Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ein Helwan, Cairo 11795, Egypt.
Eur J Med Chem. 2013 Nov;69:591-600. doi: 10.1016/j.ejmech.2013.08.032. Epub 2013 Sep 15.
A series of 6-aryl-5-cyano thiouracil derivatives (2a-c to 11a-c) was synthesized from 6-aryl-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-carbonitriles (1a-c). The products were characterized by analytical and spectral data (IR, (1)H NMR, (13)C NMR and mass spectra). All compounds were screened for their in-vitro antibacterial and antifungal activities. Compounds 7a, 7g and 9a-c showed pronounced antimicrobial activity than standards. Some of the newly synthesized compounds were evaluated for antioxidant activity. Compounds 1c, 5c and 8c displayed promising free radical scavenging activity and found to be more potent than standard, ascorbic acid (vitamin C).
从 6-芳基-4-肼基-2-硫代-1,2-二氢嘧啶-5-甲腈(1a-c)合成了一系列 6-芳基-5-氰基硫代尿嘧啶衍生物(2a-c 至 11a-c)。产物通过分析和光谱数据(IR、(1)H NMR、(13)C NMR 和质谱)进行了表征。所有化合物均进行了体外抗菌和抗真菌活性筛选。化合物 7a、7g 和 9a-c 显示出比标准品更显著的抗菌活性。一些新合成的化合物被评估了抗氧化活性。化合物 1c、5c 和 8c 表现出有希望的自由基清除活性,并且发现比标准品抗坏血酸(维生素 C)更有效。