Nagarajan Sangaraiah, Shanmugavelan Poovan, Sathishkumar Murugan, Selvi Ramasamy, Ponnuswamy Alagusundaram, Harikrishnan Hariharan, Shanmugaiah Vellasamy, Murugavel Saminathan
Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625 021, Tamilnadu, India.
Department of Organic Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625 021, Tamilnadu, India.
Bioorg Med Chem Lett. 2014 Nov 1;24(21):4999-5007. doi: 10.1016/j.bmcl.2014.09.027. Epub 2014 Sep 16.
A greener water mediated protocol for the efficient synthesis of a library of 2-amino-6-styryl pyrimidines (4) and their dihydro analogues (3) has been reported. Most of the saturated compounds (3) rather than their unsaturated analogues (4) showed better anti-bacterial (in vitro) activity against three human pathogens viz. Staphylococcus aureus, Klebsiella pneumonia and Escherichia coli. In particular, three of them (3 b, 3 i &3 k) exhibited high inhibition against the growth of all the three pathogens comparable with that of the reference drug, tetracycline.
据报道，一种更环保的水介导方法可高效合成2-氨基-6-苯乙烯基嘧啶（4）及其二氢类似物（3）库。大多数饱和化合物（3）而非其不饱和类似物（4）对三种人类病原体，即金黄色葡萄球菌、肺炎克雷伯菌和大肠杆菌，表现出更好的（体外）抗菌活性。特别是其中三种化合物（3b、3i和3k）对所有三种病原体的生长均表现出高抑制作用，与参考药物四环素相当。
