Abstract
BackgroundSome novel substituted pyrazolone, pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidinone, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives have been reported to possess various pharmacological activities like antimicrobial, antitumor and anti-inflammatory.ResultsA novel series of azoles and azines were designed and prepared via reaction of 1,3-diphenyl-1H-pyrazol-5(4H)-one with some electrophilic and nucleophilic reagents. The structures of target compounds were confirmed by elemental analyses and spectral data.ConclusionsThe antimicrobial activity of the target synthesized compounds were tested against various microorganisms such as Escherichia coli; Bacillus megaterium; Bacillus subtilis (Bacterial species), Fusarium proliferatum; Trichoderma harzianum; Aspergillus niger (fungal species) by the disc diffusion method. In general, the novel synthesized compounds showed a good antimicrobial activity against the previously mentioned microorganisms.
Highlights
Some novel substituted pyrazolone, pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, pyrazolo[3,4d]thiazolo[3,2-a]pyrimidinone, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives have been reported to possess various pharmacological activities like antimicrobial, antitumor and anti-inflammatory
The compounds containing nitrogen are important category of heterocyclic compounds, which play a significant roles in modern pesticide industry (85% of pesticides with high activity and low toxicity contain nitrogen heterocyclic compound) [1]
Pyrazol-5-one derivative 2 was exploited as a key intermediate for the synthesis of hitherto unknown fused pyrazole
Summary
The research study reports the successful synthesis and antimicrobial activity of new pyrazolone, pyrazolopyridazine, pyranopyrazole, pyrazolopyrimidine, pyrazolothiazolopyrimidinone, thiazolopyrimidine, thienopyrazole and pyrazolothienopyrimidine derivatives. The antimicrobial study revealed that all the tested compounds showed moderate to good antimicrobial and antifungal activities against pathogenic strains. Authors’ contributions MAMA, SMB were responsible for the organic synthesis, and characterization experiments and department of Pharmacology, Faculty of Pharmacy, Mansoura University, Egypt for performing the antimicrobial evaluation. Both authors read and approved the final manuscript
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