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Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas
Medicinal Chemistry ( IF 1.9 ) Pub Date : 2020-07-31 , DOI: 10.2174/1573406416666191226142744
Sandra Piras 1 , Paola Corona 1 , Roberta Ibba 1 , Federico Riu 1 , Gabriele Murineddu 1 , Giuseppina Sanna 2 , Silvia Madeddu 2 , Ilenia Delogu 2 , Roberta Loddo 2 , Antonio Carta 1
Affiliation  

Background: Coxsackievirus infections are associated with cases of aseptic meningitis, encephalitis, myocarditis, and some chronic disease.

Methods: A series of benzo[d][1,2,3]triazol-1(2)-yl derivatives (here named benzotriazol-1(2)-yl) (4a-i, 5a-h, 6a-e, g, i, j and 7a-f, h-j) were designed, synthesized and in vitro evaluated for cytotoxicity and antiviral activity against two important human enteroviruses (HEVs) members of the Picornaviridae family [Coxsackievirus B 5 (CVB-5) and Poliovirus 1 (Sb-1)].

Results: Compounds 4c (CC50 >100 μM; EC50 = 9 μM), 5g (CC50 >100 μM; EC50 = 8 μM), and 6a (CC50 >100 μM; EC50 = 10 μM) were found active against CVB-5. With the aim of evaluating the selectivity of action of this class of compounds, a wide spectrum of RNA (positive- and negativesense), double-stranded (dsRNA) or DNA viruses were also assayed. For none of them, significant antiviral activity was determined.

Conclusion: These results point towards a selective activity against CVB-5, an important human pathogen that causes both acute and chronic diseases in infants, young children, and immunocompromised patients.



中文翻译:

新型1- [4-(5,6-二甲基(H)-1H(2H)-苯并三唑-1(2)-基)苯基] -3-烷基(芳基)脲的初步抗柯萨奇活性

背景:柯萨奇病毒感染与无菌性脑膜炎,脑炎,心肌炎和某些慢性疾病有关。

方法:一系列苯并[d] [1,2,3]三唑-1(2)-基衍生物(此处称为苯并三唑-1(2)-基)(4a-i,5a-h,6a-e, g,i,j和7a-f,hj)被设计,合成并体外评估了对Picornaviridae家族的两个重要人类肠道病毒(HEV)成员[Coxsackievirus B 5(CVB-5)和脊髓灰质炎病毒1]的细胞毒性和抗病毒活性(Sb-1)]。

结果:发现化合物4c(CC50> 100μM; EC50 = 9μM),5g(CC50> 100μM; EC50 = 8μM)和6a(CC50> 100μM; EC50 = 10μM)具有抗CVB-5活性。为了评估这类化合物的作用选择性,还检测了广谱的RNA(正反义),双链(dsRNA)或DNA病毒。对于它们中没有一个,确定了显着的抗病毒活性。

结论:这些结果表明对CVB-5有选择性活性,CVB-5是一种重要的人类病原体,可引起婴儿,幼儿和免疫功能低下的患者的急性和慢性疾病。

更新日期:2020-07-31
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