%0 Journal Article
%A Barreca, Maria L.
%A Balzarini, Jan
%A Chimirri, Alba
%A Clercq, Erik De
%A Luca, Laura De
%A Höltje, Hans Dieter
%A Höltje, Monika
%A Monforte, Anna Maria
%A Monforte, Pietro
%A Pannecouque, Christophe
%A Rao, Angela
%A Zappalà, Maria
%D 2002
%T Design, Synthesis, Structure−Activity Relationships, and Molecular Modeling
Studies of 2,3-Diaryl-1,3-thiazolidin-4-ones as Potent Anti-HIV Agents
%U https://acs.figshare.com/articles/journal_contribution/Design_Synthesis_Structure_Activity_Relationships_and_Molecular_Modeling_Studies_of_2_3-Diaryl-1_3-thiazolidin-4-ones_as_Potent_Anti-HIV_Agents/3681435
%R 10.1021/jm020977+.s001
%2 https://acs.figshare.com/ndownloader/files/5771283
%K NNRTI
%K nonnucleoside HIV
%K Molecular Modeling Studies
%K Computational studies
%K nanomolar concentrations
%K RT inhibitors
%K TBZ
%X Starting from 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), we performed the design, synthesis,
and the structure−activity relationship studies of a series of 2,3-diaryl-1,3-thiazolidin-4-ones.
Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar
concentrations with minimal cytotoxicity, thereby acting as nonnucleoside HIV-1 RT inhibitors
(NNRTIs). Computational studies were used to delineate the ligand-RT interactions and to
probe the binding of the ligands to HIV-1 RT.
%I ACS Publications