Article
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
Bioorganic & medicinal chemistry letters - 15 Jul 2010
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, Villaseñor Armando G, Hang Julie Qi, Heilek Gabrielle M, Klumpp Klaus
Abstract excerpt
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 K103N/Y181C and Y188L mutants, among others. Thus, the N-benzyl compound 5k has a particularly attractive profile....
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