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.

Abstract:

:A series of novel, potent orthopoxvirus egress inhibitors was identified during high-throughput screening of the ViroPharma small molecule collection. Using structure--activity relationship information inferred from early hits, several compounds were synthesized, and compound 14 was identified as a potent, orally bioavailable first-in-class inhibitor of orthopoxvirus egress from infected cells. Compound 14 has shown comparable efficaciousness in three murine orthopoxvirus models and has entered Phase I clinical trials.

journal_name

J Med Chem

authors

Bailey TR,Rippin SR,Opsitnick E,Burns CJ,Pevear DC,Collett MS,Rhodes G,Tohan S,Huggins JW,Baker RO,Kern ER,Keith KA,Dai D,Yang G,Hruby D,Jordan R

doi

10.1021/jm061484y

subject

Has Abstract

pub_date

2007-04-05 00:00:00

pages

1442-4

issue

7

eissn

0022-2623

issn

1520-4804

journal_volume

50

pub_type

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