Exploration of antimicrobial potential of pyrazolo[3,4- b ]pyridine scaffold bearing benzenesulfonamide and trifluoromethyl moieties

Medicinal Chemistry Research(2013)

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摘要
The synthesis and biological evaluation of a library of thirty differently substituted pyrazolo[3,4- b ]pyridines bearing benzenesulfonamide moiety at position-1 and trifluoromethyl group at position-4 are reported. Fused heterocyclic system present in the target compounds ( 5a – j , 6a – j , and 7a – j ) was constructed by refluxing various 5-aminopyrazoles ( 3a – c ) with differently substituted trifluoromethyl- β -diketones ( 4a – j ) in glacial acetic acid. All the target compounds ( 5 – 7 ) were evaluated for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus , Bacillus subtilis (Gram-positive), Escherichia coli , Pseudomonas aeruginosa (Gram-negative) and in vitro antifungal activity against two pathogenic fungal yeasts namely, Saccharomyces cerevisiae and Candida albicans . Graphical Abstract Thirty differently substituted pyrazolo[3,4- b ]pyridines bearing benzenesulfonamide moiety at position-1 and trifluoromethyl group at position-4 were synthesized and screened for antibacterial and antifungal activities.
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关键词
Pyrazolo[3,4-b]pyridines,Benzenesulfonamide,Trifluoromethyl-β-diketones,Antibacterial activity,Antifungal activity
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