N-(3,3a,4,4a,5,5a,6,6a-Octahydro-1,3-dioxo-4,6- ethenocycloprop[f]isoindol-2-(1H)-yl)carboxamides: Identification of Novel Orthopoxvirus Egress Inhibitors
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- 作者：Thomas R. Bailey ; Susan R. Rippin ; Elizabeth Opsitnick ; Christopher J. Burns ; Daniel C. Pevear ; Marc S. Collett ; Gerry Rhodes ; Sanjeev Tohan ; John W. Huggins ; Robert O. Baker ; Earl R. Kern ; Kathy A. K
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：April 5, 2007
- 年：2007
- 卷：50
- 期：7
- 页码：1442 - 1444
- 全文大小：46K
- 年卷期：v.50,no.7(April 5, 2007)
- ISSN：1520-4804
文摘
A series of novel, potent orthopoxvirus egress inhibitors wasidentified during high-throughput screening of the ViroPharma smallmolecule collection. Using structure-activity relationship informationinferred from early hits, several compounds were synthesized, andcompound 14 was identified as a potent, orally bioavailable first-in-class inhibitor of orthopoxvirus egress from infected cells. Compound14 has shown comparable efficaciousness in three murine orthopoxvirusmodels and has entered Phase I clinical trials.