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

UTKU S., Gokce M., ASLAN G., BAYRAM ABİHA G., ÜLGER M., EMEKDAŞ G., ...More

TURKISH JOURNAL OF CHEMISTRY, vol.35, no.2, pp.331-339, 2011 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 35 Issue: 2
  • Publication Date: 2011
  • Doi Number: 10.3906/kim-1009-63
  • Journal Name: TURKISH JOURNAL OF CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.331-339
  • Keywords: 3(2H)-Pyridazinone, acetophenone hydrazone, antimycobacterial activity, antitubercular drugs, ANTIINFLAMMATORY ACTIVITY, MULTIDRUG-RESISTANT, TUBERCULOSIS, DERIVATIVES, IMPACT
  • Gazi University Affiliated: Yes

Abstract

The difficulty in managing tuberculosis includes the prolonged duration of the treatment, the emergence of drug resistance, and coinfection with HIV/AIDS. Tuberculosis control requires new drugs that act on novel drug targets to help in combating resistant forms of Mycobacterium tuberculosis and reduce the treatment duration. For this purpose, 6-substituted-3(2H)-pyridazinone-2-acetyl-2-(substituted/nonsubstituted acetophenone) hydrazone derivatives were synthesized and their structures were elucidated by elemental analyses, IR, and H-1-NMR. The in vitro antimycobacterial activities of synthesized compounds 5a-l were determined by the agar proportion method against Mycobacterium tuberculosis H37Rv. Among the target compounds, 5b and 5f exhibited the best antimycobacterial activity, with a MIC value of 5 mu g/mL.