发明名称 |
ANTI-VIRAL COMPOSITIONS COMPRISING HETEROCYCLIC SUBSTITUTED PHENYL FURANS AND RELATED COMPOUNDS |
摘要 |
A group of compounds that inhibit HIV replication by blocking HIV entry was identified. One representative compound, designated NB-206, and its analogs inhibited HIV replication (p24 production) with IC50 values at nanomolar levels. It was proved that NB-206 and its analogs are HIV entry inhibitors by targeting the HIV gp41 since: 1) they inhibited HIV-mediated cell fusion; 2) they inhibited HIV replication only when they were added to the cells less than one hour after virus addition; 3) they blocked the formation of the gp41 core that is detected by sandwich enzyme linked immunosorbent assay (ELISA) using a conformation- specific MAb NC-I; and 4) they inhibited the formation of the gp41 six-helix bundle revealed by fluorescence native-polyacrylamide gel electrophoresis (FN-PAGE) . These results suggested that NB-206 and its analogs may interact with the hydrophobic cavity and block the formation of the fusion- active gp41 coiled coil domain, resulting in inhibition of HIV-I mediated membrane fusion and virus entry. |
申请公布号 |
WO2006138118(A2) |
申请公布日期 |
2006.12.28 |
申请号 |
WO2006US21993 |
申请日期 |
2006.06.06 |
申请人 |
NEW YORK BLOOD CENTER;JIANG, SHIBO;DEBNATH, ASIM, KUMAR;LU, HONG |
发明人 |
JIANG, SHIBO;DEBNATH, ASIM, KUMAR;LU, HONG |
分类号 |
A61K31/53;A61K31/427;A61K31/4439;A61K31/496;A61K31/497;A61K31/501 |
主分类号 |
A61K31/53 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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