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Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses. 2010
Guozhi Tang, and
Denis J Kertesz, and
Minmin Yang, and
Xianfeng Lin, and
Zhanguo Wang, and
Wentao Li, and
Zongxing Qiu, and
Junli Chen, and
Jianghua Mei, and
Li Chen, and
Taraneh Mirzadegan, and
Seth F Harris, and
Armando G Villaseñor, and
Jennifer Fretland, and
William L Fitch, and
Julie Qi Hang, and
Gabrielle Heilek, and
Klaus Klumpp
Roche R&D Center China, Shanghai, China. gordon.tang@roche.com
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.
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