ArticleEuropean journal of medicinal chemistry2018
Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein.
Article in European journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 10 citations in OpenAlex.
- Design, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugatesJournal of enzyme inhibition and medicinal chemistry · 2022Article
- Article
- Inhibitory Effect of Lithospermic Acid on the HIV-1 Nucleocapsid Protein.Molecules (Basel, Switzerland) · 2020Article
- 5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.ACS medicinal chemistry letters · 2020Article
- A Class of Potent Inhibitors of the HIV-1 Nucleocapsid Protein Based on Aminopyrrolic Scaffolds.ACS medicinal chemistry letters · 2020Article
- Synthesis of distal and proximal fleximer base analogues and evaluation in the nucleocapsid protein of HIV-1.Bioorganic & medicinal chemistry · 2019Article
- Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein.ACS medicinal chemistry letters · 2019Article
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Authors and funding
10 authors at 4 institutions in 4 countries.
Funding
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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Registered trials
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