Academic Journal
Expression, Purification, and Comparative Inhibition of Helicobacter pylori Urease by Regio-Selectively Alkylated Benzimidazole 2-Thione Derivatives.
| Τίτλος: | Expression, Purification, and Comparative Inhibition of Helicobacter pylori Urease by Regio-Selectively Alkylated Benzimidazole 2-Thione Derivatives. |
|---|---|
| Συγγραφείς: | Mohammed SO; Medicinal and Aromatic Plants and Traditional Medicine Research Institute, National Center for Research, Khartoum 11111, Sudan., El Ashry SHE; Chemistry Department, Faculty of Science, Alexandria University, Alexandria 21568, Egypt., Khalid A; Medicinal and Aromatic Plants and Traditional Medicine Research Institute, National Center for Research, Khartoum 11111, Sudan.; Substance Abuse and Toxicology Research Center, Jazan University, Jazan 45142, Saudi Arabia., Amer MR; Chemistry Department, Faculty of Science, Alexandria University, Alexandria 21568, Egypt., Metwaly AM; Pharmacognosy and Medicinal Plants Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt.; Biopharmaceutical Products Research Department, Genetic Engineering and Biotechnology Research Institute, City of Scientific Research and Technological Applications (SRTA-City), Alexandria 21934, Egypt., Eissa IH; Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt., Elkaeed EB; Department of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Ad Diriyah, Riyadh 13713, Saudi Arabia., Elshobaky A; Botany Department, Faculty of Science, Mansoura University, Mansoura 35516, Egypt., Hafez EE; Plant Protection and Biomolecular Diagnosis Department, City of Scientific Research and Technological Applications, ARADI, Alexandria 21934, Egypt. |
| Πηγή: | Molecules (Basel, Switzerland) [Molecules] 2022 Jan 27; Vol. 27 (3). Date of Electronic Publication: 2022 Jan 27. |
| Τύπος έκδοσης: | Comparative Study; Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE |
| Imprint Name(s): | Original Publication: Basel, Switzerland : MDPI, c1995- |
| Ιατρικοί όροι (MeSH): | Urease*/antagonists & inhibitors , Urease*/biosynthesis , Urease*/genetics , Urease*/isolation & purification , Molecular Docking Simulation*, Benzimidazoles/*chemistry , Enzyme Inhibitors/*chemistry , Helicobacter pylori/*enzymology, Bacterial Proteins/antagonists & inhibitors ; Bacterial Proteins/biosynthesis ; Bacterial Proteins/genetics ; Bacterial Proteins/isolation & purification ; Helicobacter pylori/genetics |
| Περίληψη: | The urease enzyme has been an important target for the discovery of effective pharmacological and agricultural products. Thirteen regio-selectively alkylated benzimidazole-2-thione derivatives have been designed to carry the essential features of urease inhibitors. The urease enzyme was isolated from Helicobacter pylori as a recombinant urease utilizing the His-tag method. The isolated enzyme was purified and characterized using chromatographic and FPLC techniques showing a maximal activity of 200 mg/mL. Additionally, the commercial Jack bean urease was purchased and included in this study for comparative and mechanistic investigations. The designed compounds were synthesized and screened for their inhibitory activity against the two ureases. Compound 2 inhibited H. pylori and Jack bean ureases with IC |
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| Grant Information: | TUMA-2021-4 Research center at AlMaarefa University for funding this work under TUMA project |
| Contributed Indexing: | Keywords: benzimidazole 2-thione; molecular docking; o-phenylenediamine; recombinant urease; regioselectivity; urease inhibition |
| Substance Nomenclature: | 0 (Bacterial Proteins) 0 (Benzimidazoles) 0 (Enzyme Inhibitors) EC 3.5.1.5 (Urease) |
| Entry Date(s): | Date Created: 20220215 Date Completed: 20220223 Latest Revision: 20220223 |
| Update Code: | 20260130 |
| PubMed Central ID: | PMC8838460 |
| DOI: | 10.3390/molecules27030865 |
| PMID: | 35164122 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1420-3049 |
|---|---|
| DOI: | 10.3390/molecules27030865 |