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Paper Information

Journal:   JOURNAL OF THE IRANIAN CHEMICAL SOCIETY(JICS)   2014 , Volume 11 , Number 4; Page(s) 1113 To 1119.
 
Paper: 

NOVEL AND VERSATILE METHODOLOGY FOR SYNTHESIS OF β-ARYL-β-MERCAPTO KETONE DERIVATIVES AS POTENTIAL UREASE INHIBITORS

 
 
Author(s):  AHARI MOSTAFAVI MOHAMMAD MAHDI, SHARIFI ALI, MIRZAEI MOJTABA, AMANLOU MASSOUD
 
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Abstract: 

The objective was to obtain new scaffold of compounds possessing anti-urease activity. For this new and simple method for the synthesis of b-aryl-b-mercapto ketone derivatives based on Michael addition of thiophenol to chalcones in an ionic liquid as a solvent was improved. The products were obtained in good to moderate yields with high purity and characterized by spectral and elemental analyses. The activities of synthesized compounds were investigated as new inhibitors of jack bean urease. Among 22 synthesized compounds, all of them have shown inhibitory effect in micromolar range, and the most potent one has IC50=6 mM compared to hydroxyurea IC50=100 mM as a reference inhibitor. A docking study was performed using Autodock 4.2 in parallel to in vitro experiments to illustrate the corresponded binding affinities as well as binding site, and involved residues in interaction. These computational results complimented the experimental inhibition activity and enabled us to report a potent urease inhibitors based on b-aryl-b-mercapto ketone scaffold.

 
Keyword(s): β-ARYL-β-MERCAPTO KETONE, UREASE INHIBITORS, MOLECULAR DOCKING
 
 
References: 
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Click to Cite.
APA: Copy

AHARI MOSTAFAVI, M., & SHARIFI, A., & MIRZAEI, M., & AMANLOU, M. (2014). NOVEL AND VERSATILE METHODOLOGY FOR SYNTHESIS OF β-ARYL-β-MERCAPTO KETONE DERIVATIVES AS POTENTIAL UREASE INHIBITORS. JOURNAL OF THE IRANIAN CHEMICAL SOCIETY(JICS), 11(4), 1113-1119. https://www.sid.ir/en/journal/ViewPaper.aspx?id=403431



Vancouver: Copy

AHARI MOSTAFAVI MOHAMMAD MAHDI, SHARIFI ALI, MIRZAEI MOJTABA, AMANLOU MASSOUD. NOVEL AND VERSATILE METHODOLOGY FOR SYNTHESIS OF β-ARYL-β-MERCAPTO KETONE DERIVATIVES AS POTENTIAL UREASE INHIBITORS. JOURNAL OF THE IRANIAN CHEMICAL SOCIETY(JICS). 2014 [cited 2021May06];11(4):1113-1119. Available from: https://www.sid.ir/en/journal/ViewPaper.aspx?id=403431



IEEE: Copy

AHARI MOSTAFAVI, M., SHARIFI, A., MIRZAEI, M., AMANLOU, M., 2014. NOVEL AND VERSATILE METHODOLOGY FOR SYNTHESIS OF β-ARYL-β-MERCAPTO KETONE DERIVATIVES AS POTENTIAL UREASE INHIBITORS. JOURNAL OF THE IRANIAN CHEMICAL SOCIETY(JICS), [online] 11(4), pp.1113-1119. Available: https://www.sid.ir/en/journal/ViewPaper.aspx?id=403431.



 
 
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