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Title: 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors
Authors: Tiberi, Marika
Tintori, Cristina
Ceresola, Elisa Rita
Fazi, Roberta
Zamperini, Claudio
Calandro, Pierpaolo
Franchi, Luigi
Selvaraj, Manikandan
Botta, Lorenzo
Sampaolo, Michela
Saita, Diego
Ferrarese, Roberto
Clementi, Massimo
Canducci, Filippo
Botta, Maurizio 
Keywords: Pharmacology (medical); Pharmacology; Infectious Diseases
Issue Date: 2014
Project: None 
We report here the synthesis of 2-aminothiazolones along with their biological properties as novel anti-HIV agents. Such compounds have proven to act through the inhibition of the gp120-CD4 protein-protein interaction that occurs at the very early stage of the HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains and pseudotyped viruses were documented. Docking simulations have also been applied to predict the mechanism, at the molecular level, by which the inhibitors were able to interact within the Phe43 cavity of HIV-1 gp120. Furthermore, a preliminary absorption, distribution, metabolism, and excretion (ADME) evaluation was performed. Overall, this study led the basis for the development of more potent HIV entry inhibitors.
ISSN: 0066-4804
DOI: 10.1128/AAC.02739-13
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