Synthesis and Antitubercular Activity of Pyridazinone Derivatives

Husain, Asif; Ahmad, Aftab; Bhandari, Anil; Ram, Veerma

doi:10.4067/s0717-97072011000300013

Cited by 34 publications

(17 citation statements)

References 9 publications

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“…Compounds 2c and 2d showed MIC value of 25 μg/mL and compounds 3c and 3g showed MIC value of 25 μg/mL. [36] Some pyridazinone or phthalazinone compounds (4a-e, 5a-e, and 6a-e) were active against M. tuberculosis H37Rv. Compounds 4e and 5b showed 92.56% and 97.97% resistance, respectively.…”

Section: Chronicles Of Young Scientistsmentioning

confidence: 99%

“…Four more compounds, (2c, 2d, 3c, 3g, 21, 22, 29, and 33) were significant in their anti-TB action. [36] Some 3(2H)-pyridazinone and 1(2H)-phthalazinone derivatives (4a-e, 5a-e and 6a-e) were evaluated for their anti-TB activity against M. tuberculosis H37Rv [ Table 3]. The results showed [ Table 3] that compound 6e had the highest antimycobacterial activity.…”

Section: Chronicles Of Young Scientistsmentioning

confidence: 99%

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Development of structurally diverse antitubercular molecules with pyridazine ring

2013

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There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberculosis because mycobacterium species have developed resistance against currently used drugs, their toxic effect, and longer duration of therapy. The pyridazine derivatives are an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding in the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against multidrug-resistant, extensively drug-resistant mycobacterium strains, and also in patient co-infected with HIV/AIDS.

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Section: Chronicles Of Young Scientistsmentioning

confidence: 99%

Section: Chronicles Of Young Scientistsmentioning

confidence: 99%

Development of structurally diverse antitubercular molecules with pyridazine ring

2013

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“…Compounds 2e showed maxium MIC value 12.5 μg/mL and compound 2e showed lowest MIC value 100 μg/mL. Compounds 2c and 2d showed MIC value 25 μg/mL and compounds 3c and 3g showed MIC value 25 μg/mL [10]. Some pyridazinone or phthalazinone compounds (4a-e, 5a-e and 6a-e) were showed active against Mtb H37Rv.…”

mentioning

confidence: 97%

“…The compound 2g, 5-(4-hydroxy-3-methoxybenzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone emerged as a lead compound with good anti-TB activity. Four more compounds, (2c, 2d, 3c, 3g 21, 22, 29 and 33) were significant in their anti-TB action [10]. Some 3(2H)-pyridazinone and 1(2H)-phthalazinone derivatives (4a-e, 5a-e and 6a-e) were evaluated for their anti-TB activity against Mtb H37Rv at 20 μg/mL concentration.…”

Section: Compounds 1a-lmentioning

confidence: 99%

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Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Asif¹

2012

Med chem

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There has been considerable interest in the development of new molecule with antibacterial activities particularly against tuberclosis because mycobacterium species have developed resistant against currently used drugs, their toxic effect and long duration of therapy. The diazine (pyridazine, pyrimidine and piperazine) derivatives possess an important class of compound for new drugs research and development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their antitubercular activity. These observations have been guiding for the development of new molecules that possess potent antitubercular activity with minimum side effects or effective against MDR, XDR mycobacterium strains, and also in patient co-infected with HIV/AIDS.

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Optimization of 4‐amino‐pyridazin‐3(2H)‐one as a valid core scaffold for FABP4 inhibitors

Floresta

Crocetti

Silva

et al. 2023

Archiv der Pharmazie

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Current clinical research suggests that fatty acid‐binding protein 4 inhibitors (FABP4is), which are of biological and therapeutic interest, may show potential in treating cancer and other illnesses. We sought to uncover new structures through the optimization of the previously reported 4‐amino and 4‐ureido pyridazinone‐based series of FABP4is as part of a larger research effort to create more potent FABP4 inhibitors. This led to the identification of 14e as the most potent analog with IC50 = 1.57 μM, which is lower than the IC50 of the positive control. Advanced modeling investigations and in silico absorption, distribution, metabolism, and excretion ‐ toxicity calculations suggested that 14e represents a potential candidate for in vivo studies such as FABP4i.

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Synthesis and Antitubercular Activity of Pyridazinone Derivatives

Cited by 34 publications

References 9 publications

Development of structurally diverse antitubercular molecules with pyridazine ring

Development of structurally diverse antitubercular molecules with pyridazine ring

Recent Efforts for the Development of Antitubercular Drug Containing Diazine Ring

Optimization of 4‐amino‐pyridazin‐3(2H)‐one as a valid core scaffold for FABP4 inhibitors

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