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

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein.
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Gamba E, Mori M, Kovalenko L, Giannini A, Sosic A, Saladini F, Fabris D, Mély Y, Gatto B, Botta M,


Gamba E, Mori M, Kovalenko L, Giannini A, Sosic A, Saladini F, Fabris D, Mély Y, Gatto B, Botta M, (click to view)

Gamba E, Mori M, Kovalenko L, Giannini A, Sosic A, Saladini F, Fabris D, Mély Y, Gatto B, Botta M,

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European journal of medicinal chemistry 2017 12 24145() 154-164 pii 10.1016/j.ejmech.2017.12.073

Abstract

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.

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