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Yaghoub Sarrafi

Yaghoub Sarrafi

Academic rank: Professor
ORCID:
Education: PhD.
ScopusId:
Faculty: Faculty of Chemistry
Address:
Phone: 9121978350

Research

Title
Novel N,N-dimethylbarbituric-pyridinium derivatives as potent urease inhibitors: Synthesis, in vitro, and in silico studies
Type
JournalPaper
Keywords
Urease inhibitor; N,N-dimethylbarbituric; Molecular docking; Barbituric acid; Helicobacter pylori
Year
2020
Journal BIOORGANIC CHEMISTRY
DOI
Researchers Mahmood Biglari ، Roghieh Mirzazadeh ، Mehdi Asadi ، Saghi Sepehri ، Yousef Valizadeh ، Bagher Larijani ، Maryam Mohammadi-Khanaposhtani ، Massoud Amanlou ، Yaghoub Sarrafi ، mohammad mahdavi

Abstract

A new series of N,N-dimethylbarbituric-pyridinium derivatives 7a-n was synthesized and evaluated as Helicobacter pylori urease inhibitors. All the synthesized compounds (IC50 = 10.37 ± 1.0–77.52 ± 2.7 μM) were more potent than standard inhibitor hydroxyurea against urease (IC50 = 100.00 ± 0.2 μM). Furthermore, comparison of IC50 values of the synthesized compounds with the second standard inhibitor thiourea (IC50 = 22.0 ± 0.03 µM) revealed that compounds 7a-b and 7f-h were more potent than thiourea. Molecular modeling study of the most potent compounds 7a, 7b, 7f, and 7g was also conducted. Additionally, the druglikeness properties of the synthesized compounds, based on Lipinski rule and other filters, were evaluated.