5,5,6-Fused tricycles bearing imidazole and pyrazole 6-methylidene penems as broad-spectrum inhibitors of β-lactamases

Bioorganic & Medicinal Chemistry
2008.0

Abstract

Beta-lactamases are serine- and metal-dependent hydrolases, produced by the bacteria as defense against beta-lactam antibiotics. Commercially available inhibitors such as clavulanic acid, sulbactam, and tazobactam, which are currently used in the hospital settings, have reduced activity against newly emerging beta-lactamases. Bacterial production of diverse beta-lactamases including class-A, class-C, and ESBLs has motivated several research groups to search for inhibitors with a broader spectrum of activity. Previously, several novel 6-methylidene penems bearing, [5,5] [5,6] and [5,5,5] heterocycles have been synthesized in our laboratory and were shown to be potent and broad-spectrum beta-lactamase inhibitors. As a continuation of our previous work and in order to extend the structure-activity relationships, in this paper, we describe herein the synthesis and in vitro, in vivo activities of several novel 5,5,6-fused tricyclic heterocycles attached to the 6-methylidene penem core. The compounds presented in the current paper are potent and broad-spectrum inhibitors of the TEM-1 and AmpC beta-lactamases. In combination with piperacillin, their in vitro activities showed enhanced susceptibility to class A- and C-resistant strains studied in various bacteria. Some of the newly synthesized compounds such as 12a-c were shown to have in vivo activity in the acute lethal infection model against TEM-1 producing organisms. The 5,5,6-fused heterocyclic ring cores such as 21, 25, and 35 reported here are hitherto unknown in the literature.

Knowledge Graph

Similar Paper

5,5,6-Fused tricycles bearing imidazole and pyrazole 6-methylidene penems as broad-spectrum inhibitors of β-lactamases
Bioorganic & Medicinal Chemistry 2008.0
Structure-Activity Relationship of 6-Methylidene Penems Bearing 6,5 Bicyclic Heterocycles as Broad-Spectrum β-Lactamase Inhibitors:  Evidence for 1,4-Thiazepine Intermediates with C7 R Stereochemistry by Computational Methods
Journal of Medicinal Chemistry 2006.0
6-(1-Hydroxyalkyl)penam sulfone derivatives as inhibitors of class A and class C β-lactamases II
Bioorganic & Medicinal Chemistry Letters 1999.0
Penicillin-derived inhibitors that simultaneously target both metallo- and serine-β-lactamases
Bioorganic & Medicinal Chemistry Letters 2004.0
6-(1-hydroxyalkyl)penam sulfone derivatives as inhibitors of class a and class C β-lactamases I
Bioorganic & Medicinal Chemistry Letters 1999.0
Studies on penam sulfones III. Synthesis and β-lactamase inhibitory activity of sodium (6R)-6-(α-hydroxybenzyl)-2β-methoxyiminomethyl-2α-methylpenam-3α-carboxylate 1,1-dioxide and sodium 2β-acyl-2α-methylpenam-3α-carboxylate 1,1-dioxide
Bioorganic & Medicinal Chemistry Letters 1997.0
Synthesis and .beta.-lactamase inhibitory properties of 2.beta.-[(acyloxy)methyl]-2.alpha.-methylpenam-3.alpha.-carboxylic acid 1,1-dioxides
Journal of Medicinal Chemistry 1985.0
The synthesis and lactamase inhibitory activity of 6-(carboxymethylene)penicillins and 7-(carboxymethylene)cephalosporins
Bioorganic & Medicinal Chemistry Letters 1995.0
In Vitro Activity of LK-157, a Novel Tricyclic Carbapenem As Broad-Spectrum β-Lactamase Inhibitor
Antimicrobial Agents and Chemotherapy 2009.0
The synthesis and evaluation of 6-alkylidene-2'β-substituted penam sulfones as β-lactamase inhibitors
Bioorganic & Medicinal Chemistry Letters 1999.0