3. International Health Sciences and Innovation, Ankara, Turkey, 12 - 13 January 2021, vol.0, no.0, pp.122-123
Mycobacterium tuberculosis (Mtb) is the organism that causes Tuberculosis (TB), which is
among the diseases with the highest mortality rate worldwide. Globally, 2.0 million new and
relapse TB cases were identified by a WHO-recommended rapid diagnostic test in 2019.
Therefore, developing new active agents to combat TB is an urgent need.
4,5-Dihydropyridazin-3(2H)-one derivatives have been extensively investigated for their
potential as anti-TB drug candidates. In the light of this consideration and our previous study,
we designed and synthesized some new 6-methyl-4,5-dihydropyridazin-3(2H)-ones,
investigated their antimycobacterial activities.
4-Thiazolidinone and 1,3,4-oxadiazole derivatives were obtained by the cyclization of 2,4-
dichlorophenyl substituted hydrazone derivative with thioacetic acid and acetic anhydride,
respectively (Figure). In vitro antimycobacterial activity assays of the synthesized
compounds were carried out using the by agar dilution method against M. tuberculosis H37Rv.
yl)acetohydrazide derivatives, N-(2-(2,4-dichlorophenyl)-4-oxothiazolidin-3-yl)-2-(3-methyl-
6-oxo-5,6-dihydropyridazin-1(4H)-yl)acetamide and 2-((4-acetyl-5-(2,4-dichlorophenyl)-4,5-
synthesized (Figure). The structures of the target compounds were elucidated by IR, 1HNMR,
and mass spectrometry.
According to the antimycobacterial activity results, our lead compound (2,4-dichlorophenyl
substituted N-acylhydrazone derivative) is still the most active compound among the designed
compounds against M. tuberculosis H37Rv.
The results suggested that some of N'-(substitutedbenzylidene)-2-(3-methyl-6-oxo-5,6-
dihydropyridazin-1(4H)-yl)acetohydrazide derivatives could be potential antimycobacterial
agents against TB.
We thank to Dharmarajan Sriram and Perumal Yogeeswari for antimycobacterial activity
studies. This study was funded by Scientific Research Projects Coordination Unit of
Hacettepe University (Grant number: 0801301003).
Keywords: Antimycobacterial activity, tuberculosis, pharmaceutical chemistry