Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595028 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wild-type as well as drug-resistant mutant viruses. Notably, the series retains potency against the K103Â N/Y181C and Y188L mutants, among others. Thus, the N-benzyl compound 5k has a particularly attractive profile. Synthesis and SAR are presented and discussed, as well as crystal structures relating to the binding motifs.
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Authors
Denis J. Kertesz, Christine Brotherton-Pleiss, Minmin Yang, Zhanguo Wang, Xianfeng Lin, Zongxing Qiu, Donald R. Hirschfeld, Shelley Gleason, Taraneh Mirzadegan, Pete W. Dunten, Seth F. Harris, Armando G. Villaseñor, Julie Qi Hang, Gabrielle M. Heilek,