Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2018

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein

Elia Gamba
  • Fonction : Auteur
Mattia Mori
  • Fonction : Auteur
Alessia Giannini
  • Fonction : Auteur
Alice Sosic
  • Fonction : Auteur
Francesco Saladini
  • Fonction : Auteur
Dan Fabris
  • Fonction : Auteur
Barbara Gatto
  • Fonction : Auteur
Maurizio Botta
  • Fonction : Auteur

Résumé

In this report, we present a new benzoxazole derivative endowed with inhibitory activity against the HIV-1 nucleocapsid protein (NC). NC is a 55-residue basic protein with nucleic acid chaperone properties, which has emerged as a novel and potential pharmacological target against HIV-1. In the pursuit of novel NC-inhibitor chemotypes, we performed virtual screening and in vitro biological evaluation of a large library of chemical entities. We found that compounds sharing a benzoxazolinone moiety displayed putative inhibitory properties, which we further investigated by considering a series of chemical analogues. This approach provided valuable information on the structure-activity relationships of these compounds and, in the process, demonstrated that their anti-NC activity could be finely tuned by the addition of specific substituents to the initial benzoxazolinone scaffold. This study represents the starting point for the possible development of a new class of antiretroviral agents targeting the HIV-1 NC protein.

Dates et versions

hal-03779582 , version 1 (16-09-2022)

Identifiants

Citer

Elia Gamba, Mattia Mori, Lesia Kovalenko, Alessia Giannini, Alice Sosic, et al.. Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein. European Journal of Medicinal Chemistry, 2018, 145, pp.154-164. ⟨10.1016/j.ejmech.2017.12.073⟩. ⟨hal-03779582⟩
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