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Antiviral and Quantitative Structure Activity Relationship Study for Dihydropyridones Derived from Curcumin | Science Publications

机译:姜黄素衍生的二氢吡啶酮类化合物的抗病毒和定量结构活性关系研究科学出版物

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> Problem statement: Pyridones are known to have variety of biological activities like antitumor, antibacterial, anti-inflammatory and antimalarial activities. This study presents antiviral evaluation of dihydropyridones derived from curcumin, as well as curcumin for comparison. Approach: The compounds evaluated for their in vitro antiviral activities against the viruses: HIV-1, Bovin viral Diarrhea, Yellow Fever, Reovirus 1, Herpesvirus 1, Vaccinia, Vescular Stomatitis, Coxackie virus B2, Poliovirus 1 and Respiratory Syncytial viruses by using Microculture Tetrazolium assay (MTT) method. The method was based on the metabolic reduction of 3-(4,5-dimethylthiazol-2- yl)-2,5-diphenyltetrazolium bromide. Results: Antiviral biological activities represented as CC50 were within the range 100-26 for BHK-21, while they were within the range 90-≥13 against Respiratory Syncytial Virus when represented as EC50 for example. Both CC50 and EC50 values were found to increase with increasing chain length of the substituent on the nitrogen atom. Conclusion: The in vitro antiviral activities of the tested dihydropyridones can be enhanced by increasing chain length of the substituent on the nitrogen atom.
机译: > 问题陈述:吡啶酮具有多种生物活性,例如抗肿瘤,抗菌,抗炎和抗疟疾活性。这项研究提出了姜黄素和姜黄素的二氢吡啶酮类药物的抗病毒评价,以进行比较。 方法:这些化合物针对下列病毒的体外抗病毒活性进行了评估:HIV-1,牛病毒性腹泻,黄热病,呼肠孤病毒1,疱疹病毒1,牛痘,血管性口腔炎,柯萨奇B2病毒,脊髓灰质炎病毒1和通过微培养四唑测定法(MTT)检测呼吸道合胞病毒。该方法基于3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四唑溴化物的代谢还原。 结果:对于BHK-21,以CC50表示的抗病毒生物活性在> 100-26范围内,而以EC 表示的对呼吸道合胞病毒的抗病毒生物学活性在>90-≥13范围内。 50 。发现CC 50 和EC 50 值均随着氮原子上取代基链长的增加而增加。 结论:可以通过增加氮原子上取代基的链长来增强所测试的二氢吡啶酮的体外抗病毒活性。

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