Syntheses of new difluoromethylene benzoxazole and 1,2,4-oxadiazole derivatives, as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

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• 作者：Maurice Medebielle ; Samia Ait-Moh ; Conrad Burkhloder ; William R. Dolbier Jr. ; Gé ; raldine Laumond ; Anne-Marie Aubertin
• 关键词：HIV ; Benzoxazole ; 1 ; 2 ; 4-Oxadiazole ; Difluoromethyl heterocycles ; Fluorination ; Dehydroxylation ; Oxidation
• 刊名：Journal of Fluorine Chemistry
• 出版年：2005
• 出版时间：April 2005
• 年：2005
• 卷：126
• 期：4
• 页码：533-540
• 全文大小：224 K

文摘

In an effort to prepare new fluorine-containing compounds, which are active against HIV, several chemical modifications of a series of benzoxazole and 1,2,4-oxadiazole-CF₂CHOHAr derivatives were carried out. The products (9–30) which all have one or two CF₂ groups were tested for activity against HIV-1; they were devoid of significant activity, one of them being cytotoxic.