标题：Novel fluorine-containing DAPY derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2014072419
作者：Meng, Qing; Liu, Na; Huang, Boshi; Zhan, Peng; Liu, Xinyong
作者机构：[Meng, Qing; Liu, Na; Huang, Boshi; Zhan, Peng; Liu, Xinyong] Shandong Univ, Sch Pharmaceut Sci, Key Lab Chem Biol, Minist Educ,Dept Med Chem, Jinan 2 更多
通讯作者地址：[Liu, XY]Shandong Univ, Sch Pharmaceut Sci, Key Lab Chem Biol, Minist Educ,Dept Med Chem, 44 West Culture Rd, Jinan 250012, Shandong, Peoples R China.
来源：EXPERT OPINION ON THERAPEUTIC PATENTS
关键词：diarylpyrimidines; drug design; fluorine atom; HIV inhibitors;; non-nucleoside reverse transcriptase inhibitors
摘要：Diarylpyrimidine (DAPY) derivatives, one family of HIV non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) with superior activities against wild-type (WT) HIV-1 and NNRTI-resistant strains, have attracted much attention in the past decade. A series of DAPY derivatives featuring a fluorine atom on the central ring were reported as novel NNRTIs in the patent WO2014072419. Some compounds exhibited robust potency against both WT and mutant strains, which were approximately equal to or higher than those of the reference drug TMC120. Moreover, it has become evident that fluorinated molecules have a remarkable record in many other potent NNRTIs. Thus, this survey provides a sampling of renowned fluorinated NNRTIs and their mode of action, with an analysis clarifying the functional roles and impact of fluorine substitution on antiviral potency. We envision that fluorinated NNRTIs will play a continuing role in affording anti-HIV drug candidates for therapeutic applications.