Title: Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a] benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors
Authors: Chimirri, A ×
Grasso, S
Monforte, P
Rao, A
Zappala, M
Monforte, AM
Pannecouque, Christophe
Witvrouw, Myriam
Balzarini, Jan
De Clercq, Erik #
Issue Date: Jul-1999
Publisher: Int medical press
Series Title: Antiviral chemistry & chemotherapy vol:10 issue:4 pages:211-217
Abstract: Using a known human immunodeficiency virus type 1 (HIV-1) non-nucleoside 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, a series of novel 1H,3H-thiazolo[3,4-a]benzimidazole derivatives substituted on the benzene-fused ring was prepared. Their in vitro anti-HIV-1 activity, as well as their inhibitory effects on the viral reverse transcriptase, were evaluated. The structure-activity relationships for these compounds are described and the results suggest that the apolar binding pocket of RT, into which the NNRTIs must fit, can accommodate only groups with a limited size and shape.
ISSN: 0956-3202
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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