Structure-activity relationships for six ketolide antibiotics.

摘要: Six structurally related 3-keto-substituted macrolide antibiotics (ketolides) were compared for concentration-dependent inhibitory effects on growth rate, viable cell number, and protein synthesis rates in Staphylococcus aureus cells. Inhibitory 50S ribosomal subunit formation also examined, as this is a second target these antibiotics. A concentration range of 0.01 to 0.1 μg/ml was tested. An IC50 inhibition translation measured each compound, relate structural features activity. ABT-773 the most effective six compounds tested with an IC50= 0.035 μg/ml. HMR 3004 almost 0.05 Two 2-fluoroketolides (HMR 3562 3787) equivalent their activity 0.06 Telithromycin 3647) had 0.08 μg/ml, 3832 least 0.11 Each antibiotic effect formation. These results indicate specific antimicrobial agents, which contribute defined activities against susceptible organisms.