Kang So Rang, Lee Yong Rok
School of Chemical Engineering, Yeungnam University, Gyeongsan, 712-749, Republic of Korea.
Mol Divers. 2015 May;19(2):293-304. doi: 10.1007/s11030-015-9568-4. Epub 2015 Feb 5.
Efficient one-pot three-component reactions of pyrazolones with arylaldehydes and triethyl phosphite were carried out in the presence of ethylenediammonium diacetate as catalyst to synthesize biologically interesting pyrazolylphosphonate derivatives. This methodology offers several significant advantages such as environmentally benign character, the use of a mild catalyst, high yields, and ease of handling. The synthesized compounds were screened for their antioxidant and antibacterial activities. The result showed that compound 4d [Formula: see text] exhibited a strong free radical scavenger toward DPPH free radicals compared with standard BHT [Formula: see text]. In addition, compounds 4e and 4p showed potent antibacterial activities against Gram-negative bacteria of E. coli and compound 4o exhibited a potent activity against Gram-positive bacteria of S. aureus compared with standard Ampicillin.
在乙二胺二乙酸盐作为催化剂的存在下，吡唑啉酮与芳醛和亚磷酸三乙酯进行了高效的一锅三组分反应，以合成具有生物学意义的吡唑基膦酸酯衍生物。该方法具有几个显著优点，如环境友好性、使用温和的催化剂、高收率和易于操作。对合成的化合物进行了抗氧化和抗菌活性筛选。结果表明，与标准抗氧化剂丁基羟基甲苯（BHT）相比，化合物4d[化学式：见原文]对二苯基苦味酰基自由基（DPPH自由基）表现出较强的自由基清除能力。此外，与标准氨苄青霉素相比，化合物4e和4p对革兰氏阴性菌大肠杆菌显示出强效抗菌活性，化合物4o对革兰氏阳性菌金黄色葡萄球菌表现出强效活性。
