tailieunhanh - Recent advances in design of new urease inhibitors: A review

Urease is a nickel-dependent metalloenzyme found in plants, some bacteria, and fungi. Bacterial enzyme is of special importance since it has been demonstrated as a potent virulence factor for some species. Especially it is central to Helicobacter pylori metabolism and virulence being necessary for its colonization of the gastric mucosa, and is a potent immunogen that elicits a vigorous immune response. Therefore, it is not surprising that efforts to design, synthesize and evaluate of new inhibitors of urease are and active field of medicinal chemistry. In this paper recent advances on this field are reviewed. | Journal of Advanced Research 13 2018 101-112 Contents lists available at ScienceDirect Journal of Advanced Research journal homepage locate jare Review Recent advances in design of new urease inhibitors A review Pawel Kafarski Michal Talma Department of Bioorganic Chemistry Faculty of Chemistry Wroclaw University of Science and Technology Wybrzeze Wyspianskiego 27 50-370 Wroclaw Poland m Check for updates GRAPHICAL ABSTRACT ARTICLE INFO ABSTRACT Article history Received 30 November 2017 Revised 9 January 2018 Accepted 16 January 2018 Available online 31 January 2018 Keywords Urease Inhibitor design Molecular modeling Inhibitor-enzyme interactions Urease is a nickel-dependent metalloenzyme found in plants some bacteria and fungi. Bacterial enzyme is of special importance since it has been demonstrated as a potent virulence factor for some species. Especially it is central to Helicobacter pylori metabolism and virulence being necessary for its colonization of the gastric mucosa and is a potent immunogen that elicits a vigorous immune response. Therefore it is not surprising that efforts to design synthesize and evaluate of new inhibitors of urease are and active field of medicinal chemistry. In this paper recent advances on this field are reviewed. 2018 Production and hosting by Elsevier . on behalf of Cairo University. This is an open access article under the CC BY-NC-ND license http licenses by-nc-nd . Introduction Being the first organic compound synthesized by Friedrich Wohler from inorganic components 1 urea has a unique role in history. Urea is an endogenous product of protein and amino acid catabolism. For example approximately 20-35 g of urea is excreted in human urine per day. Urea is also used in huge quantities as fertilizer being an exogenous source of ammonia for plants . This compound is hydrolytically stable and the half-life of non-enzymatic hydrolysis of urea is equal years and the mechanism of this .

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• Inhibitor design
• Molecular modeling
• Inhibitor enzyme interactions
• Design of new urease inhibitors
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