Academic Journal
Design, synthesis and biological profiling of bis-thiazole linked Schiff bases as effective enzyme inhibitors for targeting urease and thymidine phosphorylase proteins.
| Title: | Design, synthesis and biological profiling of bis-thiazole linked Schiff bases as effective enzyme inhibitors for targeting urease and thymidine phosphorylase proteins. |
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| Authors: | Khan Y; Department of Chemistry, COMSATS University Islamabad, Islamabad, 45550, Pakistan. yousaf7n@gmail.com., Sarfraz H; Department of Chemistry, Quaid-I-Azam University Islamabad, Islamabad, 45320, Pakistan., Naseem M; Department of Zoology, University of Balochistan, Quetta, Pakistan., Adnan R; Department of Computer Science, COMSATS University Islamabad, Islamabad, 45550, Pakistan., Naqvi SF; Department of Zoology, Quaid-I-Azam University Islamabad, Islamabad, 45320, Pakistan., Khan A; Department of Zoology, Quaid-I-Azam University Islamabad, Islamabad, 45320, Pakistan., Gulshan U; Department of Chemistry, COMSATS University Islamabad, Islamabad, 45550, Pakistan., Aminullah S; Department of Chemistry, COMSATS University Islamabad, Islamabad, 45550, Pakistan. |
| Source: | Naunyn-Schmiedeberg's archives of pharmacology [Naunyn Schmiedebergs Arch Pharmacol] 2026 Mar; Vol. 399 (6), pp. 8883-8906. Date of Electronic Publication: 2026 Jan 15. |
| Publication Type: | Journal Article |
| Language: | English |
| Journal Info: | Publisher: Springer Verlag Country of Publication: Germany NLM ID: 0326264 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1432-1912 (Electronic) Linking ISSN: 00281298 NLM ISO Abbreviation: Naunyn Schmiedebergs Arch Pharmacol Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Berlin, New York, Springer Verlag. |
| MeSH Terms: | Urease*/antagonists & inhibitors , Urease*/metabolism , Thymidine Phosphorylase*/antagonists & inhibitors , Thymidine Phosphorylase*/metabolism , Thiazoles*/pharmacology , Thiazoles*/chemistry , Thiazoles*/chemical synthesis , Enzyme Inhibitors*/pharmacology , Enzyme Inhibitors*/chemical synthesis , Enzyme Inhibitors*/chemistry , Drug Design*, Schiff Bases/pharmacology ; Schiff Bases/chemical synthesis ; Schiff Bases/chemistry ; Structure-Activity Relationship ; Molecular Docking Simulation ; Humans |
| Abstract: | Earlier therapeutic strategies primarily focused on combating diseases caused by external pathogens; recent advancements have highlighted the pivotal role of endogenous enzymes in the progression of non-infectious disorders. Enzymes such as urease and thymidine phosphorylase have been implicated in various pathological conditions, prompting the need for effective enzyme-targeted inhibitors. In this study, a novel series of bis-thiazole linked linked Schiff Bases (1-10) was designed and synthesized as potential dual enzyme inhibitors. The structural integrity of the synthesized compounds was confirmed by FTIR, 1H-NMR, 13C-NMR and HRMS analyses. The derivatives were screened for their inhibitory activity against urease and thymidine phosphorylase. Among them, the synthesized analogues 4, 5, 7, and 8 exhibited significant activity, surpassing the reference inhibitors thiourea (IC (© 2026. The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature.) |
| Competing Interests: | Declarations. Ethics approval: Not applicable. Consent to participate: Written informed consent was obtained from each subject. Consent for publication: Written informed consent for publication was obtained from all participants. Competing interests: The authors declare no competing interests. |
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| Contributed Indexing: | Keywords: Helicobacter pylori; Human thymidine phosphorylase; Molecular docking; Proteus mirabilis; SAR; Schiff Base; Thiazole; Urease |
| Substance Nomenclature: | EC 3.5.1.5 (Urease) 0 (Schiff Bases) EC 2.4.2.4 (Thymidine Phosphorylase) 0 (Thiazoles) 0 (Enzyme Inhibitors) |
| Entry Date(s): | Date Created: 20260115 Date Completed: 20260626 Latest Revision: 20260626 |
| Update Code: | 20260626 |
| DOI: | 10.1007/s00210-025-04879-1 |
| PMID: | 41538058 |
| Database: | MEDLINE |
| ISSN: | 1432-1912 |
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| DOI: | 10.1007/s00210-025-04879-1 |