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

被引：52
作者：
La Regina, Giuseppe
Coluccia, Antonio
Piscitelli, Francesco
Bergamini, Alberto
Sinistro, Anna
Cavazza, Antonella
Maga, Giovanni
Samuele, Alberta
Zanoli, Samantha
Novellino, Ettore
Artico, Marino
Silvestri, Romano
机构：
[1] Univ Roma La Sapienza, Dipartimento Farmaceut, Inst Pasteur, Fdn Cenci Bolognetti, I-00185 Rome, Italy
[2] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy
[3] CNR, Ist Genet Mol, I-27100 Pavia, Italy
[4] Univ Roma Tor Vergata, Dipartimento Sanita Pubbl & Biol Cellulare, I-00133 Rome, Italy
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 20期
关键词：
D O I：
10.1021/jm070488f
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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 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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页码：5034 / 5038
页数：5
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