Ravi Kantha S, Venkat Reddy G, Hara Kishore K, Shanthan Rao P, Narsaiaha B, Surya Narayana Murthy U
Fluoroorganics Division, Indian Institute of Chemical Technology, Hyderabad, India.
Eur J Med Chem. 2006 Aug;41(8):1011-6. doi: 10.1016/j.ejmech.2006.03.028.
Novel pyrido[2,3-d]pyrimidines 4 have been synthesised starting from 2-amino-4-trifluoromethyl-6-substituted nicotinonitriles 1 via imine formation, selective amination followed by Dimroth rearrangement. Compounds 4 were screened against Gram +ve and -ve bacteria in vitro. Compounds 4h and 4d showed significant activity against all species of Gram positive bacteria and moderate activity against Gram negative bacteria. N-2,4 difluorophenyl compounds 4l and 4m were the least active among all the compounds. All the compounds were inactive against Pseudomonas aeruginosa at the maximum concentration of 200 microg ml(-1).
新型吡啶并[2,3 - d]嘧啶4是从2 - 氨基 - 4 - 三氟甲基 - 6 - 取代烟腈1开始合成的,通过形成亚胺、选择性胺化,然后进行迪姆罗特重排。化合物4在体外针对革兰氏阳性菌和阴性菌进行了筛选。化合物4h和4d对所有革兰氏阳性菌均表现出显著活性,对革兰氏阴性菌表现出中等活性。N - 2,4 - 二氟苯基化合物4l和4m在所有化合物中活性最低。所有化合物在最大浓度200微克/毫升(-1)时对铜绿假单胞菌均无活性。