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Synthesis, In Vitro Antimycobacterial Activity of Some 2-((5-Amino-1,3,4-Thiadiazol-2-YL)Methyl)-6-Aryl-Tetrahydropyridazin-3-One Derivatives

  • Mamdouh Allahyani,
  • Abdulaziz Alsharif,
  • Mazen Almehmadi,
  • Shivani Verma,
  • Mohammad Asif

摘要

A series of 2-((5-amino-1,3,4-thiadiazol-2-yl)methyl)-6-aryl-2,3,4,5-tetrahydro-pyridazin-3-one (4a-e) was synthesized and evaluated for its in vitro antimycobacterial activity. All the synthesized compounds were structurally confirmed by using physicochemical and spectral analysis such as melting point, Rf value, elemental analysis, IR, NMR and mass spectra. In vitro antimycobacterial activity was screened by the microplate Alamar Blue Assay (MABA) method against Mycobacterium tuberculosis H37Rv strain. Derivatives with 4-ethyl phenyl substitution (4b) and chloro phenyl substitution (4e) at the p-position of pyridazinone nuclei showed good antimycobacterial activity with a MIC value of 6.25 μg/ml compared to other aryl substitutions such as 4-methoxy phenyl (4a), 4-methyl phenyl (4c) with a MIC value of 25 and 12.5 μg/ml. The results of in vitro antimycobacterial activity revealed that the synthesized compounds have potential antimycobacterial action and can be further optimized and developed as lead compounds.