1221884-27-0Relevant articles and documents
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Monforte, Anna-Maria,Logoteta, Patrizia,Luca, Laura De,Iraci, Nunzio,Ferro, Stefania,Maga, Giovanni,De Clercq, Erik,Pannecouque, Christophe,Chimirri, Alba
experimental part, p. 1702 - 1710 (2010/05/02)
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.