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Combined 3D-QSAR Modeling and Molecular Docking Study on metronidazole-triazole-styryl hybrids as antiamoebic activity


 
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1. Title Title of document Combined 3D-QSAR Modeling and Molecular Docking Study on metronidazole-triazole-styryl hybrids as antiamoebic activity
 
2. Creator Author's name, affiliation, country A. Khaldan, K. El khatabi , R. El-mernissi, A. Sbai, M. Bouachrine , T. Lakhlifi; Moulay Ismail University, Faculty of Science, Meknes, Morocco; Morocco
 
3. Subject Discipline(s)
 
3. Subject Keyword(s) 3D-QSAR; CoMFA; CoMSIA; Molecular docking; Antiamoebic; Entamoeba histolytica; metronidazole; triazole
 
4. Description Abstract

A series of twenty-two metronidazole-triazole-styryl hybrids as antiamoebic agents were studied based on the combination of 3D-QSAR and surflex-docking. The CoMFA and CoMSIA models were carried out using eighteen compounds in the training set and four compounds in the test set gives Q2 values of 0.684 and 0.664 respectively, and R2 values of 0.882 and 0.894 respectively. The adapted alignment method with the suitable parameters resulted in reliable models. Based on contour maps produced by the CoMFA and CoMSIA, we suggested new compounds with high predicted activities, Surflex-docking revealed the important interactions between the ligand and receptor. Therefore, it confirmed the stability of predicted molecules in the receptor with PDB: 4CCQ.

 
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6. Contributor Sponsor(s)
 
7. Date (YYYY-MM-DD) 12-03-2020
 
8. Type Status & genre Peer-reviewed Article
 
8. Type Type
 
9. Format File format PDF
 
10. Identifier Uniform Resource Identifier https://revues.imist.ma/index.php/morjchem/article/view/19099
 
10. Identifier Digital Object Identifier (DOI) https://doi.org/10.48317/IMIST.PRSM/morjchem-v8i2.19099
 
11. Source Title; vol., no. (year) Moroccan Journal of Chemistry; Vol 8, No 2 (2020)
 
12. Language English=en en
 
13. Relation Supp. Files Untitled (B)
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15. Rights Copyright and permissions Copyright (c) 2020 Moroccan Journal of Chemistry