Indolyl Aryl Sulfones as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Role of Two Halogen Atoms at the Indole Ring in Developing New Analogues with Improved Antiviral Activity
Journal of Medicinal Chemistry2007Vol. 50(20), pp. 5034–5038
Citations Over TimeTop 11% of 2007 papers
Giuseppe La Regina, Antonio Coluccia, Francesco Piscitelli, Alberto Bergamini, Anna Sinistro, Antonella Cavazza, Giovanni Maga, Alberta Samuele, Samantha Zanoli, Ettore Novellino, Marino Artico, Romano Silvestri
Abstract
Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C. These compounds were highly effective against the 112 and the AB1 strains in lymphocytes and inhibited at nanomolar concentration the multiplication of the IIIBBa-L strain in macrophages. Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.
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