GE Y, TOUAMI S, CRITCHLEY I, TAYLOR M, BAIRD E, BURLI R, PENNELL A, MOSER H; Interscience Conference on Antimicrobial Agents and Chemotherapy (41st : 2001 : Chicago, Ill.).
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2001 Dec 16-19; 41: abstract no. F-1687.
Genesoft Inc, South San Francisco, CA
GSQ 1530 is a compound derived from a newly identified antibiotic class referred to as HARPs (Hetero ARomatic Polycycles). The aim of this study is to assess in vitro antimicrobial activity of GSQ1530. Using a NCCLS broth microdilution assay, GSQ1530 was co-evaluated with other antibiotics against 241 clinical isolates. The MIC[90] of GSQ 1530 against Methicillin-susceptible Staphylococcus aureus and MRSA were 2 microg/ml and 4 microg/ml, respectively. Ninety percent of streptococci were inhibited by GSQ1530 at the concentration of 2 microg/ml or less regardless of their susceptibility to other antibiotics. The MIC[90] against enterococci (including VRE) was 4 microg/ml. No cross-resistance was found between GSQ1530 and other known antibiotics. GSQ 1530 had poor activity against wild-type Gram-negative bacteria. However, GSQ 1530 had excellent activity against a drug-permeable Escherichia coli mutant (MIC = 0.5 microg/ml). The MBC test was conducted for 73 clinical isolates; GSQ1530 was cidal against streptococci and staphylococci, but static against enterococci. Thein vitro killing kinetic study revealed at least three log reduction of bacterial growth within 6 hr after exposure to 4 X MICs of GSQ1530 for both S. aureus and Streptococcus pneumoniae. The in vitro killing kinetics of GSQ1530 against the same two species was time-dependent. The checkerboard study showed that GSQ1530 had no synergistic or antagonistic effect on other class-representative antibiotics. The preliminary results demonstrate that GSQ1530, a representative compound of our novel antibiotic HARPs, has broad-spectrum anti-Gram positive bacteria activity. Ongoing in vivo studies will support further development of HARPs as agents for the treatment of the infectious disease caused by Gram-positive bacteria.
Publication Types:
Keywords:
- Anti-Bacterial Agents
- Carrier Proteins
- Cytokines
- Enterococcus
- GSQ1530
- Gram-Negative Bacteria
- Gram-Positive Bacteria
- In Vitro
- Microbial Sensitivity Tests
- Polycyclic Compounds
- Pyrroles
- Staphylococcus
- Staphylococcus aureus
- Streptococcus
- Streptococcus pneumoniae
- pleiotrophin
Other ID:
UI: 102269901
From Meeting Abstracts