論文 - 詳細
| RRC ID | 39480 |
|---|---|
| 著者 | Hisaki M, Imabori H, Azuma M, Suzutani T, Iwakura F, Ohta Y, Kawanishi K, Ichigobara Y, Node M, Nishide K, Yoshida I, Ogasawara M. |
| タイトル | Synthesis and anti-influenza virus activity of novel pyrimidine derivatives. |
| ジャーナル | Antiviral Res |
| Abstract |
Efficient synthetic routes of 2-amino-4-(omega-hydroxyalkylamino)pyrimidine derivatives were investigated in relation to the anti-influenza virus activity of these compounds. The derivatives in which cyclobutyl and cyclopentyl groups were introduced to the beta-position of the aminoalkyl group (especially the cyclobutyl group substituted by a phenylalkyl group at the 3'-position) resulted in improved antiviral potency: i.e. an average 50% effective concentration for inhibition of plaque formation (EC50, microM) of 0.1-0.01 microM for both types A and B influenza virus. The antiviral efficacies were in the order of amino group > hydroxyiminomethyl group > halogen substitution at the 5-position, and chlorine or methoxy group > hydrogen at the 6-position of the pyrimidine ring. The antiviral indices of these compounds were 2-6 with respect to the 50% inhibitory concentration for cell proliferation (IC50, microM) for growing cells, but > 500 to > 10(4) with respect to the IC50 for stationary cells, indicating that these compounds may be efficacious for the topical treatment of influenza virus infection. |
| 巻・号 | 42(2) |
| ページ | 121-37 |
| 公開日 | 1999-6-1 |
| DOI | 10.1016/s0166-3542(99)00019-4 |
| PII | S0166-3542(99)00019-4 |
| PMID | 10389655 |
| MeSH | Animals Antiviral Agents / chemical synthesis Antiviral Agents / pharmacology* Cell Line Humans Inhibitory Concentration 50 Microbial Sensitivity Tests Orthomyxoviridae / drug effects* Pyrimidines / chemical synthesis Pyrimidines / pharmacology* Structure-Activity Relationship |
| IF | 4.101 |
| 引用数 | 9 |
| WOS 分野 | PHARMACOLOGY & PHARMACY VIROLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 3 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | MDCK(RCB0995) |