Inactivation of beta-lactamase from Shigella flexneri UCSF-129 by BRL 42715, a potent inhibitor.

Abstract

The effect of a powerful inhibitor, BRL 42715, on beta-lactamase from Shigella flexneri UCSF-129, to overcome the problem of shigellosis and its resistance to ampicillin, was studied. The I50 was determined for BRL 42715 [C6-(N1-methyl-1,2,3 triazolylmethylene)penem] as 0.0049 microgram/ml being 20-fold lower than the best inhibitor, 6-beta-iodopenicillanic acid, previously reported. The MIC fell from 2,048 to 2 micrograms/ml in the presence of 1 microgram/ml of BRL 42715. The synergism of the ampicillin plus this inhibitor lasted for 9 h. BRL 42715 is an irreversible inhibitor, according to the dialysis results, and a substrate analogue.

• Authors: M Campos, G Bocaz, O Vasquez, H Gonzalez, J Caceres, C Yañez
• Journal: Microbios (Microbios) Vol. 74 Issue 298 Pg. 17-22 ( 1993) ISSN: 0026-2633 [Print] England
• PMID: 8336551 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Bacterial Agents
• Lactams
• beta-Lactamase Inhibitors
• beta-Lactams
• C6-(N1-methyl-1,2,3-trazolylmethylene)penem
• beta-Lactamases

Topics

• Ampicillin Resistance
• Anti-Bacterial Agents (pharmacology)
• Lactams
• Microbial Sensitivity Tests
• Shigella flexneri (enzymology)
• beta-Lactamase Inhibitors
• beta-Lactamases (metabolism)
• beta-Lactams