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腺苷类似物的广谱抗病毒活性。

Broad-spectrum antiviral activity of adenosine analogues.

作者信息

De Clercq E, Bergstrom D E, Holy A, Montgomery J A

出版信息

Antiviral Res. 1984 Jun;4(3):119-33. doi: 10.1016/0166-3542(84)90012-3.

DOI:10.1016/0166-3542(84)90012-3
PMID:6476818
Abstract

In recent years certain aliphatic and carbocyclic adenosine analogues have been developed which are of potential clinical importance as antiviral agents. This includes (S)-9-(2,3-dihydroxypropyl)adenine [(S)-DHPA] and carbocyclic 3-deazaadenosine (C-c3Ado). (S)-DHPA and C-c3Ado are remarkably similar in their antiviral spectrum in that they are particularly active against (-) RNA viruses such as measles, para-influenza, respiratory syncytial virus, rabies virus, vesicular stomatitis virus and (+/-)RNA viruses such as reo- and rotavirus, whereas (+)RNA viruses such as polio, coxsackie and (+/-)DNA viruses such as herpes simplex are only minimally affected or not inhibited at all. In contrast with (S)-DHPA and C-c3Ado which are quite selective in their antiviral action, other adenosine analogues, i.e., 3-deazaadenosine and 7-deazaadenosine (tubercidin), exhibit little, if any, selectivity as antiviral agents. Also, tubercidin has a broader activity spectrum, encompassing (+)RNA viruses as well as herpes simplex in addition to the (-)RNA viruses. Considering the high antiviral potency of tubercidin, attempts have been undertaken to increase its selectivity, i.e., by chemical substitutions at C-5 of the pyrrolo(2,3-d)pyrimidine ring. These attempts have been partially successful.

摘要

近年来,已经开发出了某些脂肪族和碳环腺苷类似物,它们作为抗病毒剂具有潜在的临床重要性。这包括(S)-9-(2,3-二羟基丙基)腺嘌呤[(S)-DHPA]和碳环3-脱氮腺苷(C-c3Ado)。(S)-DHPA和C-c3Ado在抗病毒谱方面非常相似,因为它们对诸如麻疹、副流感、呼吸道合胞病毒、狂犬病病毒、水疱性口炎病毒等(-)RNA病毒以及诸如呼肠孤病毒和轮状病毒等(+/-)RNA病毒特别有效,而诸如脊髓灰质炎、柯萨奇等(+)RNA病毒以及诸如单纯疱疹等(+/-)DNA病毒仅受到极小影响或根本不被抑制。与在抗病毒作用方面具有相当选择性的(S)-DHPA和C-c3Ado相反,其他腺苷类似物,即3-脱氮腺苷和7-脱氮腺苷(杀结核菌素),作为抗病毒剂几乎没有选择性。此外,杀结核菌素具有更广泛的活性谱,除了(-)RNA病毒外,还包括(+)RNA病毒以及单纯疱疹病毒。鉴于杀结核菌素的高抗病毒效力,人们已尝试提高其选择性,即通过在吡咯并(2,3-d)嘧啶环的C-5处进行化学取代。这些尝试已取得部分成功。

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