Newly synthesized 2-cyclopentylidenehydrazinylthiazoles as potential therapeutic agents against peptic ulcer
Year: 2026
Type: article
Abstract: BACKGROUND: Urease increases the stomach's pH by hydrolyzing urea and fostering the growth of Helicobacter pylori, linked to a variety of gastrointestinal issues, including peptic ulcers. Despite the availability of conventional therapies, the development of safe and effective, nontoxic urease inhibitors with better pharmacological profiles remains an unmet need. METHODS: Novel 2-cyclopentylidenehydr azinyl thiazole derivatives were first time synthesized by first reacting cyclopentanone with thiosemicarbazide to afford thiosemicarbazone which then treated with different phenacyl bromides to afford products. RESULTS: (IC50 = 0.04 ± 0.008 µM) exhibited the highest inhibitory potential against urease. Structure-activity relationship (SAR) indicated that the inhibitory potential is strongly influenced by the electronic and steric factors. Furthermore, molecular docking experiments also revealed various interactions between the ligands (compounds) and the enzyme's active site. Detailed pharmacokinetics, drug-likeness, and absorption, distribution, metabolism, and excretion (ADME) properties were also assessed. CONCLUSION: This study demonstrates that these newly synthesized thiazole derivatives may serve as potential lead candidates for the discovery of antiulcer agents.
Source: Future Medicinal Chemistry
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W7135028009