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.
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 / LA REGINA, Giuseppe; Coluccia, Antonio; Piscitelli, Francesco; Bergamini, A.; Sinistro, A.; Cavazza, A.; Maga, G.; Samuele, A.; Zanoli, S.; Novellino, E.; Artico, Marino; Silvestri, Romano. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 50:(2007), pp. 5034-5038. [10.1021/jm070488f]
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
LA REGINA, GIUSEPPE;COLUCCIA, Antonio;PISCITELLI, FRANCESCO;ARTICO, Marino;SILVESTRI, Romano
2007
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
