66122-36-9Relevant academic research and scientific papers
Synthesis and antitubercular activity of pyridazinone derivatives
Husain, Asif,Ahmad, Aftab,Bhandari, Anil,Ram, Veerma
experimental part, p. 778 - 780 (2012/03/26)
Two series of pyridazinone derivatives (19-34) were synthesized and evaluated for antitubercular activities against Mycobacterium tuberculosis H37Rv strain. The results illustrated that among the synthesized compounds, compound 25, 5-(4-hydroxy-3-methoxybenzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone emerged as a lead compound with good antitubercular activity. Four more compounds, (21, 22, 29 & 33) were significant in their antitubercular action.
Synthesis and biological evaluation of some new pyridazinone derivatives
Husain, Asif,Drabu, Sushma,Kumar, Nitin,Alam, M. Mumtaz,Ahmad, Aftab
experimental part, p. 742 - 748 (2012/04/04)
A series of pyridazinone derivatives (1934) were synthesized with an aim to synthesize safer anti-inflammatory agents. The compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation (LPO) actions. The percentage inhibition in edema at different time intervals indicated that compounds 20, 26, 28 and 34 exhibited good anti-inflammatory potential, comparable with that of ibuprofen (85.77%) within a range of 67.4877.23%. The results illustrate that 5-(4-fluoro-benzyl)-3-(4-chloro-phenyl) -1,6-dihydro-6-pyridazinone (26) and 5-(4-chloro-benzyl)-3-(4-chloro-phenyl)-1, 6-dihydro-6-pyridazinone (20) showed best anti-inflammatory activity. Furthermore, activity is more in case of chloro substitution as compared with methyl-substitution. The compounds synthesized were also evaluated for their ulcerogenic and LPO action and showed superior gastrointestinal safety profile along with reduction in LPO as compared with that of the ibuprofen.
Synthesis of some pyridazinylacetic acid derivatives as a novel class of monoamine oxidase-A inhibitors
Khattab, Sherine Nabil,Bekhit, Adnan Ahmed,El-Faham, Ayman,El Massry, Abdel Moneim,Amer, Adel
experimental part, p. 1717 - 1721 (2009/12/01)
A series of new pyridazinylacetic acid derivatives were synthesized and have been investigated for their ability to inhibit the activity of the A and B isoforms of monoamine oxidase (MAO). All compounds were found to be more selective to the MAO-A isoform with compound 5d having the highest SI values. Computational study performed with a docking technique indicated the potential of these compounds in pyridazine-based MAO-A inhibitor drug development.
