4.3 Article

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

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JOURNAL OF FLUORINE CHEMISTRY
卷 126, 期 4, 页码 535-542

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ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2004.12.016

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HIV; benzoxazole; 1,2,4-oxadiazole; difluoromethyl heterocycles; fluorination; dehydroxylation; oxidation

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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. (c) 2005 Elsevier B.V. All rights reserved.

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