Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293
Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293
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DOI：
10.1128/aac.46.6.1766-1772.2002
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发表时间：
2002-06-01
影响因子：
4.9
通讯作者：
Rübsamen-Waigmann, H
中科院分区：
文献类型：
--
作者：
Betz, UAK;Fischer, R;Rübsamen-Waigmann, H
BAY 57-1293属于一类新的抗病毒化合物，通过消除病毒引物酶-解旋酶复合物的酶活性，在体外以纳摩尔范围抑制单纯疱疹病毒（HSV）1型和2型的复制。在HSV感染的各种啮齿动物模型中，发现BAY 57-1293的体内抗病毒活性上级目前用于治疗HSV感染的所有化合物。该化合物在播散性疱疹的小鼠和大鼠致死性攻击模型、皮肤病的小鼠带状疱疹样扩散模型和小鼠眼疱疹模型中显示出显著的抗病毒活性。它在胃肠外、口服和局部制剂中具有活性。在疱疹疾病症状已经明显后开始治疗时，BAY 57-1293继续显示出疗效。
BAY 57-1293 belongs to a new class of antiviral compounds and inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity, of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations. BAY 57-1293 continued to demonstrate efficacy when the onset of treatment was initiated after symptoms of herpetic disease were already apparent.