Synthesis of new 2-substituted pyrido[2,3-d]pyrimidin-4(1H)-ones and their antibacterial activity☆
作者:B. Lakshmi Narayana、A. Raghu Ram Rao、P. Shanthan Rao
DOI:10.1016/j.ejmech.2008.05.025
日期:2009.3
2-Substituted-5,7-dimethyl pyrido[2,3-d]pyrimidin-4(1H)-ones (8) were synthesized by oxidation of 2-substituted-5,7-dimethyl dihydropyrido[2,3-d]pyrimidin-4(1H)-ones (7) which were in turn prepared from 2-amino-4,6-dimethyl nicotinamide (5) and substituted aryl aldehydes (6). 2-Amino-4,6-dimethyl nicotinamide (5) was prepared from ethyl cyanoacetate (1) via malonamamidine hydrochloride (3). The compounds
2-取代的-5,7-二甲基吡啶并[2,3- d ]嘧啶-4(1 ħ) -酮(8)通过2-取代-5,7-二甲基二氢吡啶氧化并[2,3-合成d ]嘧啶-4(1 H)-一(7),其依次由2-氨基-4,6-二甲基烟酰胺(5)和取代的芳基醛(6)制备。由氰基乙酸乙酯(1)通过丙二酸ama丙啶(3)制备2-氨基-4,6-二甲基烟酰胺(5)。通过IR,NMR,MS和元素分析对化合物进行表征。化合物7和8筛选针对革兰氏阳性和阴性细菌的抗菌活性。脱氢化合物(8)的抗菌活性低于化合物7。在所有筛选的具有抗菌活性的化合物中,7c(1.25μg/ ml)表现出更高的活性。当在200μg/ ml的浓度下筛选抗真菌活性时,发现所有合成的化合物均无活性。