Difluoromethylbenzoxazole pyrimidine thioether derivatives: a novel class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors

…, J Guillemont, J Unge, D Jochmans

文献索引：Boyer, Jeremie; Arnoult, Eric; Medebielle, Maurice; Guillemont, Jerome; Unge, Johan; Jochmans, Dirk Journal of Medicinal Chemistry, 2011 , vol. 54, # 23 p. 7974 - 7985

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被引用次数: 26

摘要

This paper reports the synthesis and antiviral properties of new difluoromethylbenzoxazole (DFMB) pyrimidine thioether derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. By use of a combination of structural biology study and traditional medicinal chemistry, several members of this novel class were synthesized using a single electron transfer chain process (radical nucleophilic substitution, SRN1) and were found to be ...