TY - JOUR
T1 - 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors
AU - Tiberi, Marika
AU - Tintori, Cristina
AU - Ceresola, Elisa Rita
AU - Fazi, Roberta
AU - Zamperini, Claudio
AU - Calandro, Pierpaolo
AU - Franchi, Luigi
AU - Selvaraj, Manikandan
AU - Botta, Lorenzo
AU - Sampaolo, Michela
AU - Saita, Diego
AU - Ferrarese, Roberto
AU - Clementi, Massimo
AU - Canducci, Filippo
AU - Botta, Maurizio
N1 - Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.
PY - 2014/6
Y1 - 2014/6
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84901275739&partnerID=8YFLogxK
U2 - 10.1128/AAC.02739-13
DO - 10.1128/AAC.02739-13
M3 - Article
C2 - 24614386
AN - SCOPUS:84901275739
SN - 0066-4804
VL - 58
SP - 3043
EP - 3052
JO - Antimicrobial Agents and Chemotherapy
JF - Antimicrobial Agents and Chemotherapy
IS - 6
ER -