Academic Journal
Newly synthesized 2-cyclopentylidenehydrazinylthiazoles as potential therapeutic agents against peptic ulcer.
| Τίτλος: | Newly synthesized 2-cyclopentylidenehydrazinylthiazoles as potential therapeutic agents against peptic ulcer. |
|---|---|
| Συγγραφείς: | Sehrish; H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.; Department of Chemistry, Jinnah University for Women, Karachi, Pakistan., Salar U; Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan., Naz F; Department of Chemistry, Jinnah University for Women, Karachi, Pakistan., Ishaq A; Center for Advanced Drug Research, COMSATS University Islamabad, Abbottabad, Pakistan.; Department of Chemistry, COMSATS University Islamabad, Abbottabad, Pakistan., Naz F; H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan., Iqbal J; Center for Advanced Drug Research, COMSATS University Islamabad, Abbottabad, Pakistan.; Department of Chemistry, COMSATS University Islamabad, Abbottabad, Pakistan., Khan KM; H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.; Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia. |
| Πηγή: | Future medicinal chemistry [Future Med Chem] 2026 Apr; Vol. 18 (8), pp. 865-880. Date of Electronic Publication: 2026 Mar 12. |
| Τύπος έκδοσης: | Journal Article; Research Support, Non-U.S. Gov't |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE |
| Imprint Name(s): | Publication: 2024- : [Milton Park, Oxfordshire] : Taylor & Francis Original Publication: London : Future Science, 2009- |
| Ιατρικοί όροι (MeSH): | Urease*/antagonists & inhibitors , Urease*/metabolism , Thiazoles*/chemistry , Thiazoles*/pharmacology , Thiazoles*/chemical synthesis , Thiazoles*/therapeutic use , Peptic Ulcer*/drug therapy , Anti-Ulcer Agents*/chemistry , Anti-Ulcer Agents*/pharmacology , Anti-Ulcer Agents*/chemical synthesis , Anti-Ulcer Agents*/therapeutic use , Enzyme Inhibitors*/chemistry , Enzyme Inhibitors*/pharmacology , Enzyme Inhibitors*/chemical synthesis, Helicobacter pylori/drug effects ; Helicobacter pylori/enzymology ; Structure-Activity Relationship ; Molecular Docking Simulation ; Humans ; Molecular Structure |
| Περίληψη: | 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: All compounds exhibited outstanding urease inhibitory activity (IC50 = 0.14 to 6.39 µM) than the standard inhibitors thiourea and acetohydroxamic acid (AHA), with IC50 values of 19.43 and 41.3 µM, respectively. In fact, CH3 bearing compound 10 (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. |
| Contributed Indexing: | Keywords: 2-cyclopentylidenehydrazinyl)thiazole; Synthesis; anti-ulcer activity; molecular docking; structure-activity relationship |
| Substance Nomenclature: | EC 3.5.1.5 (Urease) 0 (Thiazoles) 0 (Anti-Ulcer Agents) 0 (Enzyme Inhibitors) |
| Entry Date(s): | Date Created: 20260312 Date Completed: 20260710 Latest Revision: 20260726 |
| Update Code: | 20260726 |
| PubMed Central ID: | PMC13232998 |
| DOI: | 10.1080/17568919.2026.2642578 |
| PMID: | 41816927 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1756-8927 |
|---|---|
| DOI: | 10.1080/17568919.2026.2642578 |