharmacology
/ Ulcers
/ Urease
