Ferro, Stefania; Buemi, Maria Rosa; De Luca, Laura; Agharbaoui, Fatima E.; Pannecouque, Christophe; Monforte, Anna-Maria published the artcile< Searching for novel N1-substituted benzimidazol-2-ones as non-nucleoside HIV-1 RT inhibitors>, Product Details of C8H8BrCl, the main research area is benzimidazolone synthesis HIV1 reverse transcriptase inhibitor; Benzimidazolones; Design; RTs mutant; Reverse transcriptase inhibitors; Synthesis.
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) represent an integral part of the currently available combination antiretroviral therapy (cART) contributing to reduce the AIDS-mortality and turned the disease from lethal to chronic. In this context we recently reported a series of 6-chloro-1-(3-methylphenylsulfonyl)-1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. In this paper, we describe the design and the synthesis of two novel series of benzimidazolone analogs in which the linker moiety between the Ph ring and the sulfonyl group was modified and new small lipophilic groups on the benzyl sulfonyl pendant were introduced. All the new obtained compounds were evaluated as RT inhibitors and were also tested against RTs containing single amino acid mutations. Finally, mol. docking studies were performed in order to rationalize the observed activity of the most promising compound
Bioorganic & Medicinal Chemistry published new progress about Anti-HIV agents. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, Product Details of C8H8BrCl.
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