| 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
|
| リソース情報 |
| ヒト・動物細胞 |
MDCK(RCB0995) |
