Valadbeigi Edris, Ghodsi Shahram
Department of Chemistry, Faculty of Sciences, Islamic Azad University, Karaj Branch, Karaj, Iran.
Iran J Pharm Res. 2017 Spring;16(2):554-564.
A series of N-[2-(8-metoxy-2H-chromen-2-one)ethyl] piperazinyl quinolones containing a carbonyl related functional groups (oxo or oxyimino) on the ethyl spacer of coumarin and piperazin rings was synthesized and studied for their antibacterial and antifungal activities . The synthesis of compounds (6a-6l) was achieved through the versatile and efficient synthetic route that involved reaction of quinolones with appropriately α- bromo ketone or α- bromo oxime derivatives (2, 2a-c). The structures of the new compounds were confirmed by IR, Mass, H-NMR and C-NMR spectra. More good activities against gram-positive and gram-negative are shown in all compounds. The antifungal data reveals that all compounds have shown weak antifungal activity as compared to Nistatin.
合成了一系列在香豆素的乙基间隔基和哌嗪环上含有与羰基相关的官能团(氧代或氧亚氨基)的N-[2-(8-甲氧基-2H-色烯-2-酮)乙基]哌嗪基喹诺酮类化合物,并对其抗菌和抗真菌活性进行了研究。化合物(6a-6l)的合成是通过通用且高效的合成路线实现的,该路线涉及喹诺酮与适当的α-溴代酮或α-溴代肟衍生物(2, 2a-c)反应。通过红外光谱、质谱、氢核磁共振谱和碳核磁共振谱确认了新化合物的结构。所有化合物对革兰氏阳性菌和革兰氏阴性菌均表现出较好的活性。抗真菌数据表明,与制霉菌素相比,所有化合物的抗真菌活性均较弱。