Title: Anti-HIV agents: design and discovery of new potent RT inhibitors
Authors: Barreca, Maria Letizia ×
Chimirri, Alba
De Clercq, Erik
De Luca, Laura
Monforte, Anna-Maria
Monforte, Pietro
Rao, Angela
Zappalà, Maria #
Issue Date: Mar-2003
Series Title: Farmaco (Società chimica italiana : 1989) vol:58 issue:3 pages:259-63
Abstract: This paper reports our work in the field of nonnucleoside RT inhibitors (NNRTIs). On the basis of extensive studies on 1H,3H-thiazolo[3,4-a]benzimidazole derivatives (TBZs) followed by structure-activity relationship (SAR) considerations and molecular modeling, the design and synthesis of a series of 2,3-diaryl-1,3-thiazolidin-4-ones have been performed. Some derivatives proved to be highly effective in inhibiting human immunodeficiency virus type-1 (HIV-1) replication at nanomolar concentrations with minimal toxicity, acting as reverse transcriptase (RT) inhibitors. Computational studies were used in order to probe the binding of our ligands to HIV-1-RT.
ISSN: 0014-827X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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