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What is New in Antimicrobials?

2006 Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC). What is New in Antimicrobials?. Drug - API-1252 Exclusively against Staphylococcus . Targets bacterial fatty acid synthesis “Exceptionally active” against MRSA

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What is New in Antimicrobials?

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  1. 2006 Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC)

  2. What is New in Antimicrobials? Drug - API-1252 • Exclusively against Staphylococcus. • Targets bacterial fatty acid synthesis • “Exceptionally active” against MRSA • Administered orally or IV (in mice) • Narrow Spectrum = “no off-target killing” • Human trials in 2007

  3. More against Staph Drug - PZ-601 • A Carbapenum drug • Active against drug-resistant gram (+) and some gram(-) bacteria. • Bactericidal against MRSA • Not active against PA, unless used in conjunction with aminoglycosides

  4. Against Gram(-) Drug – LN-1-255 • A penicillin-derived sulfone • Resembles the substrate of serine beta lactamase

  5. Against Streptococcus Drug – AR-709 • A diaminopyrimidine • Narrow spectrum • Inhibits dihydrofloate reductase (like trimethroprim) • Advantages over Trimethorpin are: • Better antimicrobial and bactericidal activity • A “low propensity “ to develop resistance

  6. Against Staph? • Drug – Hygromycin –A • An inhibitor of protein synthesis • Against gram(+) including MRSA • Similar to Linezolid an oxazolidinone antibiotic (Pfizer’s trade name Zyvox)

  7. Against Mycobacterium Drug – DC-159a • An 8-methoxy derivative of fluroquinoline • Orally available • Broad Spectrum - gram (+) and (gram (-) • Active against M. tuberculosis and its multiple drug resistant isolates

  8. Propionibacteria acnes Drug – BAL 19403 • A macrolide antibiotic • Antibacterial and anti-inflammatory • “wide safety margin” • Little systemic absorption • Strong candidate for topical treatment of acne

  9. Hepatitis –C Virus • Drug – HCV-796 • A selective, non-nucleoside inhibitor • A modified benzofuran • “Very Potent” against HCV in mammalian cells • Advances to Phase II clinical trials

  10. Natural Antimicrobial Peptides • Part of the Host defense system • Broad ability to kill microbes • Large peptides (over 100 a.a) are often lytic, nutrient binding proteins or specifically target microbial macromolecules • Small peptides disrupt the structure or function of microbial cell membranes • Found in epithelial cells, phagocytes and body fluids • They are endogenous antibiotics • Help in inflammation, wound repair and regulation of the adaptive immune system

  11. Ceraginins • Intriguing class of membrane-active mimics of antimicrobial peptides • Broad spectrum • Rapid in killing action • Very potent • Topical application to control eye infections • Useful to prevent biofilm contamination from catheters

  12. Antimicrobial Peptides • Cationic peptides- plants, insects& others • Disrupt plasma membrane integrity • Megainin –from skin of frogs • Squalamine – from spiny dogfish shark • Protegrins – from pigs

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