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Year : 1998  |  Volume : 30  |  Issue : 2  |  Page : 63-67

2-Pyridones emerging as a most potent novel class of antimicrobial agents Possible future development in relation to fluoroquinolone-resistance

Correspondence Address:
Barar V Kiran

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Source of Support: None, Conflict of Interest: None

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Initial discovery of nalidixic acid (a naphthyridine) was followed by synthesis and development of related compounds like pyridopyrimidine, cinnoline and quinolones, etc. Many of them were marketed long before the molecular basis of their action was elucidated in terms of DNA gyrase inhibition. Among these, nalidixic acid and fluoroquinolones had the greatest success. Fluoroquinolones available for clinical use over the past 10 years are norfloxacin, pefloxacin, ciprofloxacin, ofloxacin, enoxacin and lomefloxacin. with the addition of promising congeners under clinical development such as sparfloxacin, levofloxacin, clinafloxacin, grepafloxacin (OPC-17116), trovafloxacin (CP-99,219) and Du6859a. 2-Pyridones are the most recent addition to this array of DNA gyrase inhibitors emerging as antimicrobial wonder drugs. They have structural similarities with fluoroquinolones as regards position of carbonyl and carboxyl groups, or fluorine in the core, but are distinct in having a nitrogen (N) atom located at one of the two junctions of the two six-membered rings.This position of 'N' possibly makes 2-pyridones, as agents having exceptional breadth of spectrum, with remarkable action against DNA gyrase and topoisomerase-IV enzymes. A compound designated ABT-719 (also A-86719.1), which is a 2-pyridone, has been tested (in vitro) for its considerable activity against many gram positive and anaerobic infections and has been compared with ciprofloxacin in isolates for a greater gram negative activity. It also has been found to be effective against several systemic infections and the most challenging and troublesome vancomycin-, methicillin- and ciprofloxacin-resistant pathogens. However, 2-pyridones are in Phase II and Phase III clinical development, the outcome of which is awaited.


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