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

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-CF 2CHOHAr derivatives were carried out. The products ( 9– 30) which all have one or two CF 2 groups were tested for activity agains...

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Bibliographic Details
Published in:Journal of fluorine chemistry 2005-04, Vol.126 (4), p.533-540
Main Authors: Medebielle, Maurice, Ait-Mohand, Samia, Burkhloder, Conrad, Dolbier, William R., Laumond, Géraldine, Aubertin, Anne-Marie
Format: Article
Language:English
Subjects:
1,2,4-Oxadiazole
Benzoxazole
Dehydroxylation
Difluoromethyl heterocycles
Fluorination
HIV
Oxidation
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Summary: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-CF 2CHOHAr derivatives were carried out. The products ( 9– 30) which all have one or two CF 2 groups were tested for activity against HIV-1; they were devoid of significant activity, one of them being cytotoxic.
ISSN:0022-1139
1873-3328
DOI:10.1016/j.jfluchem.2004.12.016