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KMID : 0606920060140040220
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Biomolecules & Therapeutics
2006 Volume.14 No. 4 p.220 ~ p.225
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β-Lactamase Inhibitory Activities of New 6-tricyclic Substituted Exomethylene Penam Sulfones
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Lee Su-Jin
Kim Hyun-Jin
Sheen Yhun-Y.
Lee Kwan-Soon
Park Choo Hea-Young
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Abstract
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Derivatives of penicillanic acid sulfones are known to be irreversible inhibitors of β-lactamase. Eight 6-tricyclic methylene penicillanic acid sulfones were prepared. and their β-lactamase inhibitory activities were evaluated against β-lactamase types Ⅰ, Ⅱ, Ⅲ and Ⅳ. Among the tricycles attached to 6-exomethylenepenam sul- fones, thiazolobenzimidazole (12a-12b), fluorene (12c), and carbazole (12e), showed inhibitory activity on type Ⅰ, Ⅱ and Ⅲ β-lactamase. But phenanthrene (12d), and anthracene (12f-12h) derivatives showed little β-lactamase inhibitory activity. The synergic effects of the selected compound (12b) in 1:4 combination with piperacillin showed some protection to piperacillin for the resistant strains of E. coli DC2 and P. aeruginosa 1771.
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KEYWORD
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β-Lactamase Inhibitor, 6-exomethylenepenam, Penam sulfones
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