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J-110,441, a Potent beta-Lactamase Inhibitor with Broad Spectrum Including Class B and Class C beta-Lactamases.

NAGANO R, YAMADA K, SUGIMOTO Y, IMAMURA H, HASHIZUME T, MORISHIMA H; Interscience Conference on Antimicrobial Agents and Chemotherapy.

Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 1999 Sep 26-29; 39: 299 (abstract no. 402).

Tsukuba Res. Inst. Banyu Pharmaceutical, Tsukuba, JAPAN.

Clinically available beta-lactamase inhibitors are known to be useful for potentiating beta-lactam antibiotics against Class A beta-lactamase producers, while efforts have been continued to obtain a potent inhibitor of Class B and Class C beta-lactamases. Carbapenem-derived J-110,441, which has benzothienylthio moiety on C-2 position of 1beta-methylcarbapenem nucleus and very weak anti-gram-negative activity, was identified as a potent inhibitor of IMP-1 beta-lactamase, a transferable Class B metallo-beta-lactamase. Interestingly, J-110,441 inhibited various Class B metallo-beta-lactamases such as IMP-1 coded on the transferable bla[IMP] gene, CcrA from Bacteroides fragilis, and L-1 from Stenotrophomonas maltophilia with K[i] values of 0.0037micro-M, 0.24micro-M, and 1.02micro-M, respectively. Further studies showed that J-110,441 inhibited plasmidic TEM type Class A serine-beta-lactamase and chromosomal Class C serine-beta-lactamase from Enterobacter cloacae with K[i] values of 1.02 micro-M and 0.0062 micro-M, respectively. In the whole cell susceptibility testing, the MICs of imipenem for IMP-1-producing clinical isolates were reduced in combination with J-110,441. Similarly, ceftazidime-resistance caused by high expression of chromosomal Class C beta-lactamase was sensitized in the presence of J-110,441. In this paper, we will describe the interaction of J-110,441 with various beta-lactamases including Class B and Class C beta-lactamases and examine its capacity to achieve a possible new type of beta-lactamase inhibitor. [table: see text]

Publication Types:
  • Meeting Abstracts
  • Bacteroides fragilis
  • Carbapenems
  • Ceftazidime
  • Cesium
  • Enterobacter cloacae
  • Enzyme Inhibitors
  • Imipenem
  • Microbial Sensitivity Tests
  • Monobactams
  • beta-Lactamases
  • classification
Other ID:
  • GWAIDS0009154
UI: 102246651

From Meeting Abstracts

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