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NMR-Based Activity Assays for Determining Compound Inhibition, IC50 Values, Artifactual Activity, and Whole-Cell Activity of Nucleoside Ribohydrolases

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Cyclopentyl-linked N-Acylthioureas as Promising Urease Inhibitors: Insights from in vitro Bioassay,

Khansa Mumtaz¹, Sumera Zaib², Aamer Saeed¹

¹Department of Chemistry, Quaid-i-Azam University, Islamabad 45320, Pakistan.

Acta Chimica Slovenica

|December 18, 2025

Summary

This summary is machine-generated.

New N-acylthioureas effectively inhibit urease, an enzyme produced by Helicobacter pylori bacteria. Compounds 4a and 4b show significant potential for treating gastritis and related gastrointestinal disorders.

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Published on: November 22, 2024

Area of Science:

Medicinal Chemistry
Microbiology
Enzyme Inhibition

Background:

Helicobacter pylori (H. pylori) is a Gram-negative bacterium linked to gastrointestinal issues like chronic gastritis and gastric cancer.
Urease enzyme inhibition presents a viable therapeutic strategy against H. pylori-associated diseases.

Purpose of the Study:

To synthesize and evaluate cyclopentyl-bearing N-acylthioureas as potential urease inhibitors.
To identify potent compounds for managing H. pylori infections and associated gastrointestinal conditions.

Main Methods:

Synthesis and characterization of N-acylthiourea compounds (4a-j).
In vitro assessment of urease inhibitory activity compared to a thiourea standard.
Molecular docking and molecular dynamics simulations to analyze ligand-target interactions.
ADME property prediction for druglikeness.

Main Results:

All synthesized compounds demonstrated urease inhibitory activity.
Compounds 4a and 4b exhibited the most potent inhibition, with IC50 values of 2.21 ± 0.62 μM and 3.92 ± 0.59 μM, respectively.
These compounds were approximately 10- and 6-fold more effective than the standard thiourea.
Molecular modeling confirmed favorable interactions and stability of potent inhibitors.

Conclusions:

Cyclopentyl-bearing N-acylthioureas are effective urease inhibitors.
Compounds 4a and 4b show promise as lead compounds for developing novel treatments for H. pylori-related gastritis and other gastrointestinal disorders.