新型N1-取代的1,3-二氢-2H-苯并咪唑-2-酮作为有效的非核苷类逆转录酶抑制剂。
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
作者信息
Monforte Anna-Maria, Rao Angela, Logoteta Patrizia, Ferro Stefania, De Luca Laura, Barreca Maria Letizia, Iraci Nunzio, Maga Giovanni, De Clercq Erik, Pannecouque Christophe, Chimirri Alba
机构信息
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy.
出版信息
Bioorg Med Chem. 2008 Aug 1;16(15):7429-35. doi: 10.1016/j.bmc.2008.06.012. Epub 2008 Jun 13.
Several N(1)-substituted 1,3-dihydro-2H-benzimidazol-2-ones were synthesized and evaluated as anti-HIV agents. Some of them proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentration as potent non-nucleoside HIV-1 RT inhibitors (NNRTIs) with low cytotoxicity. SAR studies highlighted that the nature of the substituents at N(1) and on the benzene ring of benzimidazolone moiety significantly influenced the anti-HIV activity of this class of potent antiretroviral agents.
合成了几种N(1)-取代的1,3-二氢-2H-苯并咪唑-2-酮，并将其作为抗HIV药物进行评估。其中一些化合物被证明在纳摩尔浓度下作为有效的非核苷HIV-1逆转录酶抑制剂（NNRTIs）能高效抑制HIV-1复制，且细胞毒性低。构效关系研究表明，苯并咪唑酮部分N(1)位和苯环上取代基的性质对这类强效抗逆转录病毒药物的抗HIV活性有显著影响。
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