Synthesis and characterization of selected fused isoxazole and pyrazole derivatives and their antimicrobial activity
Synthesis and characterization of selected fused isoxazole and pyrazole derivatives and their antimicrobial activity
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DOI：
10.2298/jsc0911219d
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发表时间：
2009-01-01
影响因子：
1
通讯作者：
Ansari, Faisal Y.
中科院分区：
文献类型：
--
作者：
Dabholkar, Vijay V.;Ansari, Faisal Y.
以5，5-二甲基环己烷-1，3-二酮（1）和3-[（4-氯亚苄基）氨基]-2-硫代咪唑烷-4-酮（2）为配体，合成了新的具有抗菌活性的稠合异恶唑和吡唑衍生物。芳香醛与I和2缩合，分别得到2-芳亚甲基-5，5-二甲基环己烷-1，3-二酮（3）和5-芳亚甲基-3-[（4-氯亚苄基）氨基]-2-硫代咪唑烷-4-酮（4）。化合物3和4与亲核试剂发生杂环化反应得到标题化合物。新合成的杂环化合物（5-8）基于其化学性质和光谱数据进行表征，并且发现其抑制金黄色葡萄球菌和白喉棒状杆菌。
New potent antibacterials, fused isoxazole and pyrazole derivatives, were synthesized using 5,5-dimethylcyclohexane-1,3-dione (1) and 3-[(4-chlorobenzylidene)amino]-2-thioxoimidazolidin-4-one (2) as synthons. Aromatic aldehydes on condensation with I and 2 gave 2-arylidene-5,5-dimethylcyclohexane-1,3-dione (3) and 5-arylidene-3-[(4-chlorobenzylidene)amino]-2-thioxoimidazolidin-4-one (4), respectively. Compounds 3 and 4 were forced to undergo heterocyclization reaction with nucleophilic reagents to give the title compounds. The newly synthesized heterocyles (5-8) were characterized based on their chemical properties and spectroscopic data, and were found to inhibit Staphylococcus aureus and Corynebacterium diphtheriae.