Synthesis, antioxidant and toxicological study of novel pyrimido quinoline derivatives from 4-hydroxy-3-acyl quinolin-2-one

被引:95
作者
Sankaran, Mathan [1 ]
Kumarasamy, Chandraprakash [1 ]
Chokkalingam, Uvarani [1 ]
Mohan, Palathurai Subramaniam [1 ]
机构
[1] Bharathiar Univ, Dept Chem, Sch Chem Sci, Coimbatore 641046, Tamil Nadu, India
关键词
Pyrimido; Triazepine quinolines; Antioxidant activities; Toxicity; BIGINELLI REACTION; CRYPTOSANGUINOLENTINE; MECHANISM; SYSTEMS;
D O I
10.1016/j.bmcl.2010.09.018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel pyrimido and other fused quinoline derivatives like 4-methyl pyrimido [5,4-c]quinoline-2,5(1H,6H)-dione (4a), 4-methyl-2-thioxo-1,2-dihydropyrimido [5,4-c]quinoline-5(6H)-one (4b), 2-amino-4-methyl-1,2-dihydropyrimido [5,4-c]quinolin-5(6H)-one (4c), 3-methylisoxazolo [4,5-c]quinolin-4(5H)-one (4d), 3-methyl-1H-pyrazolo [4,3-c]quinoline-4(5H)-one (5e), 5-methyl-1H-[1,2,4] triazepino [6,5-c]quinoline-2,6(3H,7H)-dione (5f), 5-methyl-2-thioxo-2,3-dihydro-1H-[1,2,4]triazepino [6,5-c]quinolin-6(7H)one (5g) were synthesized regioselectively from 4-hydroxy-3-acyl quinolin-2-one 3. They were screened for their in vitro antioxidant activities against radical scavenging capacity using DPPH, Trolox equivalent antioxidant capacity (TEAC), total antioxidant activity by FRAP, superoxide radical (O-2(degrees-)) scavenging activity, metal chelating activity and nitric oxide scavenging activity. Among the compounds screened, 4c and 5g exhibited significant antioxidant activities. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:7147 / 7151
页数:5
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