Synthesis of pyrazole-4-carbaldehyde derivatives for …

In view of these particulars and by taking into account a modification on the quinolone nucleus can bring significant changes in pharmacological activities and can afford new classes of therapeutically active compounds for biomedical screening containing therapeutically active moieties pyrazole and quinolin-2-one and as part of our current studies in developing new antimicrobial agents containing quinoline () and 1H-pyrazole-4-carbaldehyde () derivatives, we report herein the synthesis of some new derivatives of 4-pyrazolyl-N-arylquinoline-2,5-dione (4al) via multicomponent reaction approach. The constitution of all the products was characterized using elemental analysis, FT-IR, 1H NMR, 13C NMR and mass spectrometry. All compounds were screened for in vitro antimicrobial activity against eight human pathogens, of which three were Gram-positive bacterial pathogens Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis, three were Gram-negative bacterial pathogens Salmonella typhi, Vibrio cholerae, Escherichia coli and two were fungal pathogens Aspergillus fumigatus and Candida albicans, using broth microdilution MIC method ().

Page 196 Pyrazole-3(4)-carbaldehyde: synthesis, reactions and biological activity Bakr F
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Conclusion: 3-(benzofuran-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde was utilized as key intermediate for the synthesis of some new heterocycles, namely 2,3-dihydro-1,3,4-thiadiazole, pyrazole and coumarin derivatives under both grinding and convenential conditions. Most of the newly synthesized products revealed moderate activity against the tested microorganisms.


A series of pyrazole-4-carbaldehyde ..

Vanelle, New pyrazolo [3,4-b] pyrazines: Synthesis and biological activity, Pharmazie, 55, 8, , 572, 2000
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A number of methods have been reported for the synthesis of dihydropyrano[2,3-c]pyranopyrazoles employing different catalysts such as ionic liquids , , organic bases , , , , amberlyst , glycine , per-6-amino-β-cyclodextrin , and iodine . Zonouz et al. have reported a one pot four component reaction under non-catalytic green synthesis of pyranopyrazole in water . Many recent reports have confirmed that pyranopyrazole derivatives are important class of heterocyclic compounds with natural and synthetic molecules . They exhibited numerous biological activities such as antimicrobial , , antibacterial , anticancer , analgesic and anti-inflammatory , properties. Pyrazole ring fused heterocycles have also been identified as anti HIV agents . Presence of pyran skeleton is central core in a number of natural products . In the area of catalytic transformations, organocatalysts are metal free simple organic molecules that are able to function as potent and selective catalyst for large transformations. -Proline is simple amino acid and its derivatives were effectively useful in much organic transformation, such as asymmetric aldol reaction , Mannich reaction and Michael reaction . Hence we have chosen -proline catalyst for this reaction condition.


of Pyrazole Derivatives Possessing Anticancer ..

In view of these particulars and by taking into account a modification on the quinolone nucleus can bring significant changes in pharmacological activities and can afford new classes of therapeutically active compounds for biomedical screening containing therapeutically active moieties pyrazole and quinolin-2-one and as part of our current studies in developing new antimicrobial agents containing quinoline () and 1H-pyrazole-4-carbaldehyde () derivatives, we report herein the synthesis of some new derivatives of 4-pyrazolyl-N-arylquinoline-2,5-dione (4al) via multicomponent reaction approach. The constitution of all the products was characterized using elemental analysis, FT-IR, 1H NMR, 13C NMR and mass spectrometry. All compounds were screened for in vitro antimicrobial activity against eight human pathogens, of which three were Gram-positive bacterial pathogens Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis, three were Gram-negative bacterial pathogens Salmonella typhi, Vibrio cholerae, Escherichia coli and two were fungal pathogens Aspergillus fumigatus and Candida albicans, using broth microdilution MIC method ().