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Bioorg Med Chem Lett. 2010 Oct 15;20(20):6020-3. doi: 10.1016/j.bmcl.2010.08.068. Epub 2010 Aug 19.

Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.

Author information

1
Roche R&D Center China, Shanghai, China. gordon.tang@roche.com

Abstract

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.

PMID:
20829038
DOI:
10.1016/j.bmcl.2010.08.068
[Indexed for MEDLINE]

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