Cyanoacetamide based Barbiturates, Thiobarbiturates and their Biological Studies
JOURNAL OF THE CHEMICAL SOCIETY OF PAKISTAN(2015)
Abstract
Various cyanoacetamide based Knoevenagel adducts were coupled with barbituric acid / thiobarbituric acid and triethylorthoformate via a one pot three component reaction in 2-butanol availing the desired compound in excellent yields. All the synthesized compounds (2-15) were extensively characterized by H-1-NMR, C-13-NMR, Mass spectrometry and elemental analysis and were screened for antibacterial, antiurease, antioxidant, cytotoxicity and chymotrypsin inhibition studies. In case of antibacterial studies 2 was found appreciably active against the six selected strains whereas the rest of the compounds were moderately active. The urease inhibition studies revealed compound 5 and 12 as potent whereas the rest were found inactive where thiourea was used as control. Antioxidant activity results exhibited with 2 as the most active and rest of compounds showed good activity. In case of chymotrypsin inhibition studies all the synthesized compounds were found inactive with the exception of 6 which was moderately active.
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Key words
Knoevenagel Adduct,Barbituric acid,Thiobarbituric acid,Urease Inhibition,Antioxidant and Chymotrypsin
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