Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
作者： A Chimirri , S Grasso , P Monforte , A Rao , M Zappalà
DOI: 10.1177/095632029901000405
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摘要: Using a known human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitor (NNRTI), 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole (TBZ NSC 625487) as the lead structure for drug design, series of novel 1H,3H-thiazolo[3,4-a]benzimidazole derivatives substituted on benzene-fused ring was prepared. Their in vitro anti-HIV-1 activity, well their inhibitory effects viral transcriptase, were evaluated. The structure-activity relationships these compounds are described and results suggest that apolar binding pocket RT, into which NNRTIs must fit, can accommodate only groups with limited size shape.
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