1303518-48-0Relevant articles and documents
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses
Tang, Guozhi,Kertesz, Denis J.,Yang, Minmin,Lin, Xianfeng,Wang, Zhanguo,Li, Wentao,Qiu, Zongxing,Chen, Junli,Mei, Jianghua,Chen, Li,Mirzadegan, Taraneh,Harris, Seth F.,Villase?or, Armando G.,Fretland, Jennifer,Fitch, William L.,Hang, Julie Qi,Heilek, Gabrielle,Klumpp, Klaus
scheme or table, p. 6020 - 6023 (2010/11/05)
Further investigation of the recently reported piperidine-4-yl- aminopyrimidine class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) has been carried out. Thus, preparation of a series of N-phenyl piperidine analogs resulted in the identification of 3-carboxamides as a particularly active series. Analogs such as 28 and 40 are very potent versus wild-type HIV-1 and a broad range of NNRTI-resistant mutant viruses. Synthesis, structure-activity relationship (SAR), clearance data, and crystallographic evidence for the binding motif are discussed.
