Synthesis, characterization and biological activity studies on amide derivatives

S. Türk, K. Turan, S. Ulusoy, S. Karakuş, G. Boşgelmez-Tinaz
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Abstract

DOI : 10.26650/IstanbulJPharm.2018.18007 In this study, with intent to find out novel anti-biofilm and antiviral agents, a series of amide  derivatives were synthesized and their structures were elucidated by FT-IR and 1H-NMR and  13C-NMR and MS methods. And also, their purity were proven by TLC, HPLC and elemental  analyses. And finally, the synthesized compounds were examined for their biofilm formation  and swarming motility inhibitory activities in P. aeruginosa PA01. These compounds were  found to reduce biofilm formation by 8.7-25.6% and swarming motility by 18.3-33.8% in P.  aeruginosa PA01 at a concentration of 200 μM. Besides, all of the compounds were evaluated for their antiviral activity against influenza A viruses. The plaque inhibition assays indicated  that compound 6 (N-(4-{[5-(ethylamino)-1,3,4-thiadiazol-2-yl]methyl}phenyl)-4-  fluorobenzamide) has considerable inhibitory effect on influenza A virus plaque formation.
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酰胺类衍生物的合成、表征及生物活性研究
为了寻找新的抗生物膜和抗病毒药物,本研究合成了一系列酰胺衍生物,并通过FT-IR和1H-NMR以及13C-NMR和MS方法对其结构进行了鉴定。并通过薄层色谱、高效液相色谱和元素分析对其纯度进行了验证。最后,对合成的化合物在铜绿假单胞菌PA01中的生物膜形成和蜂群运动抑制活性进行了研究。在200 μM浓度下,这些化合物可使P. aeruginosa PA01的生物膜形成减少8.7-25.6%,使蜂群运动减少18.3-33.8%。此外,对所有化合物的抗病毒活性进行了评价。斑块抑制实验表明,化合物6 (N-(4-{[5-(乙胺)-1,3,4-噻二唑-2-基]甲基}苯基)-4-氟苯酰胺)对甲型流感病毒斑块形成具有显著的抑制作用。
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