Foroughifar Naser, Karimi Beromi Somayeh, Pasdar Hoda, Shahi Masoumeh
Department of Chemistry, Tehran North Branch, Islamic Azad University, Tehran, Iran.
Iran J Pharm Res. 2017 Spring;16(2):596-601.
Heterocyclic compounds containing a pyrimidine nucleus are of special interests thanks to their applications in medicinal chemistry as they are the basic skeleton of several bioactive compounds such as antifungal, antibacterial, antitumor and antitubercular. As a part of our research in the synthesis of pyrimidine derivatives containing biological activities, some new tetrahydropyrimidine derivatives (1-10) were synthesized via Biginelli reaction using HCl or DABCO as a catalyst with good yields. All structures of products were confirmed by IR, H NMR and C NMR spectroscopy. The antibacterial activity of some synthesized compounds was investigated against (ATCC 6538), (ATCC 12228) (ATCC14579) (ATCC 25922), (ATCC 13883) and (PAO1) bacteria. Some of these compounds such as 8 and 10 exhibited a good to significant antibacterial activity.
含有嘧啶核的杂环化合物因其在药物化学中的应用而备受关注,因为它们是几种生物活性化合物(如抗真菌、抗菌、抗肿瘤和抗结核化合物)的基本骨架。作为我们合成具有生物活性的嘧啶衍生物研究的一部分,使用盐酸或1,4-二氮杂二环[2.2.2]辛烷作为催化剂,通过Biginelli反应合成了一些新的四氢嘧啶衍生物(1-10),产率良好。所有产物的结构均通过红外光谱、氢核磁共振光谱和碳核磁共振光谱得到证实。研究了一些合成化合物对金黄色葡萄球菌(ATCC 6538)、大肠杆菌(ATCC 12228)、枯草芽孢杆菌(ATCC14579)、肺炎克雷伯菌(ATCC 25922)、铜绿假单胞菌(ATCC 13883)和铜绿假单胞菌(PAO1)的抗菌活性。其中一些化合物,如8和10,表现出良好到显著的抗菌活性。