Anti-methicillin resistant Staphylococcus aureus activity, synergism with oxacillin and molecular docking studies of metronidazole-triazole hybrids
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- 作者：Beena Negia ; Deepak Kumara ; Widuranga Kumbukgollab ; Sampath Jayaweerab ; Prija Ponnana ; Ramandeep Singhc ; Sakshi Agarwalc ; Diwan S. Rawata ; dsrawat@chemistry.du.ac.in" class="auth_mail" title="E-mail the corresponding author
- 关键词：MRSA ; Metronidazole ; PBP2a ; Oxacillin ; Triazole ; Methicillin ; Oxacillin
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：10 June 2016
- 年：2016
- 卷：115
- 期：Complete
- 页码：426-437
- 全文大小：1624 K
文摘
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In vitro anti-MRSA activity of a series of 35 metronidazole-triazole hybrids was reported against 30 different MRSA strains.
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One compound evaluated along with oxacillin and showed synergistic activity.
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Compounds were nontoxic up to 50 μM concentration against THP-1 cell lines.
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The time-kill kinetics studies suggested the compounds to be bacteriostatic.
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In silico studies, compounds showed good docking scores and pharmacokinetic properties and follow the Lipinski's rule of 5.