title: Novel fluorine-containing DAPY derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2014072419.
abstract: 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.
authors.affiliation: a Shandong University, School of Pharmaceutical Sciences, Key Laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry , 44, West Culture Road, 250012, Jinan, Shandong, P. R. China zhanpeng1982@sdu.edu.cn , xinyongl@sdu.edu.cn.
authors.forename: Qing
authors.initials: Q
authors.lastname: Meng
authors.affiliation: a Shandong University, School of Pharmaceutical Sciences, Key Laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry , 44, West Culture Road, 250012, Jinan, Shandong, P. R. China zhanpeng1982@sdu.edu.cn , xinyongl@sdu.edu.cn.
authors.forename: Na
authors.initials: N
authors.lastname: Liu
authors.affiliation: a Shandong University, School of Pharmaceutical Sciences, Key Laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry , 44, West Culture Road, 250012, Jinan, Shandong, P. R. China zhanpeng1982@sdu.edu.cn , xinyongl@sdu.edu.cn.
authors.forename: Boshi
authors.initials: B
authors.lastname: Huang
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.affiliation: a Shandong University, School of Pharmaceutical Sciences, Key Laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry , 44, West Culture Road, 250012, Jinan, Shandong, P. R. China zhanpeng1982@sdu.edu.cn , xinyongl@sdu.edu.cn.
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
mesh_terms: D015195:Drug Design; D024882:Drug Resistance, Viral; D005461:Fluorine / Q000737:chemistry; D015658:HIV Infections / Q000188:drug therapy* / Q000201:enzymology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D010330:Patents as Topic; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; D005461:Fluorine; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase
keywords: HIV inhibitors; diarylpyrimidines; drug design; fluorine atom; non-nucleoside reverse transcriptase inhibitors