US EPA

7479519 

Journal Article 

Synthesis and bio-activity evaluation of carbamate and sulfonamide derivatives of febuxostat 

Vedavathi, P; Naga Raju, C 

2013 

5 

6 

106-110 

English 

Febuxostat was modified as their carbamates and sulfonamides by the reaction of Febuxostat with hydrazine followed by various Chloroformates/sulfonylchlorides in the presence of triethylamine at 40-45°C in THF. The newly synthesized compounds were characterized by IR, NMR (1H &13C), LCMS and C, H, N elemental analysis. Antimicrobial screening of all the title compounds demonstrating the compounds exhibited good activity. 

Antimicrobial activity; Carbamate; Febuxostat; Sulfonamide; 2,2,2 trichloroethyl 2 [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]hydrazinecarboxylate; 3 chloro n' [2 (3 cyano isobutoxyphenyl) 4 methylthiazole 5 carbonyl] 4 fluorobenzenesulfonohydrazide; 4 bromo n' [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]benzenesulfonohydrazide; 4 chloro n' [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl] 3 nitrobenzenesulfonohydrazide; 4 nitrobenzyl 2 [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]hydrazinecarboxylate; 4 nitrophenyl 2 [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]hydrazinecarboxylate; antiinfective agent; carbamic acid derivative; carbon; chloride; chloroform; febuxostat; gatifloxacin; hydrazine; hydrogen; isobutyl 2 [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]hydrazinecarboxylate; methyl 2 [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl]hydrazine carboxylate; n' [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl] 4 fluorobenzenesulfonohydrazide; n' [2 (3 cyano 4 isobutoxyphenyl) 4 methylthiazole 5 carbonyl] 4 nitrobenzenesulfonohydrazide; nitrogen; sulfonamide; triethylamine; unclassified drug; antimicrobial activity; article; Bacillus subtilis; biological activity; carbon nuclear magnetic resonance; drug screening; drug structure; drug synthesis; Escherichia coli; infrared spectroscopy; Klebsiella pneumoniae; liquid chromatography; mass spectrometry; nonhuman; proton nuclear magnetic resonance; Staphylococcus aureus; structure analysis; temperature measurement