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Title: Structural investigation of the naphthyridone scaffold: identification of a 1,6-naphthyridone derivative with potent and selective anti-HIV activity
Authors: Tabarrini, Oriana ×
Massari, Serena
Sancineto, Luca
Daelemans, Dirk
Sabatini, Stefano
Manfroni, Giuseppe
Cecchetti, Violetta
Pannecouque, Christophe #
Issue Date: Jul-2011
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Series Title: ChemMedChem vol:6 issue:7 pages:1249-1257
Article number: 10.1002/cmdc.201100073
Abstract: Building upon a large, previously reported series of anti-HIV 6-desfluoroquinolones endowed with a peculiar mechanism of action, the inhibition of Tat-mediated transcription, replacement of the quinolone nucleus with a naphthyridone core was shown to be very productive. In this work, the naphthyridone scaffold was investigated in depth by synthesizing various analogues. This led to the identification of NM13 as the most selective derivative obtained in MT-4 cells. It is the result of the successful combination of the 1,6-naphthyridone nucleus and the C7 benzothiazolpiperazine group, which, for the first time, not only grants potent anti-HIV activity but displays very high selectivity. Further studies aimed at a more thorough investigation of the anti-HIV profile of this new derivative are in progress.
URI: 
ISSN: 1860-7179
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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