دورية
Synthesis and Preliminary Biological Evaluation of 3'-Substituted Cephem Sulfones as Potential β-Lactamase Inhibitors
العنوان: | Synthesis and Preliminary Biological Evaluation of 3'-Substituted Cephem Sulfones as Potential β-Lactamase Inhibitors |
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المؤلفون: | De Angelis, Francesco, Attorrese, Giuseppe, Cavicchio, Giancarlo, Ciampa, Sabatino, Di Tullio, Alessandra, Fattori, Daniela, Nicoletti, Rosario, Domenici, Enrico |
المصدر: | European Journal of Organic Chemistry; August 2001, Vol. 2001 Issue: 16 p3075-3081, 7p |
مستخلص: | 3'-Substituted cephem sulfones, as well as the unsubstituted congener, were synthesized and biologically evaluated as β-lactamase inhibitors. Sodium 3'-substituted cephalosporanate sulfones 4 and 5 were prepared starting from 7-aminodeacetoxycephalosporanic acid (7-ADCA, 6) by a bromodeamination reaction, followed by reduction of the 7-halo derivative. Selective, radical bromination at C-3' on the Δ3-isomer, followed by nucleophilic substitution and then retroisomerization at Δ2, afforded the required derivatives. 3'-Unsubstituted and 3'-acetoxycephem sulfones 2 and 3 were prepared using routine chemistry. The 3'-substituted cephem sulfone derivatives, evaluated as β-lactamase inhibitors by IC |
قاعدة البيانات: | Supplemental Index |
تدمد: | 1434193X 10990690 |
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DOI: | 10.1002/1099-0690(200108)2001:16<3075::AID-EJOC3075>3.0.CO;2-A |