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

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

  • Bioorg Med Chem Lett. 2010 Oct 15;20(20):6020-3. doi: 10.1016/j.bmcl.2010.08.068.
Guozhi Tang 1,  Denis J Kertesz,  Minmin Yang,  Xianfeng Lin,  Zhanguo Wang,  Wentao Li,  Zongxing Qiu,  Junli Chen,  Jianghua Mei,  Li Chen,  Taraneh Mirzadegan,  Seth F Harris,  Armando G Villaseñor,  Jennifer Fretland,  William L Fitch,  Julie Qi Hang,  Gabrielle Heilek,  Klaus Klumpp
Affiliations

Affiliation

  • 1 Roche R&D Center China, Shanghai, China. gordon.tang@roche.com
PMID: 20829038 DOI: 10.1016/j.bmcl.2010.08.068
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.

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