Mori, Mattia; Dasso Lang, Maria Chiara; Saladini, Francesco; Palombi, Nastasja; Kovalenko, Lesia; De Forni, Davide; Poddesu, Barbara; Friggeri, Laura; Giannini, Alessia; Malancona, Savina; Summa, Vincenzo; Zazzi, Maurizio; Mely, Yves; Botta, Maurizio published the artcile< Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein>, Application In Synthesis of 20099-90-5, the main research area is aminothiazole preparation antiretroviral HIV 1 nucleocapsid protein inhibitor; structure activity aminothiazole antiretroviral nucleocapsid protein inhibitor.
Small mol. inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and tested in vitro 18 NC inhibitors (NCIs) bearing a double functionalization. In these NCIs, one part of the mol. is designed to interact noncovalently with the NC hydrophobic pocket, while the second portion is designed to interact with the N-terminal domain of NC. This binding hypothesis was verified by mol. dynamics simulations, while the linkage between these two pharmacophores was found to enhance antiretroviral activity both on the wild-type virus and on HIV-1 strains with resistance to currently licensed drugs. The two most interesting compounds, I and II, showed no cytotoxicity, thus becoming valuable leads for further investigations.
ACS Medicinal Chemistry Letters published new progress about Anti-HIV agents. 20099-90-5 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO3, Application In Synthesis of 20099-90-5.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary