RNA-TARGETED ANTIMICOBIAL AGENTS

DESCRIPTION (provided by applicant): The problem of antibiotic resistance requires that new entities and targets be identified. Pinnacle Pharmaceutical's platform technology is in the area of RNA metabolism. Phase I studies have validated a novel, proprietary, high-throughput screening assay for one such target. A screen of 3200 plant extracts led to the identification of seven active principles, none of which had previously been shown to affect the assay target. This Phase II application proposes (1) continued high-throughput screening of compound libraries (2) continued verification of the molecular mechanism of lead compounds, (3) structural modification of one lead identified in Phase I and other lead compounds identified in Phase II, (4) characterization of key compounds for their spectrum of activity against clinically relevant target microorganisms, (5) initiation of preclinical characterization of optimized inhibitors, including determining their chemical stability and toxicological properties. Successful completion of this Phase II research will lead to the identification of a new class of anti-infective agents.