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
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- 作者：Giuseppe La Regina ; Antonio Coluccia ; Francesco Piscitelli ; Alberto Bergamini ; Anna Sinistro ; Antonella Cavazza ; Giovanni Maga ; Alberta Samuele ; Samantha Zanoli ; Ettore Novellino ; Marino Artico ; Romano
- 刊名：Journal of Medicinal Chemistry
- 出版年：2007
- 出版时间：October 4, 2007
- 年：2007
- 卷：50
- 期：20
- 页码：5034 - 5038
- 全文大小：69K
- 年卷期：v.50,no.20(October 4, 2007)
- ISSN：1520-4804
文摘
Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indolering 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 inhibitedat nanomolar concentration the multiplication of the IIIBBa-L strain in macrophages. Compound 16 wasexceptionally potent against RT WT and RTs carrying the K103N, Y181I, and L100I mutations.