2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors

Marika Tiberi, Cristina Tintori, Elisa Rita Ceresola, Roberta Fazi, Claudio Zamperini, Pierpaolo Calandro, Luigi Franchi, Manikandan Selvaraj, Lorenzo Botta, Michela Sampaolo, Diego Saita, Roberto Ferrarese, Massimo Clementi, Filippo Canducci, Maurizio Botta

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)3043-3052
Number of pages10
JournalAntimicrobial Agents and Chemotherapy
Volume58
Issue number6
DOIs
Publication statusPublished - 2014

Fingerprint

HIV-1
HIV Fusion Inhibitors
Anti-HIV Agents
Antiviral Agents
Proteins
Viruses

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology
  • Infectious Diseases

Cite this

Tiberi, M., Tintori, C., Ceresola, E. R., Fazi, R., Zamperini, C., Calandro, P., ... Botta, M. (2014). 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors. Antimicrobial Agents and Chemotherapy, 58(6), 3043-3052. https://doi.org/10.1128/AAC.02739-13

2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors. / 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.

In: Antimicrobial Agents and Chemotherapy, Vol. 58, No. 6, 2014, p. 3043-3052.

Research output: Contribution to journalArticle

Tiberi, M, Tintori, C, Ceresola, ER, Fazi, R, Zamperini, C, Calandro, P, Franchi, L, Selvaraj, M, Botta, L, Sampaolo, M, Saita, D, Ferrarese, R, Clementi, M, Canducci, F & Botta, M 2014, '2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors', Antimicrobial Agents and Chemotherapy, vol. 58, no. 6, pp. 3043-3052. https://doi.org/10.1128/AAC.02739-13
Tiberi M, Tintori C, Ceresola ER, Fazi R, Zamperini C, Calandro P et al. 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors. Antimicrobial Agents and Chemotherapy. 2014;58(6):3043-3052. https://doi.org/10.1128/AAC.02739-13
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. / 2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors. In: Antimicrobial Agents and Chemotherapy. 2014 ; Vol. 58, No. 6. pp. 3043-3052.
@article{dd6e64a44f9b486fb33a5fd4be153b2b,
title = "2-Aminothiazolones as anti-hiv agents that act as gp120-cd4 inhibitors",
abstract = "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.",
author = "Marika Tiberi and Cristina Tintori and Ceresola, {Elisa Rita} and Roberta Fazi and Claudio Zamperini and Pierpaolo Calandro and Luigi Franchi and Manikandan Selvaraj and Lorenzo Botta and Michela Sampaolo and Diego Saita and Roberto Ferrarese and Massimo Clementi and Filippo Canducci and Maurizio Botta",
year = "2014",
doi = "10.1128/AAC.02739-13",
language = "English",
volume = "58",
pages = "3043--3052",
journal = "Antimicrobial Agents and Chemotherapy",
issn = "0066-4804",
publisher = "American Society for Microbiology",
number = "6",

}

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

PY - 2014

Y1 - 2014

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

UR - http://www.scopus.com/inward/citedby.url?scp=84901275739&partnerID=8YFLogxK

U2 - 10.1128/AAC.02739-13

DO - 10.1128/AAC.02739-13

M3 - Article

VL - 58

SP - 3043

EP - 3052

JO - Antimicrobial Agents and Chemotherapy

JF - Antimicrobial Agents and Chemotherapy

SN - 0066-4804

IS - 6

ER -