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Studies on Dibenzylamines as Inhibitors of Venezuelan Equine Encephalitis Virus.
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2019-07-11 , DOI: 10.1021/acsinfecdis.9b00035 Theresa H Nguyen 1 , Nicole N Haese 2 , Nikhil Madadi 1 , Sanjay Sarkar 3 , Kiley Bonin 2 , Cassilyn E Streblow 2 , Sharon Taft-Benz 3 , Nichole A Tower 4 , Lynn Rasmussen 4 , Robert Bostwick 4 , Corinne E Augelli-Szafran 1 , Mark J Suto 1 , Thomas E Morrison 5 , Victor DeFilippis 2 , Mark T Heise 3 , Daniel N Streblow 2 , Ashish K Pathak 1
ACS Infectious Diseases ( IF 4.0 ) Pub Date : 2019-07-11 , DOI: 10.1021/acsinfecdis.9b00035 Theresa H Nguyen 1 , Nicole N Haese 2 , Nikhil Madadi 1 , Sanjay Sarkar 3 , Kiley Bonin 2 , Cassilyn E Streblow 2 , Sharon Taft-Benz 3 , Nichole A Tower 4 , Lynn Rasmussen 4 , Robert Bostwick 4 , Corinne E Augelli-Szafran 1 , Mark J Suto 1 , Thomas E Morrison 5 , Victor DeFilippis 2 , Mark T Heise 3 , Daniel N Streblow 2 , Ashish K Pathak 1
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Alphaviruses are arthropod-transmitted members of the Togaviridae family that can cause severe disease in humans, including debilitating arthralgia and severe neurological complications. Currently, there are no approved vaccines or antiviral therapies directed against the alphaviruses, and care is limited to treating disease symptoms. A phenotypic cell-based high-throughput screen was performed to identify small molecules that inhibit the replication of Venezuelan Equine Encephalitis Virus (VEEV). The compound, 1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-N-(3-fluoro-4-methoxybenzyl)ethan-1-amine (1), was identified as a highly active, potent inhibitor of VEEV with an effective concentration for 90% inhibition of virus (EC90) of 0.89 μM and 7.49 log reduction in virus titers at 10 μM concentration. These data suggest that further investigation of compound 1 as an antiviral therapeutic against VEEV, and perhaps other alphaviruses, is warranted. Experiments suggested that the antiviral activity of compound 1 is directed at an early step in the VEEV replication cycle by blocking viral RNA and protein synthesis.
中文翻译：
二苄胺作为委内瑞拉马脑炎病毒抑制剂的研究。
甲病毒是披膜病毒科的节肢动物传播成员，可导致人类严重疾病，包括使人虚弱的关节痛和严重的神经系统并发症。目前，没有针对甲病毒的批准疫苗或抗病毒疗法，护理仅限于治疗疾病症状。进行了基于表型细胞的高通量筛选，以确定抑制委内瑞拉马脑炎病毒 (VEEV) 复制的小分子。化合物 1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-N-(3-fluoro-4-methoxybenzyl)ethan-1-amine (1) 被鉴定为VEEV 的高活性、强效抑制剂，90% 病毒抑制有效浓度 (EC90) 为 0.89 μM，10 μM 浓度下病毒滴度降低 7.49 对数。这些数据表明，有必要进一步研究化合物 1 作为针对 VEEV 和其他甲病毒的抗病毒治疗剂。实验表明，化合物 1 的抗病毒活性通过阻断病毒 RNA 和蛋白质合成针对 VEEV 复制周期的早期步骤。
更新日期：2019-11-18
中文翻译：
二苄胺作为委内瑞拉马脑炎病毒抑制剂的研究。
甲病毒是披膜病毒科的节肢动物传播成员，可导致人类严重疾病，包括使人虚弱的关节痛和严重的神经系统并发症。目前，没有针对甲病毒的批准疫苗或抗病毒疗法，护理仅限于治疗疾病症状。进行了基于表型细胞的高通量筛选，以确定抑制委内瑞拉马脑炎病毒 (VEEV) 复制的小分子。化合物 1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-N-(3-fluoro-4-methoxybenzyl)ethan-1-amine (1) 被鉴定为VEEV 的高活性、强效抑制剂，90% 病毒抑制有效浓度 (EC90) 为 0.89 μM，10 μM 浓度下病毒滴度降低 7.49 对数。这些数据表明，有必要进一步研究化合物 1 作为针对 VEEV 和其他甲病毒的抗病毒治疗剂。实验表明，化合物 1 的抗病毒活性通过阻断病毒 RNA 和蛋白质合成针对 VEEV 复制周期的早期步骤。
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