The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
SYNTHESES AND BIOLOGICAL ACTIVITIES OF NEW PENEM DERIVATIVES WITH SIDE CHAINS DERIVED FROM 4-HYDROXYPROLINE
GERHARD EMMERPETER KNEUSSELJOHANNES HILDEBRANDTFRIEDERIKE TURNOWSKYALEXANDER HASELBERGERAXEL WENZELPETER STÜTZ
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1985 Volume 38 Issue 10 Pages 1371-1386

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Abstract

New penem derivatives with various substituted, enantiomerically pure pyrrolidine-thio side chains at the C-2 position were synthesized and their chemotherapeutic potentials assessed in comparison with Sch 29482. The following criteria were used for preliminary evaluation : Antibacterial activity in vitro, β-lactamase inhibition and apparent hydrolysis rates by crude murine and human kidney enzyme preparations. The most active compounds, 16e, 16f and 18 exhibit properties typical of this substance class with a tendency towards greater antibacterial potency in comparison with Sch 29482, especially against Pseudomonas aeruginosa. No clear-cut structure-activity relationships could be found with respect to β-lactamase inhibition and stability against degrading renal enzymes.

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© Japan Antibiotics Research Association
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