- Tetrahydrocarbazole amides with potent activity against human papillomaviruses.
Tetrahydrocarbazole amides with potent activity against human papillomaviruses.
Bioorganic & medicinal chemistry letters (2009-06-27)
Kristjan S Gudmundsson, Sharon D Boggs, Paul R Sebahar, Leah D'Aurora Richardson, Andrew Spaltenstein, Pamela Golden, Phiroze B Sethna, Kevin W Brown, Kelly Moniri, Robert Harvey, Karen R Romines
PMID19556128
摘要
Synthesis of a series of tetrahydrocarbazole amides with potent activity against human papillomaviruses is described. Synthetic approaches allowing for variation of the substitution pattern of the tetrahydrocarbazole and the amide are outlined and resulting changes in antiviral activity and certain developability parameters are highlighted. Several compounds with in vitro antiviral activity (W12 antiviral assay) in the single digit nanomolar range were identified and N-[(1R)-6-chloro-2,3,4,9-tetrahydro-1H-carbazol-1-yl]-2-pyridinecarboxamide was selected for further evaluation.
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