Shahi Masoume, Foroughifar Naser, Mobinikhaledi Akbar
Department of Chemistry, Tehran North Branch, Islamic Azad University, Tehran, Iran.
Department of Chemistry, Faculty of Science, Arak University, , 38156-8-8349, Arak, Iran.
Iran J Pharm Res. 2015 Summer;14(3):757-63.
There has been special interest in the chemistry of quinolone and pyrimidine derivatives due to their diverse biological activities such as anticonvulsant, anti-malarial agents, antibacterial, antiviral, cytostatic, antithelemintic, antigenotoxic, anti-cancer agents. These compounds are also used as targeting delayed-type hypersensivity and anti-convulsant agents. As a part of our research works in the synthesis of pyrimidine derivatives containing biological activities, a series of novel pyrano[2,3-d]pyrimidine derivatives 2 and tetrahydro quinolone dione derivatives 3 were synthesized via reaction of tetrahydrobenzo[b]pyrano derivatives 1 with different reagents in suitable yields. The characterization of these synthesized compounds was established by IR, (1)H NMR and (13)C NMR spectroscopic data. Furthermore, all compounds were subsequently evaluated for their in-vitro antibacterial activity against three bacteria: Staphylococcus aureus (ATTC-25923), Escherichia Coli (ATTC-25922) and Bacillus anthracic (ATTC-25924).
由于喹诺酮和嘧啶衍生物具有多种生物活性,如抗惊厥、抗疟疾、抗菌、抗病毒、抑制细胞生长、抗蠕虫、抗遗传毒性、抗癌等,因此人们对它们的化学性质产生了特别的兴趣。这些化合物还被用作靶向迟发型超敏反应和抗惊厥剂。作为我们合成具有生物活性的嘧啶衍生物研究工作的一部分,通过四氢苯并[b]吡喃衍生物1与不同试剂反应,以合适的产率合成了一系列新型吡喃并[2,3 - d]嘧啶衍生物2和四氢喹诺酮二酮衍生物3。这些合成化合物的表征通过红外光谱、氢核磁共振光谱和碳核磁共振光谱数据确定。此外,随后对所有化合物针对三种细菌进行了体外抗菌活性评估:金黄色葡萄球菌(ATTC - 25923)、大肠杆菌(ATTC - 25922)和炭疽芽孢杆菌(ATTC - 25924)。