Synthesis of 2,5-disubstituted-1,4-benzoquinone derivatives as potential antimicrobial and cytotoxic agents

被引:0
|
作者
Hassan, MA [1 ]
Maslat, AO
Abussaud, M
Ahmed, IC
AlKofahi, AS
机构
[1] Jordan Univ Sci & Technol, Dept Med Chem & Pharmacognosy, Fac Pharm, Irbid, Jordan
[2] Yarmouk Univ, Dept Biol, Irbid, Jordan
[3] Univ Alexandria, Fac Pharm, Dept Pharmaceut Chem, Alexadria, Egypt
关键词
benzoquinone derivatives; synthesis; antimicrobial; cytotoxicity; mutagenicity;
D O I
10.1002/(SICI)1521-4184(199812)331:12<385::AID-ARDP385>3.3.CO;2-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A number of 2,5-disubstituted-1,4-benzoquinone derivatives were prepared and characterized by elemental analysis, infrared (LR), nuclear magnetic resonance ( H-NMR), and mass spectra (MS). These compounds and their synthetic precursors were evaluated for their in vitro antimicrobial and cytotoxic activity. The most potent antimicrobial compound was the thiadiazolyl derivative 4b, which was 2- to 4 times more active than the antimicrobial drug sulfathiazole. All the tested compounds were active in the Brine Shrimp Lethality (BS) Test. Compound 4e which was the most active in the BS test was also found to possess a significant cytotoxicity against two tumor cell lines. Some of the compounds were found to be mutagenic at relatively high concentration.
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页码:385 / 388
页数:4
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