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首页> 外文期刊>European journal of pharmaceutical sciences >Evaluation of novel pyrrolopyrimidine derivatives as antiviral against gastroenteric viral infections
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Evaluation of novel pyrrolopyrimidine derivatives as antiviral against gastroenteric viral infections

机译:评价新型吡咯基嘧啶衍生物作为抗病毒性病毒感染的抗病毒

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摘要

Viral gastroenteritis is a major global public-health threat. All age groups are susceptible for this infection, but its most serious consequences affect children. Rotavirus, Coxsackievirus and Adenovirus are the most common viruses that cause gastroenteritis. Herein, we synthesized novel pyrrole, pyrrolo[2,3-d]pyrimidine and pyrrolo [3,2-e] [1,2,4]triazolo[4,3-c]pyrimidine derivatives. The non-toxic doses of these compounds were determined using BGM cell lines. We examined all the new compounds for their anti-viral activities against Rotavirus Wa strain and Coxsackievirus B4. Compounds 2a, 2d, 5a, 5c, 5d, 7b, 7j, 7n, 14b, 14c, 14e and 14f exhibited significant antiviral activity. We interpreted the action of these compounds using molecular docking against the homology models of viral polymerase enzymes of these viruses. RMSD value of 5d/Coxsackievirus was higher than the RMSD value for 5d/rotavirus and hence better as a stability parameter, which can be correlated to the biological activity.
机译:病毒性胃肠炎是一个主要的全球性公共卫生威胁。所有年龄组群体易受这种感染,但其最严重的后果会影响儿童。 RotaVirus,Coxsackievirus和腺病毒是导致胃肠炎的最常见病毒。在此,我们合成了新型吡咯,吡咯烷[2,3-D]嘧啶和吡咯[3,2-e] [1,2,4]三唑唑[4,3-C]嘧啶衍生物。使用BGM细胞系测定这些化合物的无毒剂量。我们检查了对RotaVirus WA菌株和Coxsackievirus B4的抗病毒活动的所有新化合物。化合物2a,2d,5a,5c,5d,7b,7j,7n,14b,14c,14e和14f表现出显着的抗病毒活性。我们将这些化合物的作用解释了使用分子对接对这些病毒的病毒聚合酶的同源模型进行分子。 5d / coxsackievirus的RMSD值高于5d / rotavirus的RMSD值,因此稳定参数更好,其可以与生物活性相关。

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