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ID: ALA1142975

Journal: J Med Chem

Title: 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.

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.

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.

CiteXplore: 17335190

DOI: 10.1021/jm061484y