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

…, J Chen, J Mei, L Chen, T Mirzadegan, SF Harris…

Index: 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.; Villasenor, Armando G.; Fretland, Jennifer; Fitch, William L.; Hang, Julie Qi; Heilek, Gabrielle; Klumpp, Klaus Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 20 p. 6020 - 6023

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Citation Number: 21

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, ...