An efficient multi component reaction for the synthesis of new 3‐(2‐amino‐6‐arylpyrimidin‐4‐yl)‐4‐hydroxyquinolin‐2(1H)‐ones has been described. Synthesized derivatives were screened for their in vitro antimicrobial and 2, 2‐diphenyl‐1‐picrylhydrazyl (DPPH) scavenging activity. Among the tested compounds 3 k, 3 m and 3 r shown better antibacterial properties and have displayed broad spectrum of activity than Neomycin against Staphylococcus aureus, Bacillus cereus, Klebsiella planticola, Escherechia coli, S.aureus and Pseudomonas aeruginosa. Moreover 3 r, 3 t and 3 n were found to have potent antifungal activity against Candida parapsilosis, Candida albicans, Aspergillus niger, Candida glabrata, Issatchenkia hanoiensis and Candida than the standard Miconazole. Furthermore 3 c, 3 j, 3 d, 3 m, and 3 h showed strong DPPH free radical scavenging activity than Ascorbic acid.
Synthesis of 2-amino-6-(1, 2-dihydro-4-hydroxy-2-oxoquinolin-3-yl)-4-arylpyridine-3-carbonitrile has been accomplished via NbCl 5 catalysed multicomponent reaction (MCR). The tested compounds showed better potency than Neomycin and a broad spectrum of antibacterial activity against Staphylococcus aureus, Bacillus cereus and Escherichia coli. Similarly some of these have showed good activity against Staphylococcus aureus, Klebsiella planticola and Escherichia coli that were comparable to Ciprofloxacin. Also these compounds possess good antifungal activity that was better than Miconazole and comparable to Ciprofloxacin hydrochloride.
An effective and simple method for the synthesis of title compounds (IV) with phosphorus as additional chiral center is described and the antioxidant activities are examined.
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