1881281-01-1

PTC-847 (PTC847) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.1 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-847 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-847 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-847 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-847 showed 93% inhibition aginst Ng RNR activity at 4 uM, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.