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Quinazolinone azolyl ethanols: Potential lead antimicrobial agents with dual action modes targeting methicillin-resistant Staphylococcus aureus DNA
Peng X.-M.1; Peng L.-P.1; Li S.2; Avula S.R.1; Kannekanti V.K.1; Zhang S.-L.3; Tam K.Y.3; Zhou C.-H.1
2016-10-01
Source PublicationFuture Medicinal Chemistry
ISSN17568927 17568919
Volume8Issue:16Pages:1927-1940
Abstract

Aim: Due to bacterial drug resistance, a new series of quinazolinone azolyl ethanols were synthesized and evaluated. Results: In vitro antibacterial assay showed that triazolyl ethanol quinazolinone 3a was the most active compound, especially against methicillin-resistant Staphylococcus aureus (MRSA) with minimal inhibitory concentration value of 8 μg/ml, which was superior to chloromycin and comparable to norfloxacin. Molecular docking study displayed that compound 3a could interact with MRSA DNA by the formation of hydrogen bonds. Further interactions of quinazolinone 3a with MRSA DNA suggested that it could intercalate into MRSA DNA to form 3a-DNA complex. DNA cleavage properties of 3a-Cu and 3a-Zn complexes were confirmed by agarose gel electrophoresis experiments. Conclusion: Compound 3a should be a potential lead antibacterial molecule with dual action modes.

KeywordAntibacterial Antifungal Dna Cleavage Dna Intercalation Imidazole Quinazolinone Triazole
DOI10.4155/fmc-2016-0002
URLView the original
Indexed BySCI
Language英语
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal
WOS IDWOS:000386339000005
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Cited Times [WOS]:28   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Southwest China Normal University
2.Chongqing University of Technology
3.Universidade de Macau
Recommended Citation
GB/T 7714
Peng X.-M.,Peng L.-P.,Li S.,et al. Quinazolinone azolyl ethanols: Potential lead antimicrobial agents with dual action modes targeting methicillin-resistant Staphylococcus aureus DNA[J]. Future Medicinal Chemistry,2016,8(16):1927-1940.
APA Peng X.-M..,Peng L.-P..,Li S..,Avula S.R..,Kannekanti V.K..,...&Zhou C.-H..(2016).Quinazolinone azolyl ethanols: Potential lead antimicrobial agents with dual action modes targeting methicillin-resistant Staphylococcus aureus DNA.Future Medicinal Chemistry,8(16),1927-1940.
MLA Peng X.-M.,et al."Quinazolinone azolyl ethanols: Potential lead antimicrobial agents with dual action modes targeting methicillin-resistant Staphylococcus aureus DNA".Future Medicinal Chemistry 8.16(2016):1927-1940.
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