Multi-target Control of Staphylococcus and Enterococcus

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: 1 R43 AI36741-1,
Agency Tracking Number: 24798
Amount: $75,000.00
Phase: Phase I
Program: SBIR
Awards Year: 1994
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
Metagene Corp.
One Progress Blvd, Box 26, Alachua, FL, 32615
DUNS: N/A
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Randy Fischer
 (904) 462-3904
Business Contact
Phone: () -
Research Institution
N/A
Abstract
No class of antibiotic is completely effective against infections caused by species ofStaphylococcus and Enterococcus. Increasing incidence of multiple drug resistance among thestaphylococci and enterococci, as well as escalating nosocomial infection rates, complicates treatmentof severe infections. New antimicrobials are urgently needed. These pathogens possess a novel patternfor control of aromatic amino acid biosynthesis whereby multiple enzyme targets are potentiallyvulnerable to attack by a single compound. Prospects for selective action against the pathogen and notthe host are excellent since analogs of pathway intermediates that are absent in mammals will besynthesized analog structures will be sought which cause false feedback inhibition at the early-pathwaylevel in addition to causing competitive inhibition of substrate- depleted mid-pathway enzymes.Chemical design of inhibitors will be oriented to objectives of optimizing stability, transport, andobtaining compounds exhibiting a range of single and multiple-target effects. Effective classes of in vitroenzyme inhibitors identified in Phase I will be optimized in Phase II and then tested in vivo forantimicrobial efficacy.

* information listed above is at the time of submission.

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