Synthesis and in vitro antimycobacterial activities of novel 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/ nonsubstituted acetophenone) hydrazone

摘要

The difficulty in managing tuberculosis includes theprolonged duration of the treatment, the emergence of drug resistance,and coinfection with HIV/AIDS. Tuberculosis control requires new drugsthat act on novel drug targets to help in combating resistant forms ofMycobacterium tuberculosis and reduce the treatment duration. Forthis purpose, 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substitutedonsubstituted acetophenone) hydrazone derivatives weresynthesized and their structures were elucidated by elementalanalyses, IR, and ^1H-NMR. The in vitro antimycobacterial activitiesof synthesized compounds 5a-l were determined by the agar proportionmethod against Mycobacterium tuberculosis H37Rv. Among the targetcompounds, 5b and 5f exhibited the best antimycobacterial activity,with a MIC value of 5 mu g/mL.