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Research in Pharmaceutical Sciences، جلد ۱۳، شماره ۳، صفحات ۲۱۳-۲۲۱
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عنوان انگلیسی Synthesis, antimicrobial evaluation and docking studies of some novel quinazolinone Schiff base derivatives
چکیده انگلیسی مقاله The quinazolin-4(3H)-one structural motif possesses a wide spectrum of biological activities. DNA gyrase play an important role in induction of bacterial death. It has been shown that many quinazolin-4(3H)-one derivatives have antibacterial effects through inhibition of DNA gyrase. Based on this information we decided to synthesize novel quinazolinone Schiff base derivatives in order to evaluate their antibacterial effects. A series of novel quinazolinone Schiff base derivatives were designed and synthesized from benzoic acid. The potential DNA gyrase inhibitory activity of these compounds was investigated using in silico molecular docking simulation. All new synthesized derivatives were screened for their antimicrobial activities against three species of Gram-negative bacteria including Escherichia coli , Pseudomonas aeruginosa , Salmonella entritidis and three species of Gram-positive bacteria comprising of Staphylococcus aurous, Bacillus subtilis, Listeria monocitogenes as well as for antifungal activities against Candida albicans using the conventional micro dilution method. Most of the compounds have shown good antibacterial activities, especially against E. coli at 128 μg/mL concentration while no remarkable antifungal activities were observed for these compounds. All the synthesized compounds exhibit dock score values between -5.96 and -8.58 kcal/mol. The highest dock score among them was -8.58 kcal/mol for compound 4c .
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نویسندگان مقاله | Rezvan Rezaee Nasab
3Medicinal Plants Research Center, Yasuj University of Medical Sciences, Yasuj, I.R. Iran.


| Mahboubeh Mansourian
1Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran. 4Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.


| Farshid Hassanzadeh


نشانی اینترنتی http://rps.mui.ac.ir/index.php/jrps/article/view/1826
فایل مقاله اشکال در دسترسی به فایل - ./files/site1/rds_journals/115/article-115-628428.pdf
کد مقاله (doi)
زبان مقاله منتشر شده en
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نوع مقاله منتشر شده Original Article
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