Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

作者：Monforte Anna Maria^*; Logoteta Patrizia; De Luca Laura; Iraci Nunzio; Ferro Stefania; Maga Giovanni; De Clercq Erik; Pannecouque Christophe; Chimirri Alba

来源：Bioorganic & Medicinal Chemistry, 2010, 18(4): 1702-1710.

DOI：10.1016/j.bmc.2009.12.059

• 1,3-Dihydro-benzimidazol-2-ones
• HIV-1 reverse transcriptase
• Molecular modeling
• Synthesis

A series of novel benzimidazolones and their analogues, characterized by the presence of one or more methyl groups or other bioisosteric moieties at different positions of the phenyl ring at N-1, were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Most of the new compounds proved to be highly effective in inhibiting both HIV-1 replication in MT4 cells with minimal cytotoxicity and RT enzyme at nanomolar concentrations. Some derivatives were also tested against RTs containing single amino acid mutations responsible for resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs). The different potencies displayed by the new compounds were studied using molecular modeling.

• 出版日期2010-2-15
• 单位河北医科大学