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Syntheses of new difluoromethylene benzoxazole and 1,2,4-oxadiazole derivatives, as potent non-nucleoside HIV-1 reverse transcriptase inhibitors |
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| Authors: | Maurice Medebielle Samia Ait-Mohand William R. Dolbier Jr. Anne-Marie Aubertin |
| Affiliation: | a Université Denis Diderot Paris 7, Laboratoire d’Electrochimie Moléculaire, UMR CNRS 7591, 2 place Jussieu, 75251 Paris Cedex 05, France b Université Claude Bernard Lyon 1, Laboratoire SERCOF, UMR CNRS 5181, 43 bd du 11 Novembre 1918, 69622 Villeurbanne Cedex, France c University of Florida, Department of Chemistry, P.O. Box 117200, Gainesville, FL 32611-7200, USA d Université Louis Pasteur, EA 3770, Institutde Virologie, 3 Rue Koeberle, 67000 Strasbourg, France |
| Abstract: | 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. |
| Keywords: | HIV Benzoxazole 1,2,4-Oxadiazole Difluoromethyl heterocycles Fluorination Dehydroxylation Oxidation |
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