Chandrasekaran S, Nagarajan S
Department of Chemistry, Annamalai University, Annamalai Nagar-608 002, India.
Farmaco. 2005 Apr;60(4):279-82. doi: 10.1016/j.farmac.2005.01.012.
Some novel 2-amino-6-aryl-4-(2-thienyl)pyrimidines were synthesized from 3-aryl-1-thien-2-ylprop-2-en-1-ones and guanidine hydrochloride in presence of alkali by conventional heating in alcoholic medium and microwave heating in solvent-free conditions. The compounds were evaluated for in vitro anti-bacterial activity. The anti-bacterial data revealed that compounds 5a-e had better activity against tested gram-positive organisms than the reference ciprofloxacin and norfloxacin. However, the compounds were nearly inactive against gram-negative bacteria. Compounds 5c and e were the most active compounds against gram-positive bacteria.
一些新型的2-氨基-6-芳基-4-(2-噻吩基)嘧啶是通过在碱性条件下，使3-芳基-1-噻吩-2-基丙-2-烯-1-酮与盐酸胍在醇介质中常规加热以及在无溶剂条件下微波加热合成的。对这些化合物进行了体外抗菌活性评估。抗菌数据表明，化合物5a - e对测试的革兰氏阳性菌的活性优于参考药物环丙沙星和诺氟沙星。然而，这些化合物对革兰氏阴性菌几乎没有活性。化合物5c和e是对革兰氏阳性菌活性最高的化合物。
