1033951-50-6Relevant articles and documents
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses
Kertesz, Denis J.,Brotherton-Pleiss, Christine,Yang, Minmin,Wang, Zhanguo,Lin, Xianfeng,Qiu, Zongxing,Hirschfeld, Donald R.,Gleason, Shelley,Mirzadegan, Taraneh,Dunten, Pete W.,Harris, Seth F.,Villasenor, Armando G.,Hang, Julie Qi,Heilek, Gabrielle M.,Klumpp, Klaus
scheme or table, p. 4215 - 4218 (2010/08/22)
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 K103 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.
