2-Aminothiazolones as Anti-HIV Agents That Act as gp120-CD4 Inhibitors

摘要: 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 inhibition gp120-CD4 protein-protein interaction that occurs at very early stage HIV-1 entry process. No cytotoxicity was found for these compounds, and broad antiviral activities against laboratory strains pseudotyped viruses were documented. Docking simulations also been applied predict mechanism, molecular level, by which inhibitors able interact within Phe43 cavity gp120. Furthermore, a preliminary absorption, distribution, metabolism, excretion (ADME) evaluation performed. Overall, this study led basis development more potent HIV inhibitors.