Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses PMID: 20829038

ADC Targets in Oncology

2026-04-10

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

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.