Synthesis of new 2(1H)-quinoxalinone derivatives for antimicrobial and antiinflammatory evaluation

Faculty Pharmacy Year: 2009
Type of Publication: Article Pages: 782-797
Authors: DOI: 10.1007/s00044-009-9203-y
Journal: MEDICINAL CHEMISTRY RESEARCH BIRKHAUSER BOSTON INC Volume: 18
Research Area: Pharmacology \& Pharmacy ISSN ISI:000272617700007
Keywords : Antiinflammatory activity, Antimicrobial activity, 2(1H)-Quinoxalinones, Synthesis    
Abstract:
New 2(1H)-quinoxalinones and their hexahydro derivatives were prepared for investigating their antimicrobial and antiinflammatory activities. The study showed that thiosemicarbazide 6a derived from the hexahydro-2(1H)-quinoxalinone series has nearly the same antibacterial activity as the reference drug ciprofloxacin. Moreover, the 2(1H)-quinoxalinones bearing N-phenyltriazole (9a) or 4-chlorophenyl-2,3-dihydrothiazole (13b) moieties were the most active ones after 4 h with use of the rat hind paw edema method, whereas their antiinflammatory and ulcerogenic activities were comparable with the selective COX-2 inhibitor celecoxib.
   
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