期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 5, 页码 1854-1868出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01336
关键词
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资金
- University of Antwerp (IOF POC project)
- Hercules Foundation
- NSF [0087210]
- Ohio Board of Regents [CAP-491]
- Youngstown State University
New non-nucleoside reverse transcriptase inhibitors (NNRTI), which are similar in structure to earlier described di(arylamino)pyrimidines but featuring a 2,6-di(arylamino)-3-fluoropyridine, 2,4-di(arylamino)-5-fluoropyrimidine, or 1,3-di(arylamino)-4-fluorobenzene moiety instead of a 2,4-disubstituted pyrimidine moiety, are reported. The short and practical synthesis of novel NNRTI relies on two sequential Pd-catalyzed aminations as the key steps. It is demonstrated through direct comparison with reference compounds that the presence of a fluorine atom increases the in vitro anti-HIV activity, both against the wild type virus and drug-resistant mutant strains.
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