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牛疱疹病毒1对抗病毒药物的敏感性:(E)-5-(2-溴乙烯基)-2'-脱氧尿苷的体外与体内疗效

Susceptibility of bovid herpesvirus 1 to antiviral drugs: in vitro versus in vivo efficacy of (E)-5-(2-Bromovinyl)-2'-deoxyuridine.

作者信息

Babiuk L A, Acres S D, Misra V, Stockdale P H, De Clercq E

出版信息

Antimicrob Agents Chemother. 1983 May;23(5):715-20. doi: 10.1128/AAC.23.5.715.

Abstract

The relative efficacies of a variety of antiviral drugs against bovid herpesvirus 1 was investigated. (E)-5-(2-Bromovinyl)-2'-deoxyuridine and trifluorothymidine were found to be inhibitory at doses of 0.01 micrograms/ml in in vitro yield reduction and plaque reduction assays. In contrast, acylovir was inactive even at concentrations as high as 1,000 micrograms/ml. Other drugs, including phosphonoformic acid, 9-beta-D-arabinofuranosyladenine, 5-iodo-2-deoxyuridine, and 1-beta-D-arabinofuranosylcytosine were active at concentrations previously shown to inhibit herpes simplex virus. Oral administration of (E)-5-(2-bromovinyl)-2'-deoxyuridine to calves infected with bovid herpesvirus 1 had no effect on the level of virus shedding, clinical signs, or susceptibility to secondary bacterial infection with Pasteurella haemolytica. The reason for this lack of in vivo activity was that sufficient levels of the drug in blood were not achieved by oral administration.

摘要

研究了多种抗病毒药物对牛疱疹病毒1的相对疗效。在体外产量降低和蚀斑减少试验中,发现(E)-5-(2-溴乙烯基)-2'-脱氧尿苷和三氟胸苷在剂量为0.01微克/毫升时具有抑制作用。相比之下,阿昔洛韦即使在浓度高达1000微克/毫升时也无活性。其他药物,包括膦甲酸、9-β-D-阿拉伯呋喃糖基腺嘌呤、5-碘-2'-脱氧尿苷和1-β-D-阿拉伯呋喃糖基胞嘧啶,在先前显示能抑制单纯疱疹病毒的浓度下具有活性。给感染牛疱疹病毒1的小牛口服(E)-5-(2-溴乙烯基)-2'-脱氧尿苷,对病毒排出水平、临床症状或继发溶血性巴氏杆菌细菌感染的易感性没有影响。体内缺乏活性的原因是口服给药未能在血液中达到足够的药物水平。

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