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

摘要

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 IIIB_(Ba-L)strain in macrophages.Compound 16 was exceptionally potent against RT WT and RTs carrying the K103N,Y181I,and L100I mutations.